Microfluidics-Facilitated Synthesis of Methacrylated Chitosan-Coated Liposomes: An Innovative Platform for Prolonged Ocular Retention and Controlled Drug Release.

IF 5.5 2区化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY

Biomacromolecules Pub Date : 2025-07-15 DOI:10.1021/acs.biomac.5c00849

Ahmad Mirkani, Mohammad Reza Nabid, Sarvenaz Pakian

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Abstract

This study presents methacrylated chitosan-coated liposomes (CSMA-liposomes) as an innovative ocular drug delivery technology to tackle the issue of rapid drug removal from the eye. Liposomes synthesized via microfluidic techniques were coated with CSMA to enhance mucoadhesion and prolong residence time through electrostatic and covalent interactions with mucin. Liposomal optimization produced uncoated liposomes measuring 154 nm with a PDI of 0.12, which rose to 208 nm following CSMA coating. The zeta potential shifted from -8.3 to +36 mV, indicating effective functionalization. In vitro, CSMA-liposomes exhibited significant mucoadhesion, resulting in a particle size increase to 369 nm and a zeta potential of +2.4 mV after 4 h of incubation with mucin. Ex vivo retention on bovine conjunctival tissues exhibited enhanced fluorescence retention of CSMA-liposomes relative to untreated and chitosan-coated liposomes. The release of dexamethasone sodium phosphate from CSMA-liposomes demonstrated a sustained, biphasic profile, indicating potential for improved ocular bioavailability and therapeutic effectiveness.

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微流体促进甲基丙烯酸壳聚糖包覆脂质体的合成：延长眼潴留和控制药物释放的创新平台。

本研究提出甲基丙烯酸壳聚糖包被脂质体（csma -脂质体）作为一种创新的眼部药物递送技术，以解决药物从眼睛快速移除的问题。利用微流控技术合成的脂质体包被CSMA，通过与粘蛋白的静电和共价相互作用增强黏附并延长停留时间。脂质体优化得到的未包被脂质体尺寸为154 nm， PDI为0.12，包被CSMA后PDI上升至208 nm。zeta电位从-8.3 mV转变为+36 mV，表明功能化有效。在体外，csma脂质体表现出明显的黏附作用，与黏液蛋白孵育4小时后，csma脂质体的粒径增加到369 nm， zeta电位达到+2.4 mV。与未处理和壳聚糖包被的脂质体相比，csma脂质体在牛结膜组织上的体外保留率显示出增强的荧光保留率。地塞米松磷酸钠从csma脂质体的释放表现出持续的双相特征，表明有可能改善眼部生物利用度和治疗效果。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Biomacromolecules 化学-高分子科学

CiteScore

10.60

自引率

4.80%

发文量

417

审稿时长

1.6 months

期刊介绍： Biomacromolecules is a leading forum for the dissemination of cutting-edge research at the interface of polymer science and biology. Submissions to Biomacromolecules should contain strong elements of innovation in terms of macromolecular design, synthesis and characterization, or in the application of polymer materials to biology and medicine. Topics covered by Biomacromolecules include, but are not exclusively limited to: sustainable polymers, polymers based on natural and renewable resources, degradable polymers, polymer conjugates, polymeric drugs, polymers in biocatalysis, biomacromolecular assembly, biomimetic polymers, polymer-biomineral hybrids, biomimetic-polymer processing, polymer recycling, bioactive polymer surfaces, original polymer design for biomedical applications such as immunotherapy, drug delivery, gene delivery, antimicrobial applications, diagnostic imaging and biosensing, polymers in tissue engineering and regenerative medicine, polymeric scaffolds and hydrogels for cell culture and delivery.