Drug-Loaded Colloidal Systems in Nanomedicine II

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

Deadline for manuscript submissions: closed (31 May 2022) | Viewed by 28483

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Special Issue Editor

Special Issue Information

Dear Colleagues,

Further to the success of the Special Issue of Polymers “Polymeric Colloidal Systems in Nanomedicine”, I am delighted to reopen this Special Issue, now entitled “Drug-Loaded Colloidal Systems in Nanomedicine II”.

This Special Issue will integrate fundamental research with the practical application of colloidal systems in the field of nanomedicine. Of practical interest are the drug-loaded colloidal systems, such as micelles, polymersomes, nanogels, liposomes, nanocapsules, polymeric, inorganic nanoparticles, etc., with diameters in the range of 10 nm to 400 nm. Another domain of interest is that of functionalized colloidal systems with specific ligands for active targeted drug delivery.

The authors will try to explain the correlations between the molecular characteristics of the starting polymers and colloidal characteristics, as well as the encapsulation efficiency and/or the drug release kinetics. In vitro biological analyses are welcome but not mandatory. Regular research articles and reviews will be accepted for publication in this Special Issue.

Prof. Dr. Leonard Atanase
Guest Editor

Manuscript Submission Information

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Keywords

  • Polymeric colloids
  • Micelles
  • Nanogels
  • Liposomes
  • Nanoparticles
  • Drug delivery

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Published Papers (10 papers)

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Research

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15 pages, 10367 KiB  
Article
Drug Delivery Systems Based on Pluronic Micelles with Antimicrobial Activity
by Corina Popovici, Marcel Popa, Valeriu Sunel, Leonard Ionut Atanase and Daniela Luminita Ichim
Polymers 2022, 14(15), 3007; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14153007 - 25 Jul 2022
Cited by 16 | Viewed by 2071
Abstract
Bacterial oral diseases are chronic, and, therefore, require appropriate treatment, which involves various forms of administration and dosing of the drug. However, multimicrobial resistance is an increasing issue, which affects the global health system. In the present study, a commercial amphiphilic copolymer, Pluronic [...] Read more.
Bacterial oral diseases are chronic, and, therefore, require appropriate treatment, which involves various forms of administration and dosing of the drug. However, multimicrobial resistance is an increasing issue, which affects the global health system. In the present study, a commercial amphiphilic copolymer, Pluronic F127, was used for the encapsulation of 1-(5′-nitrobenzimidazole-2′-yl-sulphonyl-acetyl)-4-aryl-thiosemicarbazide, which is an original active pharmaceutical ingredient (API) previously synthesized and characterized by our group, at different copolymer/API weight ratios. The obtained micellar systems, with sizes around 20 nm, were stable during 30 days of storage at 4 °C, without a major increase of the Z-average sizes. As expected, the drug encapsulation and loading efficiencies varied with the copolymer/API ratio, the highest values of 84.8 and 11.1%, respectively being determined for the F127/API = 10/1 ratio. Moreover, in vitro biological tests have demonstrated that the obtained polymeric micelles (PMs) are both hemocompatible and cytocompatible. Furthermore, enhanced inhibition zones of 36 and 20 mm were observed for the sample F127/API = 2/1 against S. aureus and E. coli, respectively. Based on these encouraging results, it can be admitted that these micellar systems can be an efficient alternative for the treatment of bacterial oral diseases, being suitable either by injection or by a topical administration. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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21 pages, 8405 KiB  
Article
Preparation of DNC Solid Dispersion by a Mechanochemical Method with Glycyrrhizic Acid and Polyvinylpyrrolidone to Enhance Bioavailability and Activity
by Min Lu, Wei Wei, Wenhao Xu, Nikolay E. Polyakov, Alexandr V. Dushkin and Weike Su
Polymers 2022, 14(10), 2037; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14102037 - 16 May 2022
Cited by 2 | Viewed by 1797
Abstract
To exploit aqueous-soluble formulation and improve the anticoccidial activity of 4,4′-dinitrocarbanilide (DNC, active component of nicarbazin), this paper prepared DNC/GA/PVP K30 solid dispersion (SD) with glycyrrhizic acid (GA) and polyvinylpyrrolidone (PVP) K30 by a mechanical ball milling method without using any organic solvent. [...] Read more.
To exploit aqueous-soluble formulation and improve the anticoccidial activity of 4,4′-dinitrocarbanilide (DNC, active component of nicarbazin), this paper prepared DNC/GA/PVP K30 solid dispersion (SD) with glycyrrhizic acid (GA) and polyvinylpyrrolidone (PVP) K30 by a mechanical ball milling method without using any organic solvent. Fourier transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy were used for the solid state characterization. High performance liquid chromatography, critical micelle concentration, particle characterization, and transmission electron microscopy were used to evaluate the behavior in aqueous solution. In addition, the oral bioavailability, tissue distribution, and anticoccidial activity of DNC/GA/PVP K30 SD were investigated as well. Compared with free drug, the novel formulation not only improved the solubility and dissolution rate of DNC, but also inhibited the fecal output of oocysts and enhanced the therapeutic effect of coccidiosis. According to the experiment results, the DNC/GA/PVP K30 SD increased 4.64-fold in oral bioavailability and dramatically enhanced the concentration in liver which provided a basis for further research in schistosomiasis. In summary, our findings suggested that DNC/GA/PVP K30 SD may have promising applications in the treatment of coccidiosis. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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27 pages, 16933 KiB  
Article
Assessment of Physicochemical and In Vivo Biological Properties of Polymeric Nanocapsules Based on Chitosan and Poly(N-vinyl pyrrolidone-alt-itaconic anhydride)
by Kheira Zanoune Dellali, Mohammed Dellali, Delia Mihaela Raţă, Anca Niculina Cadinoiu, Leonard Ionut Atanase, Marcel Popa, Mihaela-Claudia Spataru and Carmen Solcan
Polymers 2022, 14(9), 1811; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14091811 - 28 Apr 2022
Cited by 3 | Viewed by 1799
Abstract
Drug delivery is an important field of nanomedicine, and its aim is to deliver specific active substances to a precise site of action in order to produce a desired pharmacological effect. In the present study nanocapsules were obtained by a process of interfacial [...] Read more.
Drug delivery is an important field of nanomedicine, and its aim is to deliver specific active substances to a precise site of action in order to produce a desired pharmacological effect. In the present study nanocapsules were obtained by a process of interfacial condensation between chitosan (dissolved in the aqueous phase) and poly(N-vinyl pyrrolidone-alt-itaconic anhydride), a highly reactive copolymer capable of easily opening the anhydride ring under the action of amine groups of chitosan. The formed amide bonds led to the formation of a hydrogel membrane. The morphology of the obtained nanocapsules, their behavior in aqueous solution of physiological pH, and their ability to encapsulate and release a model drug can be modulated by the parameters of the synthesis process, such as the molar ratio between functional groups of polymers and the ratio of the phases in which the polymers are solubilized. Although a priori both polymers are biocompatible, this paper reports the results of a very detailed in vivo study conducted on experimental animals which have received the obtained nanocapsules by three administration routes—intraperitoneal, subcutaneous, and oral. The organs taken from the animals’ kidney, liver, spleen, and lung and analyzed histologically demonstrated the ability of nanocapsules to stimulate the monocytic macrophage system without producing inflammatory changes. Moreover, their in vivo behavior has been shown to depend not only on the route of administration but also on the interaction with the cells of the organs with which they come into contact. The results clearly argue the biocompatibility of nanocapsules and hence the possibility of their safe use in biomedical applications. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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18 pages, 3045 KiB  
Article
Development and Characterization of PEGylated Fatty Acid-Block-Poly(ε-caprolactone) Novel Block Copolymers and Their Self-Assembled Nanostructures for Ocular Delivery of Cyclosporine A
by Ziyad Binkhathlan, Abdullah H. Alomrani, Olsi Hoxha, Raisuddin Ali, Mohd Abul Kalam and Aws Alshamsan
Polymers 2022, 14(9), 1635; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14091635 - 19 Apr 2022
Cited by 9 | Viewed by 1930
Abstract
Low aqueous solubility and membrane permeability of some drugs are considered major limitations for their use in clinical practice. Polymeric micelles are one of the potential nano-drug delivery systems that were found to ameliorate the low aqueous solubility of hydrophobic drugs. The main [...] Read more.
Low aqueous solubility and membrane permeability of some drugs are considered major limitations for their use in clinical practice. Polymeric micelles are one of the potential nano-drug delivery systems that were found to ameliorate the low aqueous solubility of hydrophobic drugs. The main objective of this study was to develop and characterize a novel copolymer based on poly (ethylene glycol) stearate (Myrj™)-block-poly(ε-caprolactone) (Myrj-b-PCL) and evaluate its potential as a nanosystem for ocular delivery of cyclosporine A (CyA). Myrj-b-PCL copolymer with various PCL/Myrj ratios were synthesized via ring-opening bulk polymerization of ε-caprolactone using Myrj (Myrj S40 or Myrj S100), as initiators and stannous octoate as a catalyst. The synthesized copolymers were characterized using 1H NMR, GPC, FTIR, XRD, and DSC. The co-solvent evaporation method was used to prepare CyA-loaded Myrj-b-PCL micelles. The prepared micelles were characterized for their size, polydispersity, and CMC using the dynamic light scattering (DLS) technique. The results from the spectroscopic and thermal analyses confirmed the successful synthesis of the copolymers. Transmission electron microscopy (TEM) images of the prepared micelles showed spherical shapes with diameters in the nano range (<200 nm). Ex vivo corneal permeation study showed sustained release of CyA from the developed Myrj S100-b-PCL micelles. In vivo ocular irritation study (Draize test) showed that CyA-loaded Myrj S100-b-PCL88 was well tolerated in the rabbit eye. Our results point to a great potential of Myrj S100-b-PCL as an ocular drug delivery system. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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20 pages, 4281 KiB  
Article
Preclinical Evaluation of Polymeric Nanocomposite Containing Pregabalin for Sustained Release as Potential Therapy for Neuropathic Pain
by Rafaela Figueiredo Rodrigues, Juliana Barbosa Nunes, Sandra Barbosa Neder Agostini, Paloma Freitas dos Santos, Juliana Cancino-Bernardi, Rodrigo Vicentino Placido, Thamyris Reis Moraes, Jennifer Tavares Jacon Freitas, Gislaine Ribeiro Pereira, Flávia Chiva Carvalho, Giovane Galdino and Vanessa Bergamin Boralli
Polymers 2021, 13(21), 3837; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13213837 - 06 Nov 2021
Cited by 1 | Viewed by 2622
Abstract
This study offers a novel oral pregabalin (PG)-loaded drug delivery system based on chitosan and hypromellose phthalate-based polymeric nanocomposite in order to treat neuropathic pain (PG-PN). PG-PN has a particle size of 432 ± 20 nm, a polydispersity index of 0.238 ± 0.001, [...] Read more.
This study offers a novel oral pregabalin (PG)-loaded drug delivery system based on chitosan and hypromellose phthalate-based polymeric nanocomposite in order to treat neuropathic pain (PG-PN). PG-PN has a particle size of 432 ± 20 nm, a polydispersity index of 0.238 ± 0.001, a zeta potential of +19.0 ± 0.9 mV, a pH of 5.7 ± 0.06, and a spherical shape. Thermal and infrared spectroscopy confirmed nanocomposite generation. PG-PN pharmacokinetics was studied after a single oral dose in male Wistar rats. PG-PN showed greater distribution and clearance than free PG. The antinociceptive effect of PG-PN in neuropathic pain rats was tested by using the chronic constriction injury model. The parameter investigated was the mechanical nociceptive threshold measured by the von Frey filaments test; PG-PN showed a longer antinociceptive effect than free PG. The rota-rod and barbiturate sleep induction procedures were used to determine adverse effects; the criteria included motor deficit and sedative effects. PG-PN and free PG had plenty of motors. PG-PN exhibited a less sedative effect than free PG. By prolonging the antinociceptive effect and decreasing the unfavorable effects, polymeric nanocomposites with pregabalin have shown promise in treating neuropathic pain. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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16 pages, 11537 KiB  
Article
Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release
by Raissa Lohanna Gomes Quintino Corrêa, Renan dos Santos, Lindomar José Calumby Albuquerque, Gabriel Lima Barros de Araujo, Charlotte Jennifer Chante Edwards-Gayle, Fabio Furlan Ferreira and Fanny Nascimento Costa
Polymers 2021, 13(18), 3158; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13183158 - 18 Sep 2021
Cited by 2 | Viewed by 2111
Abstract
Ciprofibrate (CIP) is a highly lipophilic and poorly water-soluble drug, typically used for dyslipidemia treatment. Although it is already commercialized in capsules, no previous studies report its solid-state structure; thus, information about the correlation with its physicochemical properties is lacking. In parallel, recent [...] Read more.
Ciprofibrate (CIP) is a highly lipophilic and poorly water-soluble drug, typically used for dyslipidemia treatment. Although it is already commercialized in capsules, no previous studies report its solid-state structure; thus, information about the correlation with its physicochemical properties is lacking. In parallel, recent studies have led to the improvement of drug administration, including encapsulation in polymeric nanoparticles (NPs). Here, we present CIP’s crystal structure determined by PXRD data. We also propose an encapsulation method for CIP in micelles produced from Pluronic P123/F127 and PEO-b-PCL, aiming to improve its solubility, hydrophilicity, and delivery. We determined the NPs’ physicochemical properties by DLS, SLS, ELS, SAXS and the loaded drug amount by UV-Vis spectroscopy. Micelles showed sizes around 10–20 nm for Pluronic and 35–45 nm for the PEO-b-PCL NPs with slightly negative surface charge and successful CIP loading, especially for the latter; a substantial reduction in ζ-potential may be evidenced. For Pluronic nanoparticles, we scanned different conditions for the CIP loading, and its encapsulation efficiency was reduced while the drug content increased in the nanoprecipitation protocol. We also performed in vitro release experiments; results demonstrate that probe release is driven by Fickian diffusion for the Pluronic NPs and a zero-order model for PEO-b-PCL NPs. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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18 pages, 2346 KiB  
Article
Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization
by Ana María Martínez-Relimpio, Marta Benito, Elena Pérez-Izquierdo, César Teijón, Rosa María Olmo and María Dolores Blanco
Polymers 2021, 13(13), 2083; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13132083 - 24 Jun 2021
Cited by 6 | Viewed by 2323
Abstract
Among the different ways to reduce the secondary effects of antineoplastic drugs in cancer treatment, the use of nanoparticles has demonstrated good results due to the protection of the drug and the possibility of releasing compounds to a specific therapeutic target. The α-isoform [...] Read more.
Among the different ways to reduce the secondary effects of antineoplastic drugs in cancer treatment, the use of nanoparticles has demonstrated good results due to the protection of the drug and the possibility of releasing compounds to a specific therapeutic target. The α-isoform of the folate receptor (FR) is overexpressed on a significant number of human cancers; therefore, folate-targeted crosslinked nanoparticles based on BSA and alginate mixtures and loaded with paclitaxel (PTX) have been prepared to maximize the proven antineoplastic activity of the drug against solid tumors. Nanometric-range-sized particles (169 ± 28 nm–296 ± 57 nm), with negative Z-potential values (between −0.12 ± 0.04 and −94.1± 0.4), were synthesized, and the loaded PTX (2.63 ± 0.19–3.56 ±0.13 µg PTX/mg Np) was sustainably released for 23 and 27 h. Three cell lines (MCF-7, MDA-MB-231 and HeLa) were selected to test the efficacy of the folate-targeted PTX-loaded BSA/ALG nanocarriers. The presence of FR on the cell membrane led to a significantly larger uptake of BSA/ALG–Fol nanoparticles compared with the equivalent nanoparticles without folic acid on their surface. The cell viability results demonstrated a cytocompatibility of unloaded nanoparticle–Fol and a gradual decrease in cell viability after treatment with PTX-loaded nanoparticle–Fol due to the sustainable PTX release. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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Review

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25 pages, 1082 KiB  
Review
Paclitaxel Drug Delivery Systems: Focus on Nanocrystals’ Surface Modifications
by Razan Haddad, Nasr Alrabadi, Bashar Altaani and Tonglei Li
Polymers 2022, 14(4), 658; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14040658 - 09 Feb 2022
Cited by 24 | Viewed by 5317
Abstract
Paclitaxel (PTX) is a chemotherapeutic agent that belongs to the taxane family and which was approved to treat various kinds of cancers including breast cancer, ovarian cancer, advanced non-small-cell lung cancer, and acquired immunodeficiency syndrome (AIDS)-related Kaposi’s sarcoma. Several delivery systems for PTX [...] Read more.
Paclitaxel (PTX) is a chemotherapeutic agent that belongs to the taxane family and which was approved to treat various kinds of cancers including breast cancer, ovarian cancer, advanced non-small-cell lung cancer, and acquired immunodeficiency syndrome (AIDS)-related Kaposi’s sarcoma. Several delivery systems for PTX have been developed to enhance its solubility and pharmacological properties involving liposomes, nanoparticles, microparticles, micelles, cosolvent methods, and the complexation with cyclodextrins and other materials that are summarized in this article. Specifically, this review discusses deeply the developed paclitaxel nanocrystal formulations. As PTX is a hydrophobic drug with inferior water solubility properties, which are improved a lot by nanocrystal formulation. Based on that, many studies employed nano-crystallization techniques not only to improve the oral delivery of PTX, but IV, intraperitoneal (IP), and local and intertumoral delivery systems were also developed. Additionally, superior and interesting properties of PTX NCs were achieved by performing additional modifications to the NCs, such as stabilization with surfactants and coating with polymers. This review summarizes these delivery systems by shedding light on their route of administration, the methods used in the preparation and modifications, the in vitro or in vivo models used, and the advantages obtained based on the developed formulations. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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22 pages, 1357 KiB  
Review
Development of Polymer-Based Nanoformulations for Glioblastoma Brain Cancer Therapy and Diagnosis: An Update
by Bijuli Rabha, Kaushik Kumar Bharadwaj, Siddhartha Pati, Bhabesh Kumar Choudhury, Tanmay Sarkar, Zulhisyam Abdul Kari, Hisham Atan Edinur, Debabrat Baishya and Leonard Ionut Atanase
Polymers 2021, 13(23), 4114; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13234114 - 26 Nov 2021
Cited by 21 | Viewed by 2926
Abstract
Brain cancers, mainly high-grade gliomas/glioblastoma, are characterized by uncontrolled proliferation and recurrence with an extremely poor prognosis. Despite various conventional treatment strategies, viz., resection, chemotherapy, and radiotherapy, the outcomes are still inefficient against glioblastoma. The blood–brain barrier is one of the major issues [...] Read more.
Brain cancers, mainly high-grade gliomas/glioblastoma, are characterized by uncontrolled proliferation and recurrence with an extremely poor prognosis. Despite various conventional treatment strategies, viz., resection, chemotherapy, and radiotherapy, the outcomes are still inefficient against glioblastoma. The blood–brain barrier is one of the major issues that affect the effective delivery of drugs to the brain for glioblastoma therapy. Various studies have been undergone in order to find novel therapeutic strategies for effective glioblastoma treatment. The advent of nanodiagnostics, i.e., imaging combined with therapies termed as nanotheranostics, can improve the therapeutic efficacy by determining the extent of tumour distribution prior to surgery as well as the response to a treatment regimen after surgery. Polymer nanoparticles gain tremendous attention due to their versatile nature for modification that allows precise targeting, diagnosis, and drug delivery to the brain with minimal adverse side effects. This review addresses the advancements of polymer nanoparticles in drug delivery, diagnosis, and therapy against brain cancer. The mechanisms of drug delivery to the brain of these systems and their future directions are also briefly discussed. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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35 pages, 27522 KiB  
Review
Antimicrobial Polymeric Structures Assembled on Surfaces
by Iulia Babutan, Alexandra-Delia Lucaci and Ioan Botiz
Polymers 2021, 13(10), 1552; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13101552 - 12 May 2021
Cited by 21 | Viewed by 4283
Abstract
Pathogenic microbes are the main cause of various undesired infections in living organisms, including humans. Most of these infections are favored in hospital environments where humans are being treated with antibiotics and where some microbes succeed in developing resistance to such drugs. As [...] Read more.
Pathogenic microbes are the main cause of various undesired infections in living organisms, including humans. Most of these infections are favored in hospital environments where humans are being treated with antibiotics and where some microbes succeed in developing resistance to such drugs. As a consequence, our society is currently researching for alternative, yet more efficient antimicrobial solutions. Certain natural and synthetic polymers are versatile materials that have already proved themselves to be highly suitable for the development of the next-generation of antimicrobial systems that can efficiently prevent and kill microbes in various environments. Here, we discuss the latest developments of polymeric structures, exhibiting (reinforced) antimicrobial attributes that can be assembled on surfaces and coatings either from synthetic polymers displaying antiadhesive and/or antimicrobial properties or from blends and nanocomposites based on such polymers. Full article
(This article belongs to the Special Issue Drug-Loaded Colloidal Systems in Nanomedicine II)
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