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Pharmaceutics
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Self-Assembled Amphiphilic Copolymers in Drug Delivery, 2nd Edition
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Self-Assembled Amphiphilic Copolymers in Drug Delivery, 2nd Edition

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

Deadline for manuscript submissions: closed (30 April 2025) | Viewed by 9622

Special Issue Editors

Dr. Ana Cazacu

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Guest Editor
Department of Exact Sciences, “Ion Ionescu de la Brad” Iasi University of Life Sciences, 700490 Iasi, Romania
Interests: self-assembled materials; drug delivery systems; controlled release; biomaterials; polymers; liposomes; nanoparticles nanocomposites; nanomaterials synthesis and characterization;
Special Issues, Collections and Topics in MDPI journals
Dr. Elena-Laura Ursu

E-Mail Website
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 Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to invite you to publish your valuable research results in this Special Issue titled “Self-Assembled Amphiphilic Copolymers in Drug Delivery, 2nd Edition”. 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 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

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

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Related Special Issue

Published Papers (5 papers)

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Research

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23 pages, 18590 KiB  
Article
Binary and Ternary Inclusion Complexes of Niflumic Acid: Synthesis, Characterization, and Dissolution Profile
by Zohra Bouchekhou, Amel Hadj Ziane-Zafour, Florentina Geanina Lupascu, Bianca-Ștefania Profire, Alina Nicolescu, Denisse-Iulia Bostiog, Florica Doroftei, Ioan-Andrei Dascalu, Cristian-Dragoș Varganici, Mariana Pinteala, Lenuta Profire, Tudor Pinteala and Bachir Bouzid
Pharmaceutics 2024, 16(9), 1190; https://doi.org/10.3390/pharmaceutics16091190 - 9 Sep 2024
Cited by 1 | Viewed by 1121
Abstract
Although niflumic acid (NA) is one of the most used non-steroidal anti-inflammatory drugs, it suffers from poor solubility, low bioavailability, and significant adverse effects. To address these limitations, the complexation of NA with cyclodextrins (CDs) is a promising strategy. However, complexing CDs with [...] Read more.
Although niflumic acid (NA) is one of the most used non-steroidal anti-inflammatory drugs, it suffers from poor solubility, low bioavailability, and significant adverse effects. To address these limitations, the complexation of NA with cyclodextrins (CDs) is a promising strategy. However, complexing CDs with low molecular weight drugs like NA can lead to low CE. This study explores the development of inclusion complexes of NA with 2-hydroxypropyl-β-cyclodextrin (2HP-β-CD), including the effect of converting NA to its sodium salt (NAs) and adding hydroxypropyl methylcellulose (HPMC) on complex formation. Inclusion complexes were prepared using co-evaporation solvent and freeze-drying methods, and their CE and Ks were determined through a phase solubility study. The complexes were characterized using physicochemical analyses, including FT-IR, DSC, SEM, XRD, DLS, UV-Vis, 1H-NMR, and 1H-ROESY. The dissolution profiles of the complexes were also evaluated. The analyses confirmed complex formation for all systems, demonstrating drug–cyclodextrin interactions, amorphous drug states, morphological changes, and improved solubility and dissolution profiles. The NAs-2HP-β-CD-HPMC complex exhibited the highest CE and Ks values, a 1:1 host-guest molar ratio, and the best dissolution profile. The results indicate that the NAs-2HP-β-CD-HPMC complex has potential for delivering NA, which might enhance its therapeutic effectiveness and minimize side effects. Full article
(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery, 2nd Edition)
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20 pages, 3768 KiB  
Article
Mixed Micellar Gel of Poloxamer Mixture for Improved Solubilization of Poorly Water-Soluble Ibuprofen and Use as Thermosensitive In Situ Gel
by Namon Hirun, Pakorn Kraisit and Supaporn Santhan
Pharmaceutics 2024, 16(8), 1055; https://doi.org/10.3390/pharmaceutics16081055 - 10 Aug 2024
Cited by 2 | Viewed by 1852
Abstract
The aqueous solution of binary mixtures of amphiphilic copolymers is a potential platform for fabricating mixed polymeric micelles for pharmaceutical applications, particularly in developing drug delivery depots for a poorly water-soluble compound. This study fabricated and investigated binary mixtures of poloxamer 403 (P403) [...] Read more.
The aqueous solution of binary mixtures of amphiphilic copolymers is a potential platform for fabricating mixed polymeric micelles for pharmaceutical applications, particularly in developing drug delivery depots for a poorly water-soluble compound. This study fabricated and investigated binary mixtures of poloxamer 403 (P403) and poloxamer 407 (P407) at varying P403:P407 molar ratios to develop a vehicle for the poorly water-soluble compound, using ibuprofen as a model drug. The cooperative formation of mixed micelles was obtained, and the solubility of ibuprofen in the binary mixtures was enhanced compared to the solubility in pure water and an aqueous single P407 solution. The binary mixture with the P403:P407 molar ratio of 0.75:0.25 at a total polymer concentration of 19% w/v exhibited the temperature dependence of micellization and sol-to-gel characteristics of the thermosensitive mixed micellar gels. It possessed suitable micellization and gelation characteristics for in situ gelling systems. The release of ibuprofen from the thermosensitive mixed micellar depots was sustained through a diffusion-controlled mechanism. The findings can aid in formulating binary mixtures of P403 and P407 to achieve the desired properties of mixed micelles and micellar gels. Full article
(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery, 2nd Edition)
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19 pages, 4993 KiB  
Article
Nanosized Complexes of the Proteolytic Enzyme Serratiopeptidase with Cationic Block Copolymer Micelles Enhance the Proliferation and Migration of Human Cells
by Katya Kamenova, Anna Prancheva, Lyubomira Radeva, Krassimira Yoncheva, Maya M. Zaharieva, Hristo M. Najdenski and Petar D. Petrov
Pharmaceutics 2024, 16(8), 988; https://doi.org/10.3390/pharmaceutics16080988 - 25 Jul 2024
Cited by 2 | Viewed by 1115
Abstract
In this study, we describe the preparation of the cationic block copolymer nanocarriers of the proteolytic enzyme serratiopeptidase (SER). Firstly, an amphiphilic poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA9-b-PCL35-b-PDMAEMA9) triblock copolymer was synthesized by reversible addition-fragmentation chain-transfer (RAFT) polymerization. Then, [...] Read more.
In this study, we describe the preparation of the cationic block copolymer nanocarriers of the proteolytic enzyme serratiopeptidase (SER). Firstly, an amphiphilic poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA9-b-PCL35-b-PDMAEMA9) triblock copolymer was synthesized by reversible addition-fragmentation chain-transfer (RAFT) polymerization. Then, cationic micellar nanocarriers consisting of a PCL hydrophobic core and a PDMAEMA hydrophilic shell were formed by the solvent evaporation method. SER was loaded into the polymeric micelles by electrostatic interaction between the positively charged micellar shell and the negatively charged enzyme molecules. The particle size, zeta potential, and colloid stability of complexes as a function of SER concentration were investigated by dynamic and electrophoretic light scattering. It was found that SER retained its proteolytic activity after immobilization in polymeric carriers. Moreover, the complexes have a concentration-dependent enhancing effect on the proliferation and migration of human keratinocyte HaCaT and gingival fibroblast HGF cells. Full article
(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery, 2nd Edition)
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23 pages, 4276 KiB  
Article
Drug Integrating Amphiphilic Nano-Assemblies: 2. Spatiotemporal Distribution within Inflammation Sites
by Teresa De Toni, Teodora Dal Buono, Chris M. Li, Grisell C. Gonzalez, Sung-Ting Chuang, Peter Buchwald, Alice A. Tomei and Diana Velluto
Pharmaceutics 2024, 16(5), 652; https://doi.org/10.3390/pharmaceutics16050652 - 13 May 2024
Cited by 2 | Viewed by 2037
Abstract
The need for chronic systemic immunosuppression, which is associated with unavoidable side-effects, greatly limits the applicability of allogeneic cell transplantation for regenerative medicine applications including pancreatic islet cell transplantation to restore insulin production in type 1 diabetes (T1D). Cell transplantation in confined sites [...] Read more.
The need for chronic systemic immunosuppression, which is associated with unavoidable side-effects, greatly limits the applicability of allogeneic cell transplantation for regenerative medicine applications including pancreatic islet cell transplantation to restore insulin production in type 1 diabetes (T1D). Cell transplantation in confined sites enables the localized delivery of anti-inflammatory and immunomodulatory drugs to prevent graft loss by innate and adaptive immunity, providing an opportunity to achieve local effects while minimizing unwanted systemic side effects. Nanoparticles can provide the means to achieve the needed localized and sustained drug delivery either by graft targeting or co-implantation. Here, we evaluated the potential of our versatile platform of drug-integrating amphiphilic nanomaterial assemblies (DIANAs) for targeted drug delivery to an inflamed site model relevant for islet transplantation. We tested either passive targeting of intravenous administered spherical nanomicelles (nMIC; 20–25 nm diameter) or co-implantation of elongated nanofibrils (nFIB; 5 nm diameter and >1 μm length). To assess the ability of nMIC and nFIB to target an inflamed graft site, we used a lipophilic fluorescent cargo (DiD and DiR) and evaluated the in vivo biodistribution and cellular uptake in the graft site and other organs, including draining and non-draining lymph nodes, after systemic administration (nMIC) and/or graft co-transplantation (nFIB) in mice. Localized inflammation was generated either by using an LPS injection or by using biomaterial-coated islet-like bead implantation in the subcutaneous site. A cell transplant inflammation model was used as well to test nMIC- and nFIB-targeted biodistribution. We found that nMIC can reach the inflamed site after systemic administration, while nFIB remains localized for several days after co-implantation. We confirmed that DIANAs are taken up by different immune cell populations responsible for graft inflammation. Therefore, DIANA is a useful approach for targeted and/or localized delivery of immunomodulatory drugs to decrease innate and adaptive immune responses that cause graft loss after transplantation of therapeutic cells. Full article
(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery, 2nd Edition)
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Review

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30 pages, 2633 KiB  
Review
Polymersomes as Innovative, Stimuli-Responsive Platforms for Cancer Therapy
by Irina Negut and Bogdan Bita
Pharmaceutics 2024, 16(4), 463; https://doi.org/10.3390/pharmaceutics16040463 - 26 Mar 2024
Cited by 5 | Viewed by 2381
Abstract
This review addresses the urgent need for more targeted and less toxic cancer treatments by exploring the potential of multi-responsive polymersomes. These advanced nanocarriers are engineered to deliver drugs precisely to tumor sites by responding to specific stimuli such as pH, temperature, light, [...] Read more.
This review addresses the urgent need for more targeted and less toxic cancer treatments by exploring the potential of multi-responsive polymersomes. These advanced nanocarriers are engineered to deliver drugs precisely to tumor sites by responding to specific stimuli such as pH, temperature, light, hypoxia, and redox conditions, thereby minimizing the side effects associated with traditional chemotherapy. We discuss the design, synthesis, and recent applications of polymersomes, emphasizing their ability to improve therapeutic outcomes through controlled drug release and targeted delivery. Moreover, we highlight the critical areas for future research, including the optimization of polymersome–biological interactions and biocompatibility, to facilitate their clinical adoption. Multi-responsive polymersomes emerge as a promising development in nanomedicine, offering a pathway to safer and more effective cancer treatments. Full article
(This article belongs to the Special Issue Self-Assembled Amphiphilic Copolymers in Drug Delivery, 2nd Edition)
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