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Special Issue "Self-Assembled Amphiphilic Copolymers in Drug Delivery"

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

Deadline for manuscript submissions: closed (28 February 2023) | Viewed by 2863

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Special Issue Editors

Dr. Ana Cazacu

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Guest Editor

Department of Sciences, “Ion Ionescu de la Brad” University of Agricultural Sciences and Veterinary Medicine, 700440 Iasi, Romania
Interests: self-assembled materials; drug delivery systems; controlled release; biomaterials; polymers; liposomes; nanoparticles nanocomposites; nanomaterials synthesis and characterization;

Dr. Elena-Laura Ursu

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Guest Editor

Centre of Advanced Research in Bionanoconjugates and Biopolymers, Petru Poni Institute of Macromolecular Chemistry, 700487 Iasi, Romania
Interests: hybrid nanomaterials; G-quartet hydrogels; nanomaterials synthesis and characterization; atomic force microscopy; Raman and SERS

Special Issue Information

Dear Colleagues,

We are pleased to invite you to publish your valuable research results in this Special Issue titled “Application of Self-Assembled Amphiphilic Copolymers in Drug Delivery”. Amphiphilic copolymers present a unique chemical structure that includes both hydrophilic and hydrophobic chains, which trigger a self-assembling behavior in selective solvents due to the hydrophilic/hydrophobic interactions among different polymer blocks. Based on this behavior, amphiphilic copolymers can form micelles or polymer vesicles (polymersomes), making them attractive for numerous applications in biomedicine, including their usage as drug delivery systems. There is a high demand for new drug-polymer formulations to be used as effective carriers that allow for an efficient controlled release of the active substance in the targeted area. From this point of view, amphiphilic copolymers are emerging in biomedicine, where there is a stringent need for a system responsive to external stimuli (pH, temperature, solvents, etc.) and that is capable of loading and releasing the incorporated drug.

This Special Issue aims to collect papers related to all aspects regarding the development (process engineering, synthesis, characterization, theoretical modelling, etc.) of self-assembled amphiphilic copolymers and their application as new drug delivery systems. In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following:

Synthesis routes and property control;
Fine tuning of amphiphilic copolymers’ properties;
Chemical modifications of amphiphilic copolymers;
Process engineering of polymer matrices;
Encapsulation and delivery of hydrophilic drugs from hydrophobic copolymers;
Encapsulation and delivery of hydrophobic drugs from hydrophilic copolymers;
Controlled drug delivery studies;
Drug targeting.

We look forward to receiving your contributions.

Dr. Ana Cazacu
Dr. Elena-Laura Ursu
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. 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 2600 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

self-assembly
amphiphilic block copolymers
nanostructures
drug delivery systems
targeted drug delivery
controlled release
kinetics studies
carriers
micelles
polymersomes

Published Papers (5 papers)

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Research

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Open AccessArticle

pH-Responsive Poly(ethylene glycol)-b-poly(2-vinylpyridine) Micelles for the Triggered Release of Therapeutics

Kyle Brewer

Fengxiang Bai

and

Anton Blencowe

Pharmaceutics 2023, 15(3), 977; https://doi.org/10.3390/pharmaceutics15030977 - 18 Mar 2023

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Abstract

The use of pH-responsive polymeric micelles is a promising approach to afford the targeted, pH-mediated delivery of hydrophobic drugs within the low-pH tumour milieu and intracellular organelles of cancer cells. However, even for a common pH-responsive polymeric micelle system—e.g., those utilising poly(ethylene glycol)-b-poly(2-vinylpyridine) (PEG-b-PVP) diblock copolymers—there is a lack of available data describing the compatibility of hydrophobic drugs, as well as the relationships between copolymer microstructure and drug compatibility. Furthermore, synthesis of the constituent pH-responsive copolymers generally requires complex temperature control or degassing procedures that limit their accessibility. Herein we report the facile synthesis of a series of diblock copolymers via visible-light-mediated photocontrolled reversible addition-fragmentation chain-transfer polymerisation, with a constant PEG block length (90 repeat units (RUs)) and varying PVP block lengths (46–235 RUs). All copolymers exhibited narrow dispersity values (Đ ≤ 1.23) and formed polymeric micelles with low polydispersity index (PDI) values (typically <0.20) at physiological pH (7.4), within a suitable size range for passive tumour targeting (<130 nm). The encapsulation and release of three hydrophobic drugs (cyclin-dependent kinase inhibitor (CDKI)-73, gossypol, and doxorubicin) were investigated in vitro at pH 7.4–4.5 to simulate drug release within the tumour milieu and cancer cell endosome. Marked differences in drug encapsulation and release were observed when the PVP block length was increased from 86 to 235 RUs. With a PVP block length of 235 RUs, the micelles exhibited differing encapsulation and release properties for each drug. Minimal release was observed for doxorubicin (10%, pH 4.5) and CDKI-73 exhibited moderate release (77%, pH 4.5), whereas gossypol exhibited the best combination of encapsulation efficiency (83%) and release (91% pH 4.5) overall. These data demonstrate the drug selectivity of the PVP core, where both the block molecular weight and hydrophobicity of the core (and accordingly the hydrophobicity of the drug) have a significant effect on drug encapsulation and release. These systems remain a promising means of achieving targeted, pH-responsive drug delivery—albeit for select, compatible hydrophobic drugs—which warrants their further investigation to develop and evaluate clinically relevant micelle systems. Full article

(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery)

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Open AccessArticle

Synthesis and Characterization of Linear Copolymers Based on Pharmaceutically Functionalized Monomeric Choline Ionic Liquid for Delivery of p-Aminosalicylate

Shadi Keihankhadiv

and

Dorota Neugebauer

Pharmaceutics 2023, 15(3), 860; https://doi.org/10.3390/pharmaceutics15030860 - 07 Mar 2023

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Abstract

Bioactive linear poly(ionic liquid)s (PIL) were designed as carriers in drug delivery systems (DDS). Their synthesis was based on a monomeric ionic liquid (MIL) with a relevant pharmaceutical anion to create therapeutically functionalized monomers, which further can be used in the controlled atom transfer radical polymerization (ATRP). The presence of chloride counterions in the quaternary ammonium groups of choline MIL, e.g., [2-(methacryloyloxy)ethyl]trimethyl-ammonium chloride (ChMACl), was stimulated to undergo the anion exchange with p-aminosalicylate sodium salt (NaPAS) as the source of the pharmaceutical anion with antibacterial activity. The resultant [2-(methacryloyloxy)ethyl]trimethylammonium p-aminosalicylate (ChMAPAS) was copolymerized to attain the well-defined linear choline-based copolymers with various contents of PAS anions (24–42%), which were regulated by the initial ratio of ChMAPAS to MMA and conversion degree. The length of polymeric chains was evaluated by the total monomer conversion (31–66%) yielding degree of polymerization (DP_n = 133–272). Depending on the polymer carrier composition, PAS anions were exchanged by 60–100% within 1 h, 80–100% within 4 h, and completely after 24 h by phosphate anions in PBS imitating a physiological fluid. Full article

(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery)

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Open AccessArticle

Revisiting the Solubility–Permeability Relationship with Hydrophobic Drug Umifenovir in Pluronic Solutions: Impact of pH and Co-Solvent

Tatyana Volkova

Olga Simonova

and

German Perlovich

Pharmaceutics 2023, 15(2), 422; https://doi.org/10.3390/pharmaceutics15020422 - 27 Jan 2023

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Abstract

This study describes the influence of pluronic F-127 (F-127) and ethanol (EtOH) on the solubility of umifenovir (UMF) in buffer solutions of pH 2.0 and pH 7.4, and its permeability through cellulose membranes. A 44.4-fold greater UMF solubility in acidic medium as compared to an alkaline one was estimated at 310.15 K. The concentration of UMF in the saturated solution was enhanced by the interaction with F-127 micelles. The combined positive effect of EtOH and F-127 on the solubility was estimated. The aggregation number of F-127 micelles in the presence of 10% and 20% ethanol appeared to be reduced by 2.1-fold and 4.1-fold, respectively, as compared to buffer pH 7.4. The presence of ethanol in buffer pH 7.4 solution provided better solvent conditions but inhibited the formation of F-127 micelles. The impact of UMF on the aggregation number of F-127 was not pronounced and was expressed only by a slight increase of 1 and 3 units in 10% and 20% EtOH, respectively. According to the values of zeta potential, addition of EtOH reduced the stability of the system. The permeation of UMF in buffer pH 7.4 measured through the cellulose membrane MWCO 12–14 kDa was increased 1.4-fold by 10% EtOH. An increase in EtOH content to 20% reduced this effect to 1.2-fold. Decreasing effect of 1.5% F-127 on the permeability was inhibited by using 10% EtOH. The solution containing 1.5% F-127 and 10% EtOH was shown to be an advantageous system for UMF in view of the solubility–permeability balance. The authors suppose the findings of the study to be useful for the design of pharmaceutical formulations based on UMF antiviral drugs. Full article

(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery)

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Open AccessArticle

A CO₂-Responsive Imidazole-Functionalized Fluorescent Material Mediates Cancer Chemotherapy

Vo Thuy Thien Ngan

Po-Yen Chiou

Fasih Bintang Ilhami

Enyew Alemayehu Bayle

and

Pharmaceutics 2023, 15(2), 354; https://doi.org/10.3390/pharmaceutics15020354 - 20 Jan 2023

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Abstract

We present a breakthrough in the synthesis and development of functional gas-responsive materials as highly potent anticancer agents suitable for applications in cancer treatment. Herein, we successfully synthesised a stimuli-responsive multifunctional material (I-R6G) consisting of a carbon dioxide (CO₂)-sensitive imidazole moiety and spirolactam-containing conjugated rhodamine 6G (R6G) molecule. The resulting I-R6G is highly hydrophobic and non- or weakly fluorescent. Simple CO₂ bubbling treatment induces hydrophobic I-R6G to completely dissolve in water and subsequently form self-assembled nanoparticles, which exhibit unique optical absorption and fluorescence behaviours in water and extremely low haemolytic ability against sheep red blood cells. Reversibility testing indicated that I-R6G undergoes reversible CO₂/nitrogen (N₂)-dependent stimulation in water, as its structural and physical properties can be reversibly and stably switched by alternating cycles of CO₂ and N₂ bubbling. Importantly, in vitro cellular assays clearly demonstrated that the CO₂-protonated imidazole moiety promotes rapid internalisation of CO₂-treated I-R6G into cancer cells, which subsequently induces massive levels of necrotic cell death. In contrast, CO₂-treated I-R6G was not internalised and did not affect the viability of normal cells. Therefore, this newly created system may provide an innovative and efficient route to remarkably improve the selectivity, safety and efficacy of cancer treatment. Full article

(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery)

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Review

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Open AccessReview

Polymeric Micellar Systems—A Special Emphasis on “Smart” Drug Delivery

Irina Negut

and

Bogdan Bita

Pharmaceutics 2023, 15(3), 976; https://doi.org/10.3390/pharmaceutics15030976 - 17 Mar 2023

Viewed by 321

Abstract

Concurrent developments in anticancer nanotechnological treatments have been observed as the burden of cancer increases every year. The 21st century has seen a transformation in the study of medicine thanks to the advancement in the field of material science and nanomedicine. Improved drug delivery systems with proven efficacy and fewer side effects have been made possible. Nanoformulations with varied functions are being created using lipids, polymers, and inorganic and peptide-based nanomedicines. Therefore, thorough knowledge of these intelligent nanomedicines is crucial for developing very promising drug delivery systems. Polymeric micelles are often simple to make and have high solubilization characteristics; as a result, they seem to be a promising alternative to other nanosystems. Even though recent studies have provided an overview of polymeric micelles, here we included a discussion on the “intelligent” drug delivery from these systems. We also summarized the state-of-the-art and the most recent developments of polymeric micellar systems with respect to cancer treatments. Additionally, we gave significant attention to the clinical translation potential of polymeric micellar systems in the treatment of various cancers. Full article

(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery)

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