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Drug Delivery Systems Based on Polysaccharides: Second Edition

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Macromolecular Chemistry".

Deadline for manuscript submissions: 30 June 2025 | Viewed by 9109

Special Issue Editors


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Guest Editor
“Cristofor Simionescu” Faculty of Chemical Engineering and Environment Protection, “Gheorghe Asachi” Technical University, 700050 Iasi, Romania
Interests: polysaccharide modification; bioactive polymers; biomaterials; hydrogels; interpenetrated networks; micro- and nanoparticles (spheres and capsules); hybrid and functionalized nanoparticles for drug targeting; drug delivery; polymer–drug conjugates
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Special Issue Information

Dear Colleagues,

The use of polysaccharides in biomedical applications, and especially for obtaining systems capable of encapsulating, transporting, and delivering drugs in a sustained/controlled manner, is an area that has been intensely explored in recent decades, though it remains far from being exhausted. Polysaccharides, and also in large part their derivatives, are ideal supports for these applications, given their biocompatibility with living organisms and being of natural origin themselves. This Special Issue aims to present the latest aspects regarding the realization of polymer–biologically active principle systems in different formats, e.g., films, hydrogels, particles, capsules, implants, inserts, etc., that use polysaccharides and their derivatives as supports. A complementary field of interest is the creation of nanoparticles or nanocapsules for drug delivery, which are, respectively, particles functionalized on the surface with ligands recognizable by receptors that are well expressed in the cell membranes of different organs and hybrid particles containing magnetic nanoparticles encapsulated in polymeric matrices that are capable of active targeting after systemic administration by intravenous injection. Drug-carrying liposomes, stabilized by coating with polysaccharides, as well as their derivatives or copolymers with synthetic polymers, are also of interest for this Special Issue.

Prof. Dr. Marcel Popa
Prof. Dr. Leonard Ionut Atanase
Guest Editors

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Keywords

  • polysaccharides
  • polysaccharide derivatives
  • hydrogels
  • micro- and nanoparticles (spheres and capsules)
  • hybrid nanoparticles
  • functionalized nanoparticles for drug targeting
  • micelles based on amphiphilic polysaccharides
  • drug delivery

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Related Special Issue

Published Papers (4 papers)

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Research

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17 pages, 5620 KiB  
Article
Insulin Conformation Changes in Hybrid Alginate–Gelatin Hydrogel Particles
by Gulzhan Ye. Yerlan, Michael Shen, Bakyt B. Tyussyupova, Sagdat M. Tazhibayeva, Kuanyshbek Musabekov and Paul Takhistov
Molecules 2024, 29(6), 1254; https://doi.org/10.3390/molecules29061254 - 12 Mar 2024
Viewed by 1890
Abstract
There is a strong need to develop an insulin delivery system suitable for oral administration and preserving natural (α-helix) insulin conformation. In this work, we fabricated alginate–gelatin hydrogel beads for insulin encapsulation. Altering matrix composition and crosslinking agents has resulted in various surface [...] Read more.
There is a strong need to develop an insulin delivery system suitable for oral administration and preserving natural (α-helix) insulin conformation. In this work, we fabricated alginate–gelatin hydrogel beads for insulin encapsulation. Altering matrix composition and crosslinking agents has resulted in various surface morphologies and internal spatial organization. The structures of the insulin-loaded matrices were studied using optical and field emission electronic microscopy. We use FTIR spectroscopy to identify insulin conformation changes as affected by the hydrogel matrices. It was found that blended alginate–gelatin matrices demonstrate better encapsulation efficiency and stronger swelling resistance to a simulated gastric environment than sodium alginate beads crosslinked with the CaCl2. FTIR measurements reveal conformation changes in insulin. It is also confirmed that in the presence of gelatin, the process of insulin fibrinogenesis ceases due to intermolecular interaction with the gelatin. Performed molecular modeling shows that dipole–dipole interactions are the dominating mechanism that determines insulin behavior within the fabricated matrix. Full article
(This article belongs to the Special Issue Drug Delivery Systems Based on Polysaccharides: Second Edition)
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20 pages, 15030 KiB  
Article
Angelica Sinensis Polysaccharide-Based Nanoparticles for Liver-Targeted Delivery of Oridonin
by Henglai Sun, Jijuan Nai, Biqi Deng, Zhen Zheng, Xuemei Chen, Chao Zhang, Huagang Sheng and Liqiao Zhu
Molecules 2024, 29(3), 731; https://doi.org/10.3390/molecules29030731 - 5 Feb 2024
Cited by 9 | Viewed by 2470
Abstract
The present work aimed to study the feasibility of Angelica sinensis polysaccharide (ASP) as an instinctive liver targeting drug delivery carrier for oridonin (ORI) in the treatment of hepatocellular carcinoma (HCC). ASP was reacted with deoxycholic acid (DOCA) via an esterification reaction to [...] Read more.
The present work aimed to study the feasibility of Angelica sinensis polysaccharide (ASP) as an instinctive liver targeting drug delivery carrier for oridonin (ORI) in the treatment of hepatocellular carcinoma (HCC). ASP was reacted with deoxycholic acid (DOCA) via an esterification reaction to form an ASP-DOCA conjugate. ORI-loaded ASP-DOCA nanoparticles (ORI/ASP-DOCA NPs) were prepared by the thin-film water method, and their size was about 195 nm in aqueous solution. ORI/ASP-DOCA NPs had a drug loading capacity of up to 9.2%. The release of ORI in ORI/ASP-DOCA NPs was pH-dependent, resulting in rapid decomposition and accelerated drug release at acidic pH. ORI/ASP-DOCA NPs significantly enhanced the accumulation of ORI in liver tumors through ASGPR-mediated endocytosis. In vitro results showed that ORI/ASP-DOCA NPs increased cell uptake and apoptosis in HepG2 cells, and in vivo results showed that ORI/ASP-DOCA NPs caused effective tumor suppression in H22 tumor-bearing mice compared with free ORI. In short, ORI/ASP-DOCA NPs might be a simple, feasible, safe and effective ORI nano-drug delivery system that could be used for the targeted delivery and treatment of liver tumors. Full article
(This article belongs to the Special Issue Drug Delivery Systems Based on Polysaccharides: Second Edition)
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17 pages, 4759 KiB  
Article
Anticancer Activity of Astaxanthin-Incorporated Chitosan Nanoparticles
by Eun Ju Hwang, Young-IL Jeong, Kyong-Je Lee, Young-Bob Yu, Seung-Ho Ohk and Sook-Young Lee
Molecules 2024, 29(2), 529; https://doi.org/10.3390/molecules29020529 - 21 Jan 2024
Cited by 5 | Viewed by 2741
Abstract
Astaxanthin (AST)-encapsulated nanoparticles were fabricated using glycol chitosan (Chito) through electrostatic interaction (abbreviated as ChitoAST) to solve the aqueous solubility of astaxanthin and improve its biological activity. AST was dissolved in organic solvents and then mixed with chitosan solution, followed by a dialysis [...] Read more.
Astaxanthin (AST)-encapsulated nanoparticles were fabricated using glycol chitosan (Chito) through electrostatic interaction (abbreviated as ChitoAST) to solve the aqueous solubility of astaxanthin and improve its biological activity. AST was dissolved in organic solvents and then mixed with chitosan solution, followed by a dialysis procedure. All formulations of ChitoAST nanoparticles showed small diameters (less than 400 nm) with monomodal distributions. Analysis with Fourier transform infrared (FT-IR) spectroscopy confirmed the specific peaks of AST and Chito. Furthermore, ChitoAST nanoparticles were formed through electrostatic interactions between Chito and AST. In addition, ChitoAST nanoparticles showed superior antioxidant activity, as good as AST itself; the half maximal radical scavenging concentrations (RC50) of AST and ChitoAST nanoparticles were 11.8 and 29.3 µg/mL, respectively. In vitro, AST and ChitoAST nanoparticles at 10 and 20 µg/mL properly inhibited the production of intracellular reactive oxygen species (ROSs), nitric oxide (NO), and inducible nitric oxide synthase (iNOS). ChitoAST nanoparticles had no significant cytotoxicity against RAW264.7 cells or B16F10 melanoma cells, whereas AST and ChitoAST nanoparticles inhibited the growth of cancer cells. Furthermore, AST itself and ChitoAST nanoparticles (20 µg/mL) efficiently inhibited the migration of cancer cells in a wound healing assay. An in vivo study using mice and a pulmonary metastasis model showed that ChitoAST nanoparticles were efficiently delivered to a lung with B16F10 cell metastasis; i.e., fluorescence intensity in the lung was significantly higher than in other organs. We suggest that ChitoAST nanoparticles are promising candidates for antioxidative and anticancer therapies of B16F10 cells. Full article
(This article belongs to the Special Issue Drug Delivery Systems Based on Polysaccharides: Second Edition)
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Review

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44 pages, 8843 KiB  
Review
Chitosan and Its Derivatives as Nanocarriers for Drug Delivery
by Ranu Biswas, Sourav Mondal, Md Ahesan Ansari, Tanima Sarkar, Iustina Petra Condiuc, Gisela Trifas and Leonard Ionut Atanase
Molecules 2025, 30(6), 1297; https://doi.org/10.3390/molecules30061297 - 13 Mar 2025
Viewed by 1115
Abstract
Chitosan (CS) occurs naturally as an alkaline polysaccharide and has been demonstrated to have several activities of a biological nature. Additionally, as CS chains have functional hydroxyl and amino groups that are active, their applications can be expanded by chemically or molecularly altering [...] Read more.
Chitosan (CS) occurs naturally as an alkaline polysaccharide and has been demonstrated to have several activities of a biological nature. Additionally, as CS chains have functional hydroxyl and amino groups that are active, their applications can be expanded by chemically or molecularly altering the molecules to incorporate new functional groups. Due to its outstanding qualities, including biodegradability, biocompatibility, non-toxicity, and accessibility, it has received significant interest in all areas of biomedicine and nanomaterials being extremely promising as drug nanocarrier. The last decades have produced a lot of interest in CS-based nanoparticles (CSNPs), with an increasing number of research papers from around 1500 in 2015 to almost 5000 in 2024. The degree of crosslinking, the particulate system’s shape, size, and density, in addition to the drug’s physical and chemical properties, all have a role in how the drug is transported and released from CSNPs. When creating potential drug delivery systems based on CSNPs, all these factors must be considered. In earlier, CSNPs were employed to enhance the pharmacotherapeutics, pharmacokinetics, and solubility properties of drugs. By investigating its positively charged characteristics and changeable functional groups, CS has evolved into a versatile drug delivery system. The drug release from CSNPs will definitely be influenced by various changes to the functional groups, charges, and polymer backbone. This review mainly discusses the most important results published in the last decade. Despite the promising advantages of CSNPs, challenges related to the translation into clinical stages remain and further in vitro and in vivo studies are mandatory. Full article
(This article belongs to the Special Issue Drug Delivery Systems Based on Polysaccharides: Second Edition)
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