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Polymers and Drug Delivery
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Polymers and Drug Delivery

A special issue of Polymers (ISSN 2073-4360). This special issue belongs to the section "Polymer Applications".

Deadline for manuscript submissions: closed (20 March 2023) | Viewed by 53181

Special Issue Editor

Prof. Dr. Stanislaw Slomkowski

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Guest Editor
Department of Engineering of Polymer Materials, Centre of Molecular and Macromolecular Studies of Polish Academy of Sciences, 90-363 Lodz, Poland
Interests: fundamental and applied studies on polymer nanoparticles; microparticles; and related materials for medical applications, in particular for medical diagnostics and drug delivery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Polymers are commonly used for drug delivery; a hydrosoluble polymer can be used as a carrier for a drug to enhance its dissolution rate. Contrariwise, controlled or sustained drug release obtained with the aid of hydrophobic polymers can be used to extend the active principle release, reducing the number of administrations. In medicine, functional nanocarriers are used as basic elements of smart drug-delivery systems, ensuring the transportation of bioactive substances to designated tissues, cells, and intracellular compartments.

This Special Issue shall gather original and review papers that mainly discuss achievements in polymeric drug-delivery systems. We hope that the papers of this Issue will inspire researchers in their own work.

Prof. Dr. Stanislaw Slomkowski
Guest Editor

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22 pages, 2702 KiB  
Article
Development and Evaluation of an Innovative Approach Using Niosomes Based Polymeric Microneedles to Deliver Dual Antioxidant Drugs
by Ahlam Zaid Alkilani, Hadeel Abo-Zour, Haneen A. Basheer, Hana Abu-Zour and Ryan F. Donnelly
Polymers 2023, 15(8), 1962; https://0-doi-org.brum.beds.ac.uk/10.3390/polym15081962 - 20 Apr 2023
Cited by 4 | Viewed by 1960
Abstract
Ascorbic acid (AA) and caffeine (CAFF) work to protect cells from ultraviolet (UV) radiation and slow down the photoaging process of the skin. However, cosmetic application of AA and CAFF is limited due to poor penetration across the skin and rapid oxidation of [...] Read more.
Ascorbic acid (AA) and caffeine (CAFF) work to protect cells from ultraviolet (UV) radiation and slow down the photoaging process of the skin. However, cosmetic application of AA and CAFF is limited due to poor penetration across the skin and rapid oxidation of AA. The aim of this study was to design and evaluate the dermal delivery of dual antioxidants utilizing microneedles (MNs) loaded with AA and CAFF niosomes. The niosomal nanovesicles were prepared using the thin film method and had particle sizes ranging from 130.6–411.2 nm and a negative Zeta potential of around −35 mV. The niosomal formulation was then combined with polyvinylpyrrolidone (PVP) and polyethylene glycol 400 (PEG 400) to create an aqueous polymer solution. The best skin deposition of AA and CAFF was achieved with the formulation containing 5% PEG 400 (M3) and PVP. Furthermore, the role of AA and CAFF as antioxidants in preventing cancer formation has been well-established. Here we validated the antioxidant properties of ascorbic acid (AA) and caffeine (CAFF) in a novel niosomal formulation referred to as M3 by testing its ability to prevent H2O2-indued cell damage and apoptosis in MCF-7 breast cancer cells. Results showed that M3 was able to shield MCF-7 cells from H2O2 induced damage at concentrations below 2.1 µg/mL for AA and 1.05 µg/mL for CAFF, and also exhibited anticancer effects at higher concentrations of 210 µg/mL for AA and 105 µg/mL. The formulations were stable for two months at room temperature in terms of moisture and drug content. The use of MNs and niosomal carriers could be a promising approach for dermal delivery of hydrophilic drugs like AA and CAFF. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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14 pages, 9438 KiB  
Article
Quaternary Ammonium-Tethered Phenylboronic Acids Appended Supramolecular Nanomicelles as a Promising Bacteria Targeting Carrier for Nitric Oxide Delivery
by Yu Fang, Haiyan Cui, Xiaoqin Liang, Jianping Yu, Jianrong Wang and Guanghui Zhao
Polymers 2022, 14(20), 4451; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14204451 - 21 Oct 2022
Cited by 2 | Viewed by 1339
Abstract
The delivery of drugs to focal sites is a central goal and a key challenge in the development of nanomedicine carriers. This strategy can improve the selectivity and bioavailability of the drug while reducing its toxicity. To ensure the specific release of nitric [...] Read more.
The delivery of drugs to focal sites is a central goal and a key challenge in the development of nanomedicine carriers. This strategy can improve the selectivity and bioavailability of the drug while reducing its toxicity. To ensure the specific release of nitric oxide at the site of a bacterial infection without damaging the surrounding normal tissue, we designed a host-guest molecule containing a host molecule with a target moiety and a nitric oxide donor to release nitric oxide. The boronic acid group in the structure of this nanoparticle interacts strongly and specifically with the surface of E. coli. In addition, the quaternary amine salt can interact electrostatically with bacteria, indicating a large number of negatively charged cell membranes; altering the molecular structure of the cell membrane; increasing the permeability of the cell membrane; and causing cytoplasmic diffusion and cell lysis, resulting in lethal activity against most bacteria. The synthesised molecules were characterised by 1H NMR and mass spectrometry. The strong specific interaction of the boronic acid moiety with the surface of E. coli and the electrostatic interaction of the quaternary amine salt with the cell membrane were confirmed by antibacterial experiments on molecules with and without the targeting moiety. The targeting group-modified micelles enhanced the antibacterial effect of the micelles very effectively through specific interactions and electrostatic interactions. In addition, in vitro skin wound healing experiments also confirmed the targeting and antimicrobial effect of micelles. These results suggest that the specific release of nitric oxide at the site of bacterial infection is an important guide to further address the emergence of antibiotic-resistant strains of bacteria. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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14 pages, 4228 KiB  
Article
Formulation and Evaluation of Fenbendazole Extended-Release Extrudes Processed by Hot-Melt Extrusion
by Gilberto S. N. Bezerra, Tielidy A. de M. de Lima, Declan M. Colbert, Joseph Geever and Luke Geever
Polymers 2022, 14(19), 4188; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14194188 - 06 Oct 2022
Cited by 5 | Viewed by 1802
Abstract
This study aimed to demonstrate the feasibility of hot-melt extrusion in the development of extended-release formulations of Fenbendazole (Fen) dispersed in PEO/PCL blend-based matrices. Their thermal, physical, chemical and viscosity properties were assessed by differential scanning calorimetry, thermogravimetric analysis/derivative thermogravimetry, Fourier transform infrared [...] Read more.
This study aimed to demonstrate the feasibility of hot-melt extrusion in the development of extended-release formulations of Fenbendazole (Fen) dispersed in PEO/PCL blend-based matrices. Their thermal, physical, chemical and viscosity properties were assessed by differential scanning calorimetry, thermogravimetric analysis/derivative thermogravimetry, Fourier transform infrared spectroscopy, X-ray diffraction spectroscopy, and melt flow index. Drug dispersion was analyzed by scanning electron microscopy with electron dispersive X-ray spectroscopy, and drug release was evaluated by ultraviolet-visible spectroscopy. A thermal analysis indicated the conversion of the drug to its amorphous state. FTIR analysis endorsed the thermal studies pointing to a decrease in the drug’s crystallinity with the establishment of intermolecular interactions. XRD analysis confirmed the amorphous nature of Fen. MFI test revealed that PCL acts as a plasticizer when melt-processed with PEO. SEM images displayed irregular surfaces with voids and pores, while EDX spectra demonstrated a homogeneous drug distribution throughout the polymeric carrier. Dissolution testing revealed that PCL retards the drug release proportionally to the content of such polymer incorporated. These melt-extruded matrices showed that the drug release rate in a PEO/PCL blend can easily be tailored by altering the ratio of PCL to address the issues related to the multiple-dosing regimen of Fen in ruminants. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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27 pages, 8671 KiB  
Article
Design and Engineering of Natural Cellulose Fiber-Based Biomaterials with Eucalyptus Essential Oil Retention to Replace Non-Biodegradable Delivery Systems
by Flávia P. Morais and Joana M. R. Curto
Polymers 2022, 14(17), 3621; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14173621 - 01 Sep 2022
Cited by 3 | Viewed by 1854
Abstract
This work aims at the design and engineering of sustainable biomaterials based on natural fibers to replace non-renewable fiber sources in the development of non-woven delivery systems. Cellulose fibers were used as the main support to produce multi-structured materials with the incorporation of [...] Read more.
This work aims at the design and engineering of sustainable biomaterials based on natural fibers to replace non-renewable fiber sources in the development of non-woven delivery systems. Cellulose fibers were used as the main support to produce multi-structured materials with the incorporation of microfibrillated cellulose (MFC) as an additive. A 3D carboxymethylcellulose matrix retaining a natural bioactive product, eucalyptus essential oil, (CMC/EO), with controlled release functionalities, was also applied to these materials using bulk and spray coating methodologies. Additionally, using a 3D modeling and simulation strategy, different interest scenarios were predicted to design new formulations with improved functional properties. Overall, the results showed that MFC provided up to 5% improved strength (+48%) at the expense of reduced softness (−10%) and absorbency (−13%) and presented a good potential to be used as an additive to maximize natural eucalyptus fibers content in formulations. The addition of CMC/EO into formulations’ bulk revealed better strength properties (21–28%), while its surface coating improved absorption (23–25%). This indicated that both application methods can be used in structures proposed for different sustainable applications or a more localized therapy, respectively. This optimization methodology consists of a competitive benefit to produce high-quality functionalized biomaterials for added-value applications. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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15 pages, 6148 KiB  
Article
Ammonio Methacrylate Copolymer (Type B)-Diltiazem Interactions in Solid Dispersions and Microsponge Drug-Delivery Systems
by Iliyan Kolev, Nadezhda Ivanova, Tanya Topouzova-Hristova, Tanya Dimova, Pavlina Koseva, Ivalina Vasileva, Sonya Ivanova, Anton Apostolov, Gergana Alexieva, Atanas Tzonev and Vesselin Strashilov
Polymers 2022, 14(10), 2125; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14102125 - 23 May 2022
Viewed by 1853
Abstract
This paper presents a complex analytical study on the distribution, solubility, amorphization, and compatibility of diltiazem within the composition of Eudragit RS 100-based particles of microspongeous type. For this purpose, a methodology combining attenuated total reflectance Fourier transform infrared (ATR-FTIR) absorption spectroscopy, differential [...] Read more.
This paper presents a complex analytical study on the distribution, solubility, amorphization, and compatibility of diltiazem within the composition of Eudragit RS 100-based particles of microspongeous type. For this purpose, a methodology combining attenuated total reflectance Fourier transform infrared (ATR-FTIR) absorption spectroscopy, differential scanning calorimetry (DSC), scanning electron microscopy with energy-dispersive X-ray microanalysis (SEM-EDX), and in vitro dissolution study is proposed. The correct interpretation of the FTIR and drug-dissolution results was guaranteed by the implementation of two contrasting reference models: physical drug–polymer mixtures and casting-obtained, molecularly dispersed drug–polymer composites (solid dispersions). The spectral behavior of the drug–polymer composites in the carbonyl frequency (νCO) region was used as a quality marker for the degree of their interaction/mutual solubility. A spectral-pattern similarity between the microsponge particles and the solid dispersions indicated the molecular-type dispersion of the former. The comparative drug-desorption study and the qualitative observations over the DSC and SEM-EDX results confirmed the successful synthesis of a homogeneous coamorphous microsponge-type formulation with excellent drug-loading capacity and “controlled” dissolution profile. Among them, the drug-delivery particles with 25% diltiazem content (M-25) were recognized as the most promising, with the highest population of drug molecules in the polymer bulk and the most suitable desorption profile. Furthermore, an economical and effective analytical algorithm was developed for the comprehensive physicochemical characterization of complex delivery systems of this kind. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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13 pages, 6003 KiB  
Article
Sustained and Microenvironment-Accelerated Release of Minocycline from Alginate Injectable Hydrogel for Bacteria-Infected Wound Healing
by Chengjia Xie, Qun Zhang, Zhao Li, Shaohua Ge and Baojin Ma
Polymers 2022, 14(9), 1816; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14091816 - 29 Apr 2022
Cited by 9 | Viewed by 2374
Abstract
During wound healing, bacterial infection is one of the main limiting factors for the desired efficiency. Wound dressing-mediated antibiotics therapies could overcome this problem to a great extent due to sustained drug release and controllable dose. Here, we designed a kind of alginate [...] Read more.
During wound healing, bacterial infection is one of the main limiting factors for the desired efficiency. Wound dressing-mediated antibiotics therapies could overcome this problem to a great extent due to sustained drug release and controllable dose. Here, we designed a kind of alginate injectable hydrogel loaded with minocycline (SA@MC) as a dressing for staphylococcus aureus-infected wound healing. SA@MC hydrogel possessed good injectability and can be injected by syringes. MC participated in the gel formation, causing the microstructure change based on the morphology characterization. The element mapping and FT-IR spectra further confirmed the successful loading of MC in SA hydrogel. Interestingly, MC was released more efficiently in a weakly alkaline condition (pH 7–8) than in a weakly acidic condition (pH 4–6) from SA@MC injectable hydrogel, which means that there is an accelerated release to respond to the weakly alkaline wound microenvironment. Meanwhile, SA@MC injectable hydrogel had high biocompatibility and excellent antibacterial activity due to the sustained release of MC. Further, in vivo experiment results demonstrated that SA@MC injectable hydrogel promoted staphylococcus aureus-infected wound healing efficiently. In summary, the injectable composite hydrogel can serve as an ideal dressing to prevent bacterial infection and promote wound healing. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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12 pages, 1573 KiB  
Article
Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach
by Barkat Ali Khan, Maryam Waheed, Khaled M. Hosny, Waleed Y. Rizg, Samar S. Murshid, Majed Alharbi and Muhammad Khalid Khan
Polymers 2022, 14(7), 1489; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14071489 - 06 Apr 2022
Cited by 1 | Viewed by 1809
Abstract
Kojic acid (KA) is a BCS class II drug having low solubility and high permeability. This study was designed to enhance the aqueous solubility of KA, as well as its dissolution rate and, in turn, bioavailability, by formulating its smart nanocrystals. Nanocrystals of [...] Read more.
Kojic acid (KA) is a BCS class II drug having low solubility and high permeability. This study was designed to enhance the aqueous solubility of KA, as well as its dissolution rate and, in turn, bioavailability, by formulating its smart nanocrystals. Nanocrystals of pure KA were formulated by the top-down method under high-pressure homogenization followed by freeze drying. The nanocrystals were evaluated for stability and other physical characteristics, including zeta sizer analysis, DSC, surface morphology, XRD, drug content, solubility, FTIR and in vitro drug release. The KA nanocrystals were found to be stable when kept at exaggerated conditions. The particle size of the nanocrystals was 137.5 ± 1.7, 150 ± 2.8, and 110 ± 3.0 nm for the F1, F2 and F3 formulations, respectively. There was negative zeta potential for all the formulations. The dispersity index was 0.45 ± 0.2, 0.36 ± 0.4 and 0.41 ± 1.5 for the F1, F2 and F3, respectively. The DSC studies showed that there was no interaction between the KA and the excipients of the nanocrystals. The morphological studies confirmed the presence of rough crystalline surfaces on the nanosized particles. XRD studies showed the successful preparation of nanocrystals. The drug content was in the official range of 90 ± 10%. The solubility of KA was significantly (p < 0.05) enhanced in the formulations of its nanocrystals as compared with pure KA powder. The ATR-FTIR studies revealed the presence of functional groups in both KA and KA-loaded nanocrystals, and no interaction was found between them. The nanocrystals released 83.93 ± 1.22% of KA in 24 h. The study concluded that the nanocrystals were successfully formulated using the top-down method followed by high-pressure homogenization. The solubility, as well as the dissolution, of the KA was enhanced, and this could improve the therapeutic effects of KA. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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29 pages, 6721 KiB  
Article
A Novel Aminomethacrylate-Based Copolymer for Solubility Enhancement—From Radical Polymer Synthesis to Manufacture and Characterization of Amorphous Solid Dispersions
by Fabian-Pascal Schmied, Alexander Bernhardt, Christian Moers, Christian Meier, Thomas Endres and Sandra Klein
Polymers 2022, 14(7), 1281; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14071281 - 22 Mar 2022
Cited by 4 | Viewed by 2000
Abstract
The present study covers the synthesis, purification and evaluation of a novel aminomethacrylate-based copolymer in terms of its suitability for improving the solubility and in vitro release of poorly water-soluble drug compounds. The new copolymer was synthesized by solvent polymerization with radical initiation [...] Read more.
The present study covers the synthesis, purification and evaluation of a novel aminomethacrylate-based copolymer in terms of its suitability for improving the solubility and in vitro release of poorly water-soluble drug compounds. The new copolymer was synthesized by solvent polymerization with radical initiation and by use of a chain transfer agent. Based on its composition, it can be considered as a modified type of dimethylaminoethyl methacrylate-butyl methacrylate-methyl methacrylate “EUDRAGIT® E PO” (ModE). ModE was specifically developed to provide a copolymer with processing and application properties that exceed those of commercially available (co-)polymers in solubility enhancement technologies where possible. By varying the concentration of the chain transfer agent in the radical polymerization process, the molecular weight of ModE was varied in a range of 173–305 kDa. To evaluate the solubility-enhancing properties of ModE, a series of drug-loaded extrudates were prepared by hot melt extrusion using the novel—as well as several commercially available—(co-)polymers. These extrudates were then subjected to comparative tests for amorphousness, solubility-enhancing properties, storage stability, and drug release. Celecoxib, efavirenz, and fenofibrate were used as model drugs in all experiments. Of all the (co-)polymers included in the study, ModE with a molecular weight of 173 kDa showed the best performance in terms of desired properties and was shown to be particularly suitable for preparing amorphous solid dispersions (ASDs) of the three model drugs, which in a first set of dissolution experiments showed better release behavior under pH conditions of the fasting stomach than higher molecular weight ModE types, as well as a variety of commercially available (co-)polymers. Therefore, the results demonstrate the successful synthesis of a new copolymer, which in future studies will be investigated in more detail for universal application in the field of solubility enhancement. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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13 pages, 2256 KiB  
Article
Automatic Detoxification Medicine Delivery by Thermo-Sensitive Poly(ethylene glycol)-Based Nanogels
by Ting Fu, Jing Shen, Yuting Meng, Jun Wang, Siping Wang, Yuhui Zhang, Tongwen Wang and Xufeng Zhang
Polymers 2022, 14(5), 892; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14050892 - 24 Feb 2022
Cited by 1 | Viewed by 1377
Abstract
During the medication-assisted treatment of drug abuse, side effects and addiction liabilities are commonly observed. Thus, control of the medication dose is very important. According to body temperature abnormalities in drug abusers, a thermo-sensitive nanogel was synthesized as a drug carrier to automatically [...] Read more.
During the medication-assisted treatment of drug abuse, side effects and addiction liabilities are commonly observed. Thus, control of the medication dose is very important. According to body temperature abnormalities in drug abusers, a thermo-sensitive nanogel was synthesized as a drug carrier to automatically deliver detoxification medicines. This nanogel was prepared through the synthesis of polystyrene (PS) core microspheres, followed by coverage with a nonlinear poly(ethylene glycol)-based copolymer shell. The PS core microspheres were found to be an ideal hydrophobic core for loading the detoxification medicines effectively. The nonlinear poly(ethylene glycol)-based copolymer shell layer consisted of 2-(2-methoxyethoxy)ethyl methacrylate (MEO2MA) and oligo(ethylene glycol) methyl ether methacrylates (Mn = 300 g mol−1, MEO5MA). The monomer feeding molar ratio n(MEO2MA)/n(MEO5MA) of 1:3 enabled PS@P(MEO2MA-co-MEO5MA) nanogels to exhibit a distinguished colloidal stability and an adjustable volume phase transition temperature which is within the drug addicts’ abnormally fluctuating temperature range. Importantly, it was found that the obtained PS@P(MEO2MA-co-MEO5MA) nanogels displayed good biocompatibility with rat aortic endothelial cells in the given concentration range. The nanogels also exhibited a satisfactory loading efficiency and thermo-sensitive/sustained release characteristics for three detoxification medicines: sinomenine, diltiazem and chlorpromazine. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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10 pages, 2051 KiB  
Article
Solubilization of Paclitaxel by Self-Assembled Amphiphilic Phospholipid-Mimetic Polymers with Varied Hydrophobicity
by Chie Kojima, Tomoka Hirose, Risa Katayama and Akikazu Matsumoto
Polymers 2021, 13(16), 2805; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13162805 - 20 Aug 2021
Cited by 5 | Viewed by 2441
Abstract
2-Methacryloyloxyethyl phosphorylcholine (MPC) polymers have been used as a coating agent on medical devices and as a carrier in drug delivery systems (DDSs). Paclitaxel (PTX) is a water-insoluble anticancer drug whose solubilizer is necessary for administration. Block and random copolymers composed of hydrophilic [...] Read more.
2-Methacryloyloxyethyl phosphorylcholine (MPC) polymers have been used as a coating agent on medical devices and as a carrier in drug delivery systems (DDSs). Paclitaxel (PTX) is a water-insoluble anticancer drug whose solubilizer is necessary for administration. Block and random copolymers composed of hydrophilic MPC and butyl methacrylate, named PMB, show different properties, depending on the polymer sequence and MPC content. In the present study, we used amphiphilic MPC polymers comprising hydrophobic dodecyl methacrylate (DMA). The self-assembling properties and PTX solubilization of random and block poly(MPC-co-DMA)s (rPMDs and bPMDs) with different compositions were examined and compared. rPMDs with high DMA content formed large and relatively loose self-assembled structures, which solubilized PTX. However, bPMDs formed small and compact self-assembled structures with poor PTX solubilization. PTX solubilized by PMB with small and loose self-assembled structures showed efficient drug action, similar to free PTX; however, rPMDs fell short of demonstrating PTX efficiency. Our results suggest that the self-assembling properties and the hydrophobicity of amphiphilic MPC polymers largely affect PTX solubilization as well as drug action, which is required to be controlled by the polymer sequence, as well as the structure and composition of the hydrophobic monomer for efficient DDS. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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18 pages, 3826 KiB  
Article
Development of In-Situ Spray for Local Delivery of Antibacterial Drug for Hidradenitis Suppurativa: Investigation of Alternative Formulation
by Yoke Lan Wong, Manisha Pandey, Hira Choudhury, Wei Meng Lim, Subrat Kumar Bhattamisra and Bapi Gorain
Polymers 2021, 13(16), 2770; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13162770 - 18 Aug 2021
Cited by 9 | Viewed by 2567
Abstract
Hidradenitis suppurativa (HS) has been considered an orphan disease with limited treatments available. The available topical treatment for this condition is clindamycin lotion; however, short retention and frequent application are the main setbacks. Thus, the present study aimed to attain an optimized antibacterial [...] Read more.
Hidradenitis suppurativa (HS) has been considered an orphan disease with limited treatments available. The available topical treatment for this condition is clindamycin lotion; however, short retention and frequent application are the main setbacks. Thus, the present study aimed to attain an optimized antibacterial in situ spray formulation for the hidradenitis suppurativa skin condition, which gels once in contact with the skin surface at around 37 °C and possesses bioadhesion as well as sustained-release properties of the incorporated drug. Different concentrations of thermo-reversible gelling polymer, Pluronic F-127, were investigated along with the selected bioadhesive polymers, HPMC and SA. The optimized formulation F3 consisting of 18% Pluronic F-127 with 0.2% HPMC and 0.2% SA was characterized based on various physicochemical properties. The gelation temperature of F3 was found to be 29.0 ± 0.50 °C with a gelation time of 1.35 ± 0.40 min and a pH of 5.8. F3 had the viscosity of 178.50 ± 5.50 cP at 25 °C and 7800 ± 200 cP at 37 °C as the gel set. The optimized formulation was found to be bioadhesive and cytocompatible. Cumulative drug release was 65.05% within the time-frame of 8 h; the release pattern of the drug followed zero-order kinetics with the Higuchi release mechanism. The average zone of inhibition was found to be 43.44 ± 1.34 mm. The properties of F3 formulation reflect to improve residence time at the site of application and can enhance sustained drug release. Therefore, it could be concluded that optimized formulation has better retention and enhanced antimicrobial activity for superior efficacy against HS. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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13 pages, 2114 KiB  
Article
Inhalable Spray-Dried Chondroitin Sulphate Microparticles: Effect of Different Solvents on Particle Properties and Drug Activity
by Susana Rodrigues, Ana M. Rosa da Costa, Noelia Flórez-Fernández, María Dolores Torres, Maria Leonor Faleiro, Francesca Buttini and Ana Grenha
Polymers 2020, 12(2), 425; https://0-doi-org.brum.beds.ac.uk/10.3390/polym12020425 - 12 Feb 2020
Cited by 17 | Viewed by 2832
Abstract
Spray-drying stands as one of the most used techniques to produce inhalable microparticles, but several parameters from both the process and the used materials affect the properties of the resulting microparticles. In this work, we describe the production of drug-loaded chondroitin sulphate microparticles [...] Read more.
Spray-drying stands as one of the most used techniques to produce inhalable microparticles, but several parameters from both the process and the used materials affect the properties of the resulting microparticles. In this work, we describe the production of drug-loaded chondroitin sulphate microparticles by spray-drying, testing the effect of using different solvents during the process. Full characterisation of the polymer and of the aerodynamic properties of the obtained microparticles are provided envisaging an application in inhalable tuberculosis therapy. The spray-dried microparticles successfully associated two first-line antitubercular drugs (isoniazid and rifabutin) with satisfactory production yield (up to 85%) and drug association efficiency (60%–95%). Ethanol and HCl were tested as co-solvents to aid the solubilisation of rifabutin and microparticles produced with the former generally revealed the best features, presenting a better ability to sustainably release rifabutin. Moreover, these presented aerodynamic properties compatible with deep lung deposition, with an aerodynamic diameter around 4 μm and fine particle fraction of approximately 44%. Finally, it was further demonstrated that the antitubercular activity of the drugs remained unchanged after encapsulation independently of the used solvent. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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16 pages, 4107 KiB  
Article
A Chitosan-Based Micellar System as Nanocarrier For the Delivery of Paclitaxel
by Yang Han, Na Liang, Pengfei Yan, Yoshiaki Kawashima, Fude Cui and Shaoping Sun
Polymers 2020, 12(2), 380; https://0-doi-org.brum.beds.ac.uk/10.3390/polym12020380 - 08 Feb 2020
Cited by 15 | Viewed by 2774
Abstract
In this study, a redox-sensitive chitosan derivative with modifications by cholesterol, sulfhydryl, and mPEG (mPEG-CS(SH)-CHO) was successfully synthesized and characterized. Due to its amphiphilicity, the conjugate could spontaneously form micelles in an aqueous environment. The optimized paclitaxel (PTX)-loaded mPEG-CS(SH)-CHO micelles, with a mean [...] Read more.
In this study, a redox-sensitive chitosan derivative with modifications by cholesterol, sulfhydryl, and mPEG (mPEG-CS(SH)-CHO) was successfully synthesized and characterized. Due to its amphiphilicity, the conjugate could spontaneously form micelles in an aqueous environment. The optimized paclitaxel (PTX)-loaded mPEG-CS(SH)-CHO micelles, with a mean diameter of 158 nm, zeta potential of +26.9 mV, drug loading of 11.7%, and entrapment efficiency of 88.3%, were successfully prepared. The results of an XRD study demonstrated that PTX was loaded in the core of the micelles in a non-crystalline state. Inspiringly, the PTX-loaded micelles possessed excellent anticancer effect but low toxicity to the body. It can be concluded that the mPEG-CS(SH)-CHO micellar system is a promising drug delivery carrier for the controlled release of PTX. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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14 pages, 4944 KiB  
Article
Multi-Responsive Nanocarriers Based on β-CD-PNIPAM Star Polymer Coated MSN-SS-Fc Composite Particles
by Feng Guo, Guiying Li, Songmei Ma, Hengquan Zhou and Xinyi Chen
Polymers 2019, 11(10), 1716; https://0-doi-org.brum.beds.ac.uk/10.3390/polym11101716 - 19 Oct 2019
Cited by 23 | Viewed by 4035
Abstract
A temperature, glutathione (GSH), and H2O2 multi-responsive composite nanocarrier (MSN-SS-Fc@β-CD-PNIPAM) based on β-cyclodextrin-poly(N-isopropylacrylamide) (β-CD-PNIPAM) star polymer capped ferrocene modified mesoporous silica nanoparticles (MSN-SS-Fc) was successfully prepared. The surface of the mesoporous silica was first modified by ferrocene (Fc) [...] Read more.
A temperature, glutathione (GSH), and H2O2 multi-responsive composite nanocarrier (MSN-SS-Fc@β-CD-PNIPAM) based on β-cyclodextrin-poly(N-isopropylacrylamide) (β-CD-PNIPAM) star polymer capped ferrocene modified mesoporous silica nanoparticles (MSN-SS-Fc) was successfully prepared. The surface of the mesoporous silica was first modified by ferrocene (Fc) via a disulfide bond (–SS–) to form an oxidizing and reducing site and then complexed with a β-CD-PNIPAM star shaped polymer through host–guest interactions as a nano-valve to provide temperature responsive characteristics. The structure and properties of the complex nanoparticles were studied by FTIR, TGA, EDS, Zeta potential, and elemental analysis. Doxorubicin (DOX) and Naproxen (NAP), as model drugs, were loaded into nanocarriers to assess drug loading and release behaviour. The release of drugs from nanocarriers was enhanced with an increase of the GSH, H2O2 concentration, or temperatures of the solution. The kinetics of the release process were studied using different models. This nanocarrier presents successful multi-stimuli responsive drug delivery in optimal stimuli and provides potential applications for clinical treatment. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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Review

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19 pages, 2108 KiB  
Review
Review on Modification of Glucomannan as an Excipient in Solid Dosage Forms
by Nuur Aanisah, Yoga W. Wardhana, Anis Y. Chaerunisaa and Arif Budiman
Polymers 2022, 14(13), 2550; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14132550 - 23 Jun 2022
Cited by 8 | Viewed by 2666
Abstract
Glucomannan (GM)—a polysaccharide generally extracted from the tuber of Amorphophallus konjac—has great potential as a filler–binder in direct compression, disintegrant in tablets, or gelling agent due to its strong hydrophilicity and extremely high viscosity. However, it has poor water resistance and low [...] Read more.
Glucomannan (GM)—a polysaccharide generally extracted from the tuber of Amorphophallus konjac—has great potential as a filler–binder in direct compression, disintegrant in tablets, or gelling agent due to its strong hydrophilicity and extremely high viscosity. However, it has poor water resistance and low mechanical strength when used as an excipient in solid form. Several physical and chemical modifications have been carried out to improve these drawbacks. Chemical modification affects the characteristics of GM based on the DS. Carboxymethylation improves GM functionality by modifying its solubility and viscosity, which in turn allows it to bind water more efficiently and thus improve its elongation and gel homogeneity. Meanwhile, physical modification enhances functionality through combination with other excipients to improve mechanical properties and modify swelling ability and drug release from the matrix. This review discusses extraction of GM and its modification to enhance its applicability as an excipient in solid form. Modified GM is a novel excipient applicable in the pharmaceutical industry for direct compression, as a tablet disintegrant, a film-forming agent, and for encapsulation of macromolecular compounds or drug carriers for controlled release. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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21 pages, 13942 KiB  
Review
Recent Trends in Assessment of Cellulose Derivatives in Designing Novel and Nanoparticulate-Based Drug Delivery Systems for Improvement of Oral Health
by Khaled M. Hosny, Hala M. Alkhalidi, Waleed S. Alharbi, Shadab Md, Amal M. Sindi, Sarah A. Ali, Rana B. Bakhaidar, Alshaimaa M. Almehmady, Eman Alfayez and Mallesh Kurakula
Polymers 2022, 14(1), 92; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14010092 - 27 Dec 2021
Cited by 13 | Viewed by 4877
Abstract
Natural polymers are revolutionizing current pharmaceutical dosage forms design as excipient and gained huge importance because of significant influence in formulation development and drug delivery. Oral health refers to the health of the teeth, gums, and the entire oral-facial system that allows us [...] Read more.
Natural polymers are revolutionizing current pharmaceutical dosage forms design as excipient and gained huge importance because of significant influence in formulation development and drug delivery. Oral health refers to the health of the teeth, gums, and the entire oral-facial system that allows us to smile, speak, and chew. Since years, biopolymers stand out due to their biocompatibility, biodegradability, low toxicity, and stability. Polysaccharides such as cellulose and their derivatives possess properties like novel mechanical robustness and hydrophilicity that can be easily fabricated into controlled-release dosage forms. Cellulose attracts the dosage design attention because of constant drug release rate from the precursor nanoparticles. This review discusses the origin, extraction, preparation of cellulose derivatives and their use in formulation development of nanoparticles having multidisciplinary applications as pharmaceutical excipient and in drug delivery, as bacterial and plant cellulose have great potential for application in the biomedical area, including dentistry, protein and peptide delivery, colorectal cancer treatment, and in 3D printable dosage forms. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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43 pages, 23383 KiB  
Review
Functionalized Particles Designed for Targeted Delivery
by Teresa Basinska, Mariusz Gadzinowski, Damian Mickiewicz and Stanislaw Slomkowski
Polymers 2021, 13(12), 2022; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13122022 - 21 Jun 2021
Cited by 10 | Viewed by 2894
Abstract
Pure bioactive compounds alone can only be exceptionally administered in medical treatment. Usually, drugs are produced as various forms of active compounds and auxiliary substances, combinations assuring the desired healing functions. One of the important drug forms is represented by a combination of [...] Read more.
Pure bioactive compounds alone can only be exceptionally administered in medical treatment. Usually, drugs are produced as various forms of active compounds and auxiliary substances, combinations assuring the desired healing functions. One of the important drug forms is represented by a combination of active substances and particle-shaped polymer in the nano- or micrometer size range. The review describes recent progress in this field balanced with basic information. After a brief introduction, the paper presents a concise overview of polymers used as components of nano- and microparticle drug carriers. Thereafter, progress in direct synthesis of polymer particles with functional groups is discussed. A section is devoted to formation of particles by self-assembly of homo- and copolymer-bearing functional groups. Special attention is focused on modification of the primary functional groups introduced during particle preparation, including introduction of ligands promoting anchorage of particles onto the chosen living cell types by interactions with specific receptors present in cell membranes. Particular attention is focused on progress in methods suitable for preparation of particles loaded with bioactive substances. The review ends with a brief discussion of the still not answered questions and unsolved problems. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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30 pages, 3455 KiB  
Review
Stimuli-Responsive Aliphatic Polycarbonate Nanocarriers for Tumor-Targeted Drug Delivery
by Adrian Domiński, Tomasz Konieczny, Khadar Duale, Monika Krawczyk, Gabriela Pastuch-Gawołek and Piotr Kurcok
Polymers 2020, 12(12), 2890; https://0-doi-org.brum.beds.ac.uk/10.3390/polym12122890 - 02 Dec 2020
Cited by 16 | Viewed by 3325
Abstract
Nanoparticles based on amphiphilic copolymers with tunable physicochemical properties can be used to encapsulate delicate pharmaceutics while at the same time improving their solubility, stability, pharmacokinetic properties, reducing immune surveillance, or achieving tumor-targeting ability. Those nanocarriers based on biodegradable aliphatic polycarbonates are a [...] Read more.
Nanoparticles based on amphiphilic copolymers with tunable physicochemical properties can be used to encapsulate delicate pharmaceutics while at the same time improving their solubility, stability, pharmacokinetic properties, reducing immune surveillance, or achieving tumor-targeting ability. Those nanocarriers based on biodegradable aliphatic polycarbonates are a particularly promising platform for drug delivery due to flexibility in the design and synthesis of appropriate monomers and copolymers. Current studies in this field focus on the design and the synthesis of new effective carriers of hydrophobic drugs and their release in a controlled manner by exogenous or endogenous factors in tumor-specific regions. Reactive groups present in aliphatic carbonate copolymers, undergo a reaction under the action of a stimulus: e.g., acidic hydrolysis, oxidation, reduction, etc. leading to changes in the morphology of nanoparticles. This allows the release of the drug in a highly controlled manner and induces a desired therapeutic outcome without damaging healthy tissues. The presented review summarizes the current advances in chemistry and methods for designing stimuli-responsive nanocarriers based on aliphatic polycarbonates for controlled drug delivery. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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26 pages, 1729 KiB  
Review
Polymer Capsules with Hydrophobic Liquid Cores as Functional Nanocarriers
by Joanna Szafraniec-Szczęsny, Małgorzata Janik-Hazuka, Joanna Odrobińska and Szczepan Zapotoczny
Polymers 2020, 12(9), 1999; https://0-doi-org.brum.beds.ac.uk/10.3390/polym12091999 - 02 Sep 2020
Cited by 25 | Viewed by 6223
Abstract
Recent developments in the fabrication of core-shell polymer nanocapsules, as well as their current and future applications, are reported here. Special attention is paid to the newly introduced surfactant-free fabrication method of aqueous dispersions of nanocapsules with hydrophobic liquid cores stabilized by amphiphilic [...] Read more.
Recent developments in the fabrication of core-shell polymer nanocapsules, as well as their current and future applications, are reported here. Special attention is paid to the newly introduced surfactant-free fabrication method of aqueous dispersions of nanocapsules with hydrophobic liquid cores stabilized by amphiphilic copolymers. Various approaches to the efficient stabilization of such vehicles, tailoring their cores and shells for the fabrication of multifunctional, navigable nanocarriers and/or nanoreactors useful in various fields, are discussed. The emphasis is placed on biomedical applications of polymer nanocapsules, including the delivery of poorly soluble active compounds and contrast agents, as well as their use as theranostic platforms. Other methods of fabrication of polymer-based nanocapsules are briefly presented and compared in the context of their biomedical applications. Full article
(This article belongs to the Special Issue Polymers and Drug Delivery)
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