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Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition
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Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (30 June 2023) | Viewed by 24363

Printed Edition Available!
A printed edition of this Special Issue is available here.

Special Issue Editor

Dr. Ana Isabel Fernandes

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Guest Editor
CiiEM – Interdisciplinary Research Center Egas Moniz, Instituto Universitário Egas Moniz, Quinta da Granja, Monte de Caparica, 2829-511 Caparica, Portugal
Interests: polymers and polymeric systems; protein delivery; formulation in pediatrics; drug solubility enhancement; 3D-printing of pharmaceuticals
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Currently, many of the drug entities entering the clinic face bioavailability issues, mainly due to poor water solubility and/or permeability, in addition to issues with physicochemical instability or degradation in the body. To overcome biological barriers, drug sensitivity, and formulation problems, the use of several polymers has been considered. Polymers, either natural or synthetic, present an array of different backbones and functional groups, sizes, shapes, as well as mechanical and degradation properties, which have been exploited in drug delivery and targeting. Strategies for bioavailability enhancement using functionalized polymers include solid amorphous dispersions for improved solubility; chemical modification for extended blood residence and reduced or abrogated immunogenicity and antigenicity; protection from harsh pH or enzymatic degradation; as well as tailored rate and temporal/spatial drug release.

This Special Issue, Polymers Enhancing Bioavailability in Drug Delivery—Volume II, aims to review the specific functional benefits granted by polymers to formulations, which are very much reliant on polymer structure and design, and result in improved drug bioavailability and therapeutic index. You are welcome to submit your research or review papers to this Special Issue, thus contributing to this exciting field.

Dr. Ana Isabel Fernandes
Guest Editor

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • polymers
  • bioavailability enhancement
  • aqueous solubility enhancement
  • drug solubilization
  • improved drug pharmacokinetics
  • drug delivery and targeting

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Published Papers (14 papers)

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Editorial

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7 pages, 410 KiB  
Editorial
Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition
by Ana I. Fernandes
Pharmaceutics 2023, 15(11), 2604; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15112604 - 08 Nov 2023
Viewed by 839
Abstract
This Special Issue continues the previously published work [...] Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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Research

Jump to: Editorial, Review

20 pages, 11199 KiB  
Article
Evaluation of the In Vitro Antimicrobial Efficacy against Staphylococcus aureus and epidermidis of a Novel 3D-Printed Degradable Drug Delivery System Based on Polycaprolactone/Chitosan/Vancomycin—Preclinical Study
by Iván López-González, Ana Belén Hernández-Heredia, María Isabel Rodríguez-López, David Auñón-Calles, Mohamed Boudifa, José Antonio Gabaldón and Luis Meseguer-Olmo
Pharmaceutics 2023, 15(6), 1763; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15061763 - 18 Jun 2023
Cited by 5 | Viewed by 1413
Abstract
Acute and chronic bone infections, especially those caused by methicillin-resistant Staphylococcus aureus (MRSA), remains a major complication and therapeutic challenge. It is documented that local administration of vancomycin offers better results than the usual routes of administration (e.g., intravenous) when ischemic areas are [...] Read more.
Acute and chronic bone infections, especially those caused by methicillin-resistant Staphylococcus aureus (MRSA), remains a major complication and therapeutic challenge. It is documented that local administration of vancomycin offers better results than the usual routes of administration (e.g., intravenous) when ischemic areas are present. In this work, we evaluate the antimicrobial efficacy against S. aureus and S. epidermidis of a novel hybrid 3D-printed scaffold based on polycaprolactone (PCL) and a chitosan (CS) hydrogel loaded with different vancomycin (Van) concentrations (1, 5, 10, 20%). Two cold plasma treatments were used to improve the adhesion of CS hydrogels to the PCL scaffolds by decreasing PCL hydrophobicity. Vancomycin release was measured by means of HPLC, and the biological response of ah-BM-MSCs growing in the presence of the scaffolds was evaluated in terms of cytotoxicity, proliferation, and osteogenic differentiation. The PCL/CS/Van scaffolds tested were found to be biocompatible, bioactive, and bactericide, as demonstrated by no cytotoxicity (LDH activity) or functional alteration (ALP activity, alizarin red staining) of the cultured cells and by bacterial inhibition. Our results suggest that the scaffolds developed would be excellent candidates for use in a wide range of biomedical fields such as drug delivery systems or tissue engineering applications. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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26 pages, 14775 KiB  
Article
Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer
by Alaa R. Aboushanab, Riham M. El-Moslemany, Amal H. El-Kamel, Radwa A. Mehanna, Basant A. Bakr and Asmaa A. Ashour
Pharmaceutics 2023, 15(5), 1480; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15051480 - 12 May 2023
Cited by 3 | Viewed by 2056
Abstract
Fisetin (FS) is considered a safer phytomedicine alternative to conventional chemotherapeutics for breast cancer treatment. Despite its surpassing therapeutic potential, its clinical utility is hampered by its low systemic bioavailability. Accordingly, as far as we are aware, this is the first study to [...] Read more.
Fisetin (FS) is considered a safer phytomedicine alternative to conventional chemotherapeutics for breast cancer treatment. Despite its surpassing therapeutic potential, its clinical utility is hampered by its low systemic bioavailability. Accordingly, as far as we are aware, this is the first study to develop lactoferrin-coated FS-loaded β-cyclodextrin nanosponges (LF-FS-NS) for targeted FS delivery to breast cancer. NS formation through cross-linking of β-cyclodextrin by diphenyl carbonate was confirmed by FTIR and XRD. The selected LF-FS-NS showed good colloidal properties (size 52.7 ± 7.2 nm, PDI < 0.3, and ζ-potential 24 mV), high loading efficiency (96 ± 0.3%), and sustained drug release of 26 % after 24 h. Morphological examination using SEM revealed the mesoporous spherical structure of the prepared nanosponges with a pore diameter of ~30 nm, which was further confirmed by surface area measurement. Additionally, LF-FS-NS enhanced FS oral and IP bioavailability (2.5- and 3.2-fold, respectively) compared to FS suspension in rats. Antitumor efficacy evaluation in vitro on MDA-MB-231 cells and in vivo on an Ehrlich ascites mouse model demonstrated significantly higher activity and targetability of LF-FS-NS (30 mg/kg) compared to the free drug and uncoated formulation. Consequently, LF-FS-NS could be addressed as a promising formulation for the effective management of breast cancer. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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21 pages, 6477 KiB  
Article
Application of Sucrose Acetate Isobutyrate in Development of Co-Amorphous Formulations of Tacrolimus for Bioavailability Enhancement
by Eman M. Mohamed, Sathish Dharani, Mohammad T. H. Nutan, Phillip Cook, Rajendran Arunagiri, Mansoor A. Khan and Ziyaur Rahman
Pharmaceutics 2023, 15(5), 1442; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15051442 - 09 May 2023
Cited by 1 | Viewed by 1512
Abstract
The focus of the present work was to develop co-amorphous dispersion (CAD) formulations of tacrolimus (TAC) using sucrose acetate isobutyrate as a carrier, evaluate by in vitro and in vivo methods and compare its performance with hydroxypropyl methylcellulose (HPMC) based amorphous solid dispersion [...] Read more.
The focus of the present work was to develop co-amorphous dispersion (CAD) formulations of tacrolimus (TAC) using sucrose acetate isobutyrate as a carrier, evaluate by in vitro and in vivo methods and compare its performance with hydroxypropyl methylcellulose (HPMC) based amorphous solid dispersion (ASD) formulation. CAD and ASD formulations were prepared by solvent evaporation method followed by characterization by Fourier transformed infrared spectroscopy, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), dissolution, stability, and pharmacokinetics. XRPD and DSC indicated amorphous phase transformation of the drug in the CAD and ASD formulations, and dissolved more than 85% of the drug in 90 min. No drug crystallization was observed in the thermogram and diffractogram of the formulations after storage at 25 °C/60% RH and 40 °C/75% RH. No significant change in the dissolution profile was observed after and before storage. SAIB-based CAD and HPMC-based ASD formulations were bioequivalent as they met 90% confidence of 90–11.1% for Cmax and AUC. The CAD and ASD formulations exhibited Cmax and AUC 1.7–1.8 and 1.5–1.8 folds of tablet formulations containing the drug’s crystalline phase. In conclusion, the stability, dissolution, and pharmacokinetic performance of SAIB-based CAD and HPMC-based ASD formulations were similar, and thus clinical performance would be similar. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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18 pages, 6678 KiB  
Article
Molecular Interactions between APIs and Enteric Polymeric Excipients in Solid Dispersion: Insights from Molecular Simulations and Experiments
by Krishna M. Gupta, Xavier Chin and Parijat Kanaujia
Pharmaceutics 2023, 15(4), 1164; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15041164 - 06 Apr 2023
Cited by 1 | Viewed by 1500
Abstract
Solid dispersion of poorly soluble APIs is known to be a promising strategy to improve dissolution and oral bioavailability. To facilitate the development and commercialization of a successful solid dispersion formulation, understanding of intermolecular interactions between APIs and polymeric carriers is essential. In [...] Read more.
Solid dispersion of poorly soluble APIs is known to be a promising strategy to improve dissolution and oral bioavailability. To facilitate the development and commercialization of a successful solid dispersion formulation, understanding of intermolecular interactions between APIs and polymeric carriers is essential. In this work, first, we assessed the molecular interactions between various delayed-release APIs and polymeric excipients using molecular dynamics (MD) simulations, and then we formulated API solid dispersions using a hot melt extrusion (HME) technique. To assess the potential API–polymer pairs, three quantities were evaluated: (a) interaction energy between API and polymer [electrostatic (Ecoul), Lenard-Jones (ELJ), and total (Etotal)], (b) energy ratio (API–polymer/API–API), and (c) hydrogen bonding between API and polymer. The Etotal quantities corresponding to the best pairs: NPX-Eudragit L100, NaDLO–HPMC(P), DMF–HPMC(AS) and OPZ–HPMC(AS) were −143.38, −348.04, −110.42, and −269.43 kJ/mol, respectively. Using a HME experimental technique, few API–polymer pairs were successfully extruded. These extruded solid forms did not release APIs in a simulated gastric fluid (SGF) pH 1.2 environment but released them in a simulated intestinal fluid (SIF) pH 6.8 environment. The study demonstrates the compatibility between APIs and excipients, and finally suggests a potential polymeric excipient for each delayed-release API, which could facilitate the development of the solid dispersion of poorly soluble APIs for dissolution and bioavailability enhancement. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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17 pages, 1337 KiB  
Article
Neuroprotective Nanoparticles Targeting the Retina: A Polymeric Platform for Ocular Drug Delivery Applications
by Patrizia Colucci, Martina Giannaccini, Matteo Baggiani, Breandán N. Kennedy, Luciana Dente, Vittoria Raffa and Chiara Gabellini
Pharmaceutics 2023, 15(4), 1096; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15041096 - 29 Mar 2023
Cited by 3 | Viewed by 1881
Abstract
Neuroprotective drug delivery to the posterior segment of the eye represents a major challenge to counteract vision loss. This work focuses on the development of a polymer-based nanocarrier, specifically designed for targeting the posterior eye. Polyacrylamide nanoparticles (ANPs) were synthesised and characterised, and [...] Read more.
Neuroprotective drug delivery to the posterior segment of the eye represents a major challenge to counteract vision loss. This work focuses on the development of a polymer-based nanocarrier, specifically designed for targeting the posterior eye. Polyacrylamide nanoparticles (ANPs) were synthesised and characterised, and their high binding efficiency was exploited to gain both ocular targeting and neuroprotective capabilities, through conjugation with peanut agglutinin (ANP:PNA) and neurotrophin nerve growth factor (ANP:PNA:NGF). The neuroprotective activity of ANP:PNA:NGF was assessed in an oxidative stress-induced retinal degeneration model using the teleost zebrafish. Upon nanoformulation, NGF improved the visual function of zebrafish larvae after the intravitreal injection of hydrogen peroxide, accompanied by a reduction in the number of apoptotic cells in the retina. Additionally, ANP:PNA:NGF counteracted the impairment of visual behaviour in zebrafish larvae exposed to cigarette smoke extract (CSE). Collectively, these data suggest that our polymeric drug delivery system represents a promising strategy for implementing targeted treatment against retinal degeneration. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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15 pages, 2000 KiB  
Article
Coating of SPIONs with a Cysteine-Decorated Copolyester: A Possible Novel Nanoplatform for Enzymatic Release
by Jeovandro Maria Beltrame, Brena Beatriz Pereira Ribeiro, Camila Guindani, Graziâni Candiotto, Karina Bettega Felipe, Rodrigo Lucas, Alexandre D’Agostini Zottis, Eduardo Isoppo, Claudia Sayer and Pedro Henrique Hermes de Araújo
Pharmaceutics 2023, 15(3), 1000; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15031000 - 20 Mar 2023
Cited by 3 | Viewed by 1550
Abstract
Superparamagnetic iron oxide nanoparticles (SPIONs) have their use approved for the diagnosis/treatment of malignant tumors and can be metabolized by the organism. To prevent embolism caused by these nanoparticles, they need to be coated with biocompatible and non-cytotoxic materials. Here, we synthesized an [...] Read more.
Superparamagnetic iron oxide nanoparticles (SPIONs) have their use approved for the diagnosis/treatment of malignant tumors and can be metabolized by the organism. To prevent embolism caused by these nanoparticles, they need to be coated with biocompatible and non-cytotoxic materials. Here, we synthesized an unsaturated and biocompatible copolyester, poly (globalide-co-ε-caprolactone) (PGlCL), and modified it with the amino acid cysteine (Cys) via a thiol-ene reaction (PGlCLCys). The Cys-modified copolymer presented reduced crystallinity and increased hydrophilicity in comparison to PGlCL, thus being used for the coating of SPIONS (SPION@PGlCLCys). Additionally, cysteine pendant groups at the particle’s surface allowed the direct conjugation of (bio)molecules that establish specific interactions with tumor cells (MDA-MB 231). The conjugation of either folic acid (FA) or the anti-cancer drug methotrexate (MTX) was carried out directly on the amine groups of cysteine molecules present in the SPION@PGlCLCys surface (SPION@PGlCLCys_FA and SPION@PGlCLCys_MTX) by carbodiimide-mediated coupling, leading to the formation of amide bonds, with conjugation efficiencies of 62% for FA and 60% for MTX. Then, the release of MTX from the nanoparticle surface was evaluated using a protease at 37 °C in phosphate buffer pH~5.3. It was found that 45% of MTX conjugated to the SPIONs were released after 72 h. Cell viability was measured by MTT assay, and after 72 h, 25% reduction in cell viability of tumor cells was observed. Thus, after a successful conjugation and subsequent triggered release of MTX, we understand that SPION@PGlCLCys has a strong potential to be treated as a model nanoplatform for the development of treatments and diagnosis techniques (or theranostic applications) that can be less aggressive to patients. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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16 pages, 10185 KiB  
Article
Catheters with Dual-Antimicrobial Properties by Gamma Radiation-Induced Grafting
by Lorena Duarte-Peña, Héctor Magaña and Emilio Bucio
Pharmaceutics 2023, 15(3), 960; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15030960 - 16 Mar 2023
Viewed by 1371
Abstract
Dual antimicrobial materials that have a combination of antimicrobial and antifouling properties were developed. They were developed through modification using gamma radiation of poly (vinyl chloride) (PVC) catheters with 4-vinyl pyridine (4VP) and subsequent functionalization with 1,3-propane sultone (PS). These materials were characterized [...] Read more.
Dual antimicrobial materials that have a combination of antimicrobial and antifouling properties were developed. They were developed through modification using gamma radiation of poly (vinyl chloride) (PVC) catheters with 4-vinyl pyridine (4VP) and subsequent functionalization with 1,3-propane sultone (PS). These materials were characterized by infrared spectroscopy, thermogravimetric analysis, swelling tests, and contact angle to determine their surface characteristics. In addition, the capacity of the materials to deliver ciprofloxacin, inhibit bacterial growth, decrease bacterial and protein adhesion, and stimulate cell growth were evaluated. These materials have potential applications in the manufacturing of medical devices with antimicrobial properties, which can reinforce prophylactic potential or even help treat infections, through localized delivery systems for antibiotics. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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26 pages, 4182 KiB  
Article
Influence of the Topology of Poly(L-Cysteine) on the Self-Assembly, Encapsulation and Release Profile of Doxorubicin on Dual-Responsive Hybrid Polypeptides
by Dimitra Stavroulaki, Iro Kyroglou, Dimitrios Skourtis, Varvara Athanasiou, Pandora Thimi, Sosanna Sofianopoulou, Diana Kazaryan, Panagiota G. Fragouli, Andromahi Labrianidou, Konstantinos Dimas, Georgios Patias, David M. Haddleton and Hermis Iatrou
Pharmaceutics 2023, 15(3), 790; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15030790 - 27 Feb 2023
Cited by 2 | Viewed by 1767
Abstract
Τhe synthesis of a series of novel hybrid block copolypeptides based on poly(ethylene oxide) (PEO), poly(l-histidine) (PHis) and poly(l-cysteine) (PCys) is presented. The synthesis of the terpolymers was achieved through a ring-opening polymerization (ROP) of the corresponding protected N [...] Read more.
Τhe synthesis of a series of novel hybrid block copolypeptides based on poly(ethylene oxide) (PEO), poly(l-histidine) (PHis) and poly(l-cysteine) (PCys) is presented. The synthesis of the terpolymers was achieved through a ring-opening polymerization (ROP) of the corresponding protected N-carboxy anhydrides of Nim-Trityl-l-histidine and S-tert-butyl-l-cysteine, using an end-amine-functionalized poly(ethylene oxide) (mPEO-NH2) as macroinitiator, followed by the deprotection of the polypeptidic blocks. The topology of PCys was either the middle block, the end block or was randomly distributed along the PHis chain. These amphiphilic hybrid copolypeptides assemble in aqueous media to form micellar structures, comprised of an outer hydrophilic corona of PEO chains, and a pH- and redox-responsive hydrophobic layer based on PHis and PCys. Due to the presence of the thiol groups of PCys, a crosslinking process was achieved further stabilizing the nanoparticles (NPs) formed. Dynamic light scattering (DLS), static light scattering (SLS) and transmission electron microscopy (TEM) were utilized to obtain the structure of the NPs. Moreover, the pH and redox responsiveness in the presence of the reductive tripeptide of glutathione (GSH) was investigated at the empty as well as the loaded NPs. The ability of the synthesized polymers to mimic natural proteins was examined by Circular Dichroism (CD), while the study of zeta potential revealed the “stealth” properties of NPs. The anticancer drug doxorubicin (DOX) was efficiently encapsulated in the hydrophobic core of the nanostructures and released under pH and redox conditions that simulate the healthy and cancer tissue environment. It was found that the topology of PCys significantly altered the structure as well as the release profile of the NPs. Finally, in vitro cytotoxicity assay of the DOX-loaded NPs against three different breast cancer cell lines showed that the nanocarriers exhibited similar or slightly better activity as compared to the free drug, rendering these novel NPs very promising materials for drug delivery applications. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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16 pages, 2061 KiB  
Article
Design and Evaluation of Pegylated Large 3D Pore Ferrisilicate as a Potential Insulin Protein Therapy to Treat Diabetic Mellitus
by B. Rabindran Jermy, Mohammed Salahuddin, Gazali Tanimu, Hatim Dafalla, Sarah Almofty and Vijaya Ravinayagam
Pharmaceutics 2023, 15(2), 593; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15020593 - 09 Feb 2023
Cited by 1 | Viewed by 1679
Abstract
An iron-based SBA-16 mesoporous silica (ferrisilicate) with a large surface area and three-dimensional (3D) pores is explored as a potential insulin delivery vehicle with improved encapsulation and loading efficiency. Fe was incorporated into a framework of ferrisilicate using the isomorphous substitution technique for [...] Read more.
An iron-based SBA-16 mesoporous silica (ferrisilicate) with a large surface area and three-dimensional (3D) pores is explored as a potential insulin delivery vehicle with improved encapsulation and loading efficiency. Fe was incorporated into a framework of ferrisilicate using the isomorphous substitution technique for direct synthesis. Fe3+ species were identified using diffuse reflectance spectroscopy. The large surface area (804 m2/g), cubic pores (3.2 nm) and insulin loading were characterized using XRD, BET surface area, FTIR and TEM analyses. For pH sensitivity, the ferrisilicate was wrapped with polyethylene glycol (MW = 400 Daltons) (PEG). For comparison, Fe (10 wt%) was impregnated on a Korea Advanced Institute of Science and Technology Number 6 (KIT-6) sieve and Mesocellular Silica Foam (MSU-F). Insulin loading was optimized, and its release mechanism was studied using the dialysis membrane technique (MWCO = 14,000 Da) at physiological pH = 7.4, 6.8 and 1.2. The kinetics of the drug’s release was studied using different structured/insulin nanoformulations, including Santa Barbara Amorphous materials (SBA-15, SBA-16), MSU-F, ultra-large-pore FDU-12 (ULPFDU-12) and ferrisilicates. A different insulin adsorption times (0.08–1 h), insulin/ferrisilicate ratios (0.125–1.0) and drug release rates at different pH were examined using the Korsmeyer–Peppas model. The rate of drug release and the diffusion mechanisms were obtained based on the release constant (k) and release exponent (n). The cytotoxicity of the nanoformulation was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay using human foreskin fibroblast (HFF-1) cells. A low cytotoxicity was observed for this nanoformulation starting at the highest concentrations used, namely, 400 and 800 μg. The hypoglycemic activity of insulin/ferrisilicate/PEG on acute administration in Wistar rats was studied using doses of 2, 5 and 10 mg/kg body weight. The developed facile ferrisilicate/PEG nanoformulation showed a high insulin encapsulation and loading capacity with pH-sensitive insulin release for potential delivery through the oral route. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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25 pages, 5746 KiB  
Article
Preparation and Characterization of a Novel Multiparticulate Dosage Form Carrying Budesonide-Loaded Chitosan Nanoparticles to Enhance the Efficiency of Pellets in the Colon
by Fatemeh Soltani, Hossein Kamali, Abbas Akhgari, Mahboobeh Ghasemzadeh Rahbardar, Hadi Afrasiabi Garekani, Ali Nokhodchi and Fatemeh Sadeghi
Pharmaceutics 2023, 15(1), 69; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15010069 - 26 Dec 2022
Cited by 4 | Viewed by 1615
Abstract
An attempt was made to conquer the limitation of orally administered nanoparticles for the delivery of budesonide to the colon. The ionic gelation technique was used to load budesonide on chitosan nanoparticles. The nanoparticles were investigated in terms of size, zeta potential, encapsulation [...] Read more.
An attempt was made to conquer the limitation of orally administered nanoparticles for the delivery of budesonide to the colon. The ionic gelation technique was used to load budesonide on chitosan nanoparticles. The nanoparticles were investigated in terms of size, zeta potential, encapsulation efficiency, shape and drug release. Then, nanoparticles were pelletized using the extrusion–spheronization method and were investigated for their size, mechanical properties, and drug release. Pellets were subsequently coated with a polymeric solution composed of two enteric (eudragit L and S) and time-dependent polymers (eudragit RS) for colon-specific delivery. All formulations were examined for their anti-inflammatory effect in rats with induced colitis and the relapse of the colitis after discontinuation of treatment was also followed. The size of nanoparticles ranged between 288 ± 7.5 and 566 ± 7.7 nm and zeta potential verified their positive charged surface. The drug release from nanoparticles showed an initial burst release followed by a continuous release. Pelletized nanoparticles showed proper mechanical properties and faster drug release in acidic pH compared with alkaline pH. It was interesting to note that pelletized budesonide nanoparticles released the drug throughout the GIT in a sustained fashion, and had long-lasting anti-inflammatory effects while rapid relapse was observed for those treated with conventional budesonide pellets. It seems that there is a synergistic effect of nanoformulation of budesonide and the encapsulation of pelletized nanoparticles in a proper coating system for colon delivery that could result in a significant and long-lasting anti-inflammatory effect. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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21 pages, 3041 KiB  
Article
Rutin Nanocrystals with Enhanced Anti-Inflammatory Activity: Preparation and Ex Vivo/In Vivo Evaluation in an Inflammatory Rat Model
by Abeer S. Hassan and Ghareb M. Soliman
Pharmaceutics 2022, 14(12), 2727; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14122727 - 06 Dec 2022
Cited by 9 | Viewed by 2457
Abstract
Rutin is a polyphenolic flavonoid with an interestingly wide therapeutic spectrum. However, its clinical benefits are limited by its poor aqueous solubility and low bioavailability. In an attempt to overcome these limitations, rutin nanocrystals were prepared using various stabilizers including nonionic surfactants and [...] Read more.
Rutin is a polyphenolic flavonoid with an interestingly wide therapeutic spectrum. However, its clinical benefits are limited by its poor aqueous solubility and low bioavailability. In an attempt to overcome these limitations, rutin nanocrystals were prepared using various stabilizers including nonionic surfactants and nonionic polymers. The nanocrystals were evaluated for particle size, zeta potential, drug entrapment efficiency, morphology, colloidal stability, rutin photostability, dissolution rate, and saturation solubility. The selected nanocrystal formulation was dispersed in a hydrogel base and the drug release kinetics and permeability through mouse skin were characterized. Rutin’s anti-inflammatory efficacy was studied in a carrageenan-induced rat paw edema model. The nanocrystals had a size in the range of around 270–500 nm and a polydispersity index of around 0.3–0.5. Nanocrystals stabilized by hydroxypropyl beta-cyclodextrin (HP-β-CD) had the smallest particle size, highest drug entrapment efficiency, best colloidal stability, and highest drug photostability. Nanocrystals had around a 102- to 202-fold and 2.3- to 6.7-fold increase in the drug aqueous solubility and dissolution rate, respectively, depending on the type of stabilizer. HP-β-CD nanocrystals hydrogel had a significantly higher percent of drug released and permeated through the mouse skin compared with the free drug hydrogel. The cumulative drug amount permeated through the skin was 2.5-fold higher than that of the free drug hydrogel. In vivo studies showed that HP-β-CD-stabilized rutin nanocrystals hydrogel had significantly higher edema inhibition compared with the free drug hydrogel and commercial diclofenac sodium gel. These results highlight the potential of HP-β-CD-stabilized nanocrystals as a promising approach to enhance drug solubility, dissolution rate, and anti-inflammatory properties. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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20 pages, 2325 KiB  
Article
Antifungal Encapsulated into Ligand-Functionalized Nanoparticles with High Specificity for Macrophages
by Susana P. Mejía, Daniela López, Luz Elena Cano, Tonny W. Naranjo and Jahir Orozco
Pharmaceutics 2022, 14(9), 1932; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14091932 - 13 Sep 2022
Cited by 5 | Viewed by 1894
Abstract
Infectious diseases caused by intracellular microorganisms such as Histoplasma capsulatum represent a significant challenge worldwide. Drug encapsulation into functionalized nanoparticles (NPs) is a valuable alternative to improving drug solubility and bioavailability, preventing undesirable interactions and drug degradation, and reaching the specific therapeutic target [...] Read more.
Infectious diseases caused by intracellular microorganisms such as Histoplasma capsulatum represent a significant challenge worldwide. Drug encapsulation into functionalized nanoparticles (NPs) is a valuable alternative to improving drug solubility and bioavailability, preventing undesirable interactions and drug degradation, and reaching the specific therapeutic target with lower doses. This work reports on Itraconazole (ITZ) encapsulated into core-shell-like polymeric NPs and functionalized with anti-F4/80 antibodies for their targeted and controlled release into macrophages. Uptake assay on co-culture showed significant differences between the uptake of functionalized and bare NPs, higher with functionalized NPs. In vitro assays showed that F4/80-NPs with 0.007 µg/mL of encapsulated ITZ eliminated the H. capsulatum fungus in co-culture with macrophages effectively compared to the bare NPs, without any cytotoxic effect on macrophages after 24 h interaction. Furthermore, encapsulated ITZ modulated the gene expression of anti and pro-inflammatory cytokines (IL-1, INF-Y, IL-6 and IL-10) on macrophages. Additionally, the anti-F4/80 antibody-coating enhanced natural and adequate antifungal response in the cells, exerting a synergistic effect that prevented the growth of the fungus at the intracellular level. Functionalized NPs can potentially improve macrophage-targeted therapy, increasing NPs endocytosis and intracellular drug concentration. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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Review

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22 pages, 3138 KiB  
Review
Target-Specific Delivery and Bioavailability of Pharmaceuticals via Janus and Dendrimer Particles
by Jaison Jeevanandam, Kei Xian Tan, João Rodrigues and Michael K. Danquah
Pharmaceutics 2023, 15(6), 1614; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15061614 - 29 May 2023
Cited by 3 | Viewed by 1331
Abstract
Nanosized Janus and dendrimer particles have emerged as promising nanocarriers for the target-specific delivery and improved bioavailability of pharmaceuticals. Janus particles, with two distinct regions exhibiting different physical and chemical properties, provide a unique platform for the simultaneous delivery of multiple drugs or [...] Read more.
Nanosized Janus and dendrimer particles have emerged as promising nanocarriers for the target-specific delivery and improved bioavailability of pharmaceuticals. Janus particles, with two distinct regions exhibiting different physical and chemical properties, provide a unique platform for the simultaneous delivery of multiple drugs or tissue-specific targeting. Conversely, dendrimers are branched, nanoscale polymers with well-defined surface functionalities that can be designed for improved drug targeting and release. Both Janus particles and dendrimers have demonstrated their potential to improve the solubility and stability of poorly water-soluble drugs, increase the intracellular uptake of drugs, and reduce their toxicity by controlling the release rate. The surface functionalities of these nanocarriers can be tailored to specific targets, such as overexpressed receptors on cancer cells, leading to enhanced drug efficacy The design of these nanocarriers can be optimized by tuning the size, shape, and surface functionalities, among other parameters. The incorporation of Janus and dendrimer particles into composite materials to create hybrid systems for enhancing drug delivery, leveraging the unique properties and functionalities of both materials, can offer promising outcomes. Nanosized Janus and dendrimer particles hold great promise for the delivery and improved bioavailability of pharmaceuticals. Further research is required to optimize these nanocarriers and bring them to the clinical setting to treat various diseases. This article discusses various nanosized Janus and dendrimer particles for target-specific delivery and bioavailability of pharmaceuticals. In addition, the development of Janus-dendrimer hybrid nanoparticles to address some limitations of standalone nanosized Janus and dendrimer particles is discussed. Full article
(This article belongs to the Special Issue Polymers Enhancing Bioavailability in Drug Delivery, 2nd Edition)
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