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Hu, Litao, et al. International Journal of Biological Macromolecules (2025): 144083.
In this study, chondroitin sulfate (CS) was used as the backbone for constructing dual-drug, dual-targeting polymeric micelles designed for breast cancer therapy. The synthesis involved two distinct drug conjugation strategies. First, flurbiprofen (Fbp) was conjugated to CS via esterification. Specifically, Fbp was activated using EDCI and NHS in anhydrous DMSO, then reacted with CS under mild stirring conditions to yield CS-Fbp (C-F). After 24 h reaction, the product was dialyzed (MWCO 3500 Da) and lyophilized.
Separately, docetaxel (DTX) was modified to introduce a carboxyl group by reacting with succinic anhydride, forming DTX-COOH. This intermediate was activated with EDCI/NHS and reacted with a CS-cystamine conjugate to introduce redox-sensitive disulfide bonds, yielding CS-ss-DTX (C-ss-D). The resulting product was purified via dialysis and lyophilization.
C-F and C-ss-D were then co-assembled in aqueous media through self-assembly into spherical nanomicelles via nanoprecipitation. The micelles were characterized by TEM, DLS, and zeta potential measurements. In vitro drug release studies were conducted under varying pH and GSH concentrations, confirming dual-responsiveness. Fluorescent labeling and CLSM verified CD44-mediated uptake and Golgi targeting in MCF-7 cells.
This synthetic procedure demonstrates CS's utility in building dual-functional nanocarriers through well-controlled ester and disulfide chemistry for targeted drug delivery.
Han, Jiaxin, et al. European Polymer Journal 222 (2025): 113588.
Chondroitin sulfate, a naturally occurring glycosaminoglycan, was effectively employed as a key precursor for synthesizing oxidized chondroitin sulfate (OCS), subsequently used in the fabrication of a temperature-responsive antimicrobial hydrogel (GelOCS@Ag). The process began with the oxidation of chondroitin sulfate using sodium periodate (NaIO₄), yielding dialdehyde-functionalized OCS capable of participating in Schiff-base reactions.
To prepare the GelOCS@Ag hydrogel, OCS was dissolved in a silver nanoparticle (AgNP) aqueous solution (previously synthesized via chemical reduction of AgNO₃ with NaBH₄ in the presence of stabilizing agents such as PVP and trisodium citrate). Separately, gelatin was also dissolved in the same AgNP medium at varying concentrations (25-35% w/v). Equal volumes of OCS and gelatin solutions were then mixed at 37 °C, where Schiff-base crosslinking occurred between the aldehyde groups on OCS and amino groups on gelatin, forming a stable hydrogel matrix embedded with AgNPs.
The resulting GelOCS@Ag hydrogel displayed excellent mechanical strength, reversible adhesion triggered by temperature variation, and potent antimicrobial performance. Adhesion strength could be tuned significantly-from 12.7 kPa at 37 °C to 1.2 kPa at 10 °C-facilitating non-invasive, on-demand removal. This study underscores the utility of chondroitin sulfate in constructing multifunctional wound dressings with smart detachment and infection prevention capabilities.
Nomicisio, Cristian, et al. Carbohydrate Polymer Technologies and Applications 10 (2025): 100711.
Chondroitin sulfate was employed as a key biopolymer in the formulation of LDH-doped microparticles aimed at promoting wound healing. In this study, chondroitin sulfate was co-formulated with alginate and Zn/Al-based layered double hydroxides (LDHs), anionic clays known for their bioactive properties. The hybrid composites were engineered via spray drying to form microparticles with diameters ranging from 10-15 µm and a narrow size distribution.
To prepare the formulation, LDHs were initially dispersed in deionized water, followed by the addition of alginate and chondroitin sulfate. The homogeneous mixture was spray-dried using a Büchi B-190 Mini Spray Dryer under controlled conditions (600 mL/h feed rate, 200 °C inlet, 130 °C outlet). The resulting microparticles were cross-linked to form water-insoluble scaffolds suitable for physiological environments. This was achieved through a two-step CaCl₂ crosslinking procedure: a brief pre-treatment in ethanol and ethanolic CaCl₂, followed by immersion in aqueous 40% CaCl₂.
This study highlights chondroitin sulfate's role in developing biofunctional microparticles for chronic wound therapy.
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