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Pharmaceutics
Special Issues
Polymeric Micelles for Drug Delivery and Cancer Therapy
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Polymeric Micelles for Drug Delivery and Cancer Therapy

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 2024) | Viewed by 5478

Special Issue Editors

Prof. Dr. Jie Pan

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Guest Editor
School of Pharmacy, Tiangong University, Tianjin 300387, China
Interests: cancer; chemotherapy; drug delivery; peptide; prodrug; micelles; theranostics
Dr. Yonghui Liu

E-Mail
Guest Editor
School of Chemistry, Tiangong University, Tianjin 300387, China
Interests: drug delivery; exosome; glycopeptide; glycosylation; oligosaccharide; tumor vaccines

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute to an upcoming Special Issue on "Polymeric Micelles for Drug Delivery and Cancer Therapy". Your expertise and research in this field would serve as a valuable contribution to the advancement of the drug delivery and cancer therapy research community.

Polymeric micelles have emerged as a promising platform for drug delivery applications due to their unique physicochemical properties, such as a high drug loading capacity, controlled drug release, and prolonged circulation time.

The Special Issue aims to highlight the recent progress and advances in the use of polymeric micelles for cancer therapy and drug delivery.

For this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following:

  • Synthesis, characterization, and optimization of polymeric micelles for drug delivery and cancer therapy;
  • Mechanism of drug encapsulation, release, and interaction with biological entities;
  • Preclinical and clinical studies of polymeric micelles for cancer treatment and diagnosis;
  • Combination therapy using multifunctional polymeric micelles;
  • Design and engineering of polymeric micelles for targeted drug delivery.

We encourage submissions that report on novel findings regarding the development, characterization, and application of polymeric micelles in drug delivery and cancer therapy.

We look forward to receiving your contributions.

Prof. Dr. Jie Pan
Dr. Yonghui Liu
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

  • polymeric micelles
  • drug delivery
  • cancer therapy
  • nanoparticles
  • targeted delivery
  • mechanisms
  • preclinical studies
  • clinical trials

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Published Papers (4 papers)

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Research

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22 pages, 6010 KiB  
Article
pH-Sensitive Fluorescent Marker Based on Rhodamine 6G Conjugate with Its FRET/PeT Pair in “Smart” Polymeric Micelles for Selective Imaging of Cancer Cells
by Igor D. Zlotnikov, Alexander A. Ezhov and Elena V. Kudryashova
Pharmaceutics 2024, 16(8), 1007; https://doi.org/10.3390/pharmaceutics16081007 - 30 Jul 2024
Viewed by 320
Abstract
Cancer cells are known to create an acidic microenvironment (the Warburg effect). At the same time, fluorescent dyes can be sensitive to pH, showing a sharp increase or decrease in fluorescence depending on pH. However, modern applications, such as confocal laser scanning microscopy [...] Read more.
Cancer cells are known to create an acidic microenvironment (the Warburg effect). At the same time, fluorescent dyes can be sensitive to pH, showing a sharp increase or decrease in fluorescence depending on pH. However, modern applications, such as confocal laser scanning microscopy (CLSM), set additional requirements for such fluorescent markers to be of practical use, namely, high quantum yield, low bleaching, minimal quenching in the cell environment, and minimal overlap with auto-fluorophores. R6G could be the perfect match for these requirements, but its fluorescence is not pH-dependent. We have attempted to develop an R6G conjugate with its FRET or PeT pair that would grant it pH sensitivity in the desired range (5.5–7.5) and enable the selective targeting of tumor cells, thus improving CLSM imaging. Covalent conjugation of R6G with NBD using a spermidine (spd) linker produced a pH-sensitive FRET effect but within the pH range of 7.0–9.0. Shifting this effect to the target pH range of 5.5–7.5 appeared possible by incorporating the R6G-spd-NBD conjugate within a “smart” polymeric micelle based on chitosan grafted with lipoic acid. In our previous studies, one could conclude that the polycationic properties of chitosan could make this pH shift possible. As a result, the micellar form of the NBD-spd-R6G fluorophore demonstrates a sharp ignition of fluorescence by 40%per1 pH unit in the pH range from 7.5 to 5. Additionally, “smart” polymeric micelles based on chitosan allow the label to selectively target tumor cells. Due to the pH sensitivity of the fluorophore NBD-spd-R6G and the selective targeting of cancer cells, the efficient visualization of A875 and K562 cells was achieved. CLSM imaging showed that the dye actively penetrates cancer cells (A875 and K562), while minimal accumulation and low fluorophore emission are observed in normal cells (HEK293T). It is noteworthy that by using “smart” polymeric micelles based on polyelectrolytes of different charges and structures, we create the possibility of regulating the pH dependence of the fluorescence in the desired interval, which means that these “smart” polymeric micelles can be applied to the visualization of a variety of cell types, organelles, and other structures. Full article
(This article belongs to the Special Issue Polymeric Micelles for Drug Delivery and Cancer Therapy)
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16 pages, 3043 KiB  
Article
Preparation and Primary Bioactivity Evaluation of Novel Water-Soluble Curcumin-Loaded Polymeric Micelles Fabricated with Chitooligosaccharides and Pluronic F-68
by Pattarachat Ingrungruengluet, Dingfu Wang, Xin Li, Cheng Yang, Yaowapha Waiprib and Chunxia Li
Pharmaceutics 2023, 15(10), 2497; https://doi.org/10.3390/pharmaceutics15102497 - 20 Oct 2023
Cited by 2 | Viewed by 2725
Abstract
Curcumin (CU) is a bioactive compound extracted from turmeric and has various advantages. However, the benefit of CU is limited by its low water solubility (11 ng/mL). This research aimed to fabricate a water-soluble CU nano-formulation with chitooligosaccharides (COS) and pluronic F-68 (PF) [...] Read more.
Curcumin (CU) is a bioactive compound extracted from turmeric and has various advantages. However, the benefit of CU is limited by its low water solubility (11 ng/mL). This research aimed to fabricate a water-soluble CU nano-formulation with chitooligosaccharides (COS) and pluronic F-68 (PF) utilizing the polymeric micelle method. The optimized curcumin-loaded chitooligosaccharides/pluronic F-68 micelles (COSPFCU) exhibited high encapsulation efficiency and loading capacity (75.57 ± 2.35% and 10.32 ± 0.59%, respectively). The hydrodynamic diameter of lyophilized COSPFCU was 73.89 ± 11.69 nm with a polydispersity index below 0.3. The COSPFCU could be completely redispersed in water and showed high DPPH scavenging ability. Meanwhile, COSPFCU could significantly reduce the cytotoxicity of the RAW 264.7 cells compared to native CU. Furthermore, COSPFCU improved the inhibition of NO release activity at 72.83 ± 2.37% but 33.20 ± 3.41% for the CU, with a low cytotoxicity concentration in the RAW 264.7 cells. Full article
(This article belongs to the Special Issue Polymeric Micelles for Drug Delivery and Cancer Therapy)
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16 pages, 3908 KiB  
Article
Superparamagnetic Nanocrystals Clustered Using Poly(ethylene glycol)-Crosslinked Amphiphilic Copolymers for the Diagnosis of Liver Cancer
by Ling Jiang, Jiaying Chi, Jiahui Wang, Shaobin Fang, Tingting Peng, Guilan Quan, Daojun Liu, Zhongjie Huang and Chao Lu
Pharmaceutics 2023, 15(9), 2205; https://doi.org/10.3390/pharmaceutics15092205 - 25 Aug 2023
Viewed by 1105
Abstract
Superparamagnetic iron oxide (SPIO) nanocrystals have been extensively studied as theranostic nanoparticles to increase transverse (T2) relaxivity and enhance contrast in magnetic resonance imaging (MRI). To improve the blood circulation time and enhance the diagnostic sensitivity of MRI contrast agents, we [...] Read more.
Superparamagnetic iron oxide (SPIO) nanocrystals have been extensively studied as theranostic nanoparticles to increase transverse (T2) relaxivity and enhance contrast in magnetic resonance imaging (MRI). To improve the blood circulation time and enhance the diagnostic sensitivity of MRI contrast agents, we developed an amphiphilic copolymer, PCPZL, to effectively encapsulate SPIO nanocrystals. PCPZL was synthesized by crosslinking a polyethylene glycol (PEG)-based homobifunctional linker with a hydrophobic star-like poly(ε-benzyloxycarbonyl-L-lysine) segment. Consequently, it could self-assemble into shell-crosslinked micelles with enhanced colloidal stability in bloodstream circulation. Notably, PCPZL could effectively load SPIO nanocrystals with a high loading capacity of 66.0 ± 0.9%, forming SPIO nanoclusters with a diameter of approximately 100 nm, a high cluster density, and an impressive T2 relaxivity value 5.5 times higher than that of Resovist®. In vivo MRI measurements highlighted the rapid accumulation and contrast effects of SPIO-loaded PCPZL micelles in the livers of both healthy mice and nude mice with an orthotopic hepatocellular carcinoma tumor model. Moreover, the magnetic micelles remarkably enhanced the relative MRI signal difference between the tumor and normal liver tissues. Overall, our findings demonstrate that PCPZL significantly improves the stability and magnetic properties of SPIO nanocrystals, making SPIO-loaded PCPZL micelles promising MRI contrast agents for diagnosing liver diseases and cancers. Full article
(This article belongs to the Special Issue Polymeric Micelles for Drug Delivery and Cancer Therapy)
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Review

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18 pages, 6204 KiB  
Review
Advances in 2,3-Dimethylmaleic Anhydride (DMMA)-Modified Nanocarriers in Drug Delivery Systems
by Dong Wan, Yanan Wu, Yujun Liu, Yonghui Liu and Jie Pan
Pharmaceutics 2024, 16(6), 809; https://doi.org/10.3390/pharmaceutics16060809 - 14 Jun 2024
Viewed by 726
Abstract
Cancer represents a significant threat to human health. The cells and tissues within the microenvironment of solid tumors exhibit complex and abnormal properties in comparison to healthy tissues. The efficacy of nanomedicines is inhibited by the presence of substantial and complex physical barriers [...] Read more.
Cancer represents a significant threat to human health. The cells and tissues within the microenvironment of solid tumors exhibit complex and abnormal properties in comparison to healthy tissues. The efficacy of nanomedicines is inhibited by the presence of substantial and complex physical barriers in the tumor tissue. The latest generation of intelligent drug delivery systems, particularly nanomedicines capable of charge reversal, have shown promise in addressing this issue. These systems can transform their charge from negative to positive upon reaching the tumor site, thereby enhancing tumor penetration via transcytosis and promoting cell internalization by interacting with the negatively charged cell membranes. The modification of nanocarriers with 2,3-dimethylmaleic anhydride (DMMA) and its derivatives, which are responsive to weak acid stimulation, represents a significant advance in the field of charge-reversal nanomedicines. This review provides a comprehensive examination of the recent insights into DMMA-modified nanocarriers in drug delivery systems, with a particular focus on their potential in targeted therapeutics. It also discusses the synthesis of DMMA derivatives and their role in charge reversal, shell detachment, size shift, and ligand reactivation mechanisms, offering the prospect of a tailored, next-generation therapeutic approach to overcome the diverse challenges associated with cancer therapy. Full article
(This article belongs to the Special Issue Polymeric Micelles for Drug Delivery and Cancer Therapy)
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