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Natural Polymers in Drug Controlled Release Systems

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A special issue of Polymers (ISSN 2073-4360). This special issue belongs to the section "Biomacromolecules, Biobased and Biodegradable Polymers".

Deadline for manuscript submissions: closed (20 July 2022) | Viewed by 12241

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Special Issue Editors

Dr. Roberto Ruiz-Caro

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Guest Editor

Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, 28040 Madrid, Spain
Interests: drug controlled release; HIV; microbicides; mucoadhesiveness; natural polymers; vaginal route
Special Issues, Collections and Topics in MDPI journals

Dr. Aitana Tamayo

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Co-Guest Editor

Ceramics and Glass Institute, CSIC, Kelsen 5, 28049 Madrid, Spain
Interests: materials characterization; nanotechnology; nanomaterials synthesis; natural polymers films; advanced materials; controlled release
Special Issues, Collections and Topics in MDPI journals

Dr. Maria-Dolores Veiga

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Co-Guest Editor

Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University, 28040 Madrid, Spain
Interests: drug controlled release; smart release; mucoadhesive vaginal systems; cyclodextrins; natural polymers
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural polymers, specifically natural polysaccharides are extremely common, cheap, and widespread in nature. They play crucial roles in a huge number of research areas such as health, food, cosmetics, chemicals, biotechnology, etc., and more specifically in the pharmaceutical field. Thus, polymers derivatives from natural sources are used to elaborate different types of pharmaceutical dosage forms for various routes of administration, such as oral, vaginal, ocular, etc., due to their properties such as mucoadhesion, biodegradability, pH-dependent swelling, increasing their use in research due to their low price too, on modified release dosage forms.

For these reasons, the synthetic/chemical/enzymatic preparation and the use of not well-known natural polymers and small natural polymers modifications via different methods could be used to obtain novel properties and applications within modified drug release.

This Special Issue is devoted to the most recent research on these topics, covering all aspects concerning the structural modification and application of new natural polymers in drug-controlled release dosage forms.

Dr. Roberto Ruiz-Caro
Dr. Aitana Tamayo
Dr. Maria-Dolores Veiga
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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. Polymers is an international peer-reviewed open access semimonthly 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 2700 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

pharmaceutical technology
natural polymers
controlled release
drug delivery system
mucoadhesion
swelling behavior
structural characterization
structural modification

Published Papers (4 papers)

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Research

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12 pages, 2244 KiB

Open AccessArticle

Thiolated 2-Methyl-β-Cyclodextrin as a Mucoadhesive Excipient for Poorly Soluble Drugs: Synthesis and Characterization

by Brunella Grassiri, Andrea Cesari, Federica Balzano, Chiara Migone, Gergely Kali, Andreas Bernkop-Schnürch, Gloria Uccello-Barretta, Ylenia Zambito and Anna Maria Piras

Polymers 2022, 14(15), 3170; https://0-doi-org.brum.beds.ac.uk/10.3390/polym14153170 - 03 Aug 2022

Cited by 5 | Viewed by 1845

Abstract

Thiolated cyclodextrins are structurally simple mucoadhesive macromolecules, which are able to host drugs and increase their apparent water solubility, as well as interact with the mucus layer prolonging drug residence time on the site of absorption. The aim of this study was to synthesize through green microwave-assisted process a freely soluble thiolated 2-methyl-β-cyclodextrin (MβCD-SH). Its inclusion complex properties with dexamethasone (Dex), a poor water soluble drug, and mucoadhesive characteristics were also determined. The product was deeply characterized through NMR spectroscopy (2D COSY, 2D HSQC, 1D/2D TOCSY, and 1D ROESY), showing a thiolation degree of 67%, a selective thiolation on the C₆ residues and a monomeric structure. The association constant of MβCD and MβCD-SH with Dex resulted in 2514.3 ± 32.3 M⁻¹ and 2147.0 ± 69.3 M⁻¹, respectively, indicating that both CDs were able to host the drug. Microrheological analysis of mucin in the presence of MBCD-SH showed an increase of complex viscosity, G′ and G″, due to disulphide bond formation. The cytotoxicity screening on fibroblast BALB/3T3 clone A31 cells indicated an IC₅₀ of 27.7 mg/mL and 30.0 mg/mL, for MβCD and MβCD-SH, respectively. Finally, MβCD-SH was able to self-assemble in water into nanometric structures, both in the presence and absence of the complexed drug. Full article

(This article belongs to the Special Issue Natural Polymers in Drug Controlled Release Systems)

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14 pages, 28465 KiB

Open AccessArticle

Development of Natural Polysaccharide–Based Nanoparticles of Berberine to Enhance Oral Bioavailability: Formulation, Optimization, Ex Vivo, and In Vivo Assessment

by Kanchan Kohli, Ali Mujtaba, Rozina Malik, Saima Amin, Md Sarfaraz Alam, Abuzer Ali, Md. Abul Barkat and Mohammad Javed Ansari

Polymers 2021, 13(21), 3833; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13213833 - 05 Nov 2021

Cited by 26 | Viewed by 3155

Abstract

The phytogenous alkaloid berberine (BBR) has become a potential drug for the treatment of diabetes, hyperlipidemia, and cancer. However, its therapeutic potential is limited because ofpoor intestinal absorption due to its efflux by the P-gp expressed in the intestinal lumen. Therefore, we aimed to design and fabricate a nanoparticulate system for delivery of BBR employing naturally derived biodegradable and biocompatible polymers, mainly chitosan and alginate, to enhance the oral bioavailability of BBR. A chitosan-alginate nanoparticle system loaded with BBR (BNPs) was formulated by ionic gelation method and was optimized by employing a three-factor, three-level Box-Behnken statistical design. BNPs were characterized for various physicochemical properties, ex vivo, and in vivo evaluations. The optimized BNPs were found to be 202.2 ± 4.9 nm in size, with 0.236 ± 0.02 of polydispersity index, zeta potential −14.8 ± 1.1 mV, and entrapment efficiency of 85.69 ± 2.6%. BNPs showed amorphous nature with no prominent peak in differential scanning calorimetry (DSC) investigation. Similarly, fourier-transform infrared spectroscopy (FTIR) studies did not reveal any interaction between BBR and excipients used. The drug release followed Higuchi kinetics, since these plots demonstrated the highest linearity (R² = 0.9636), and the mechanism of release was determined to be anomalous or non-Fickian in nature. An ex-vivo gut permeation study showed that BNPs were better internalized into the cells and more highly permeated through the intestine. Furthermore, in vivo pharmacokinetic analysis in female Wistar rats showed a 4.10−fold increase in the oral bioavailability of BBR from BNPs as compared to BBR suspension. With these findings, we have gained new insight into the effective delivery of poorly soluble and permeable drugs via a chitosan-alginate nanoparticle system to improve the therapeutic performance of an oral nanomedicine. Full article

(This article belongs to the Special Issue Natural Polymers in Drug Controlled Release Systems)

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18 pages, 3474 KiB

Open AccessArticle

Self-Assembled Silk Fibroin-Based Aggregates for Delivery of Camptothecin

by Javier Pérez Quiñones, Cornelia Roschger, Andreas Zierer, Carlos Peniche-Covas and Oliver Brüggemann

Polymers 2021, 13(21), 3804; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13213804 - 03 Nov 2021

Cited by 2 | Viewed by 1562

Abstract

A water-soluble hydrolysate of silk fibroin (SF) (~30 kDa) was esterified with tocopherol, ergocalciferol, and testosterone to form SF aggregates for the controlled delivery of the anticancer drug camptothecin (CPT). Elemental analysis and ¹H NMR spectroscopy showed a degree of substitution (DS) on SF of 0.4 to 3.8 mol %. Yields of 58 to 71% on vitamins- and testosterone-grafted SF conjugates were achieved. CPT was efficiently incorporated into the lipophilic core of SF aggregates using a dialysis–precipitation method, achieving drug contents of 6.3–8.5 wt %. FTIR spectra and DSC thermograms showed that tocopherol- and testosterone-grafted SF conjugates predominantly adopted a β-sheet conformation. After the esterification of tyrosine residues on SF chains with the vitamin or testosterone, the hydrodynamic diameters almost doubled or tripled that of SF. The zeta potential values after esterification increased to about −30 mV, which favors the stability of aggregates in aqueous medium. Controlled and almost quantitative release of CPT was achieved after 6 days in PBS at 37 °C, with almost linear release during the first 8 h. MCF-7 cancer cells exhibited good uptake of CPT-loaded SF aggregates after 6 h, causing cell death and cell cycle arrest in the G2/M phase. Substantial uptake of the CPT-loaded aggregates into MCF-7 spheroids was shown after 3 days. Furthermore, all CPT-loaded SF aggregates demonstrated superior toxicity to MCF-7 spheroids compared with parent CPT. Blank SF aggregates induced no hemolysis at pH 6.2 and 7.4, while CPT-loaded SF aggregates provoked hemolysis at pH 6.2 but not at pH 7.4. In contrast, parent CPT caused hemolysis at both pH tested. Therefore, CPT-loaded SF aggregates are promising candidates for chemotherapy. Full article

(This article belongs to the Special Issue Natural Polymers in Drug Controlled Release Systems)

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Review

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27 pages, 3420 KiB

Open AccessReview

Naturally Occurring Polyelectrolytes and Their Use for the Development of Complex-Based Mucoadhesive Drug Delivery Systems: An Overview

by Raúl Cazorla-Luna, Araceli Martín-Illana, Fernando Notario-Pérez, Roberto Ruiz-Caro and María-Dolores Veiga

Polymers 2021, 13(14), 2241; https://0-doi-org.brum.beds.ac.uk/10.3390/polym13142241 - 08 Jul 2021

Cited by 35 | Viewed by 4467

Abstract

Biopolymers have several advantages for the development of drug delivery systems, since they are biocompatible, biodegradable and easy to obtain from renewable resources. However, their most notable advantage may be their ability to adhere to biological tissues. Many of these biopolymers have ionized forms, known as polyelectrolytes. When combined, polyelectrolytes with opposite charges spontaneously form polyelectrolyte complexes or multilayers, which have great functional versatility. Although only one natural polycation—chitosan has been widely explored until now, it has been combined with many natural polyanions such as pectin, alginate and xanthan gum, among others. These polyelectrolyte complexes have been used to develop multiple mucoadhesive dosage forms such as hydrogels, tablets, microparticles, and films, which have demonstrated extraordinary potential to administer drugs by the ocular, nasal, buccal, oral, and vaginal routes, improving both local and systemic treatments. The advantages observed for these formulations include the increased bioavailability or residence time of the formulation in the administration zone, and the avoidance of invasive administration routes, leading to greater therapeutic compliance. Full article

(This article belongs to the Special Issue Natural Polymers in Drug Controlled Release Systems)

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