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用于按需释放万古霉素并提高抗菌效率的光响应性聚乳酸-羟基乙酸共聚物微粒

Light-Responsive PLGA Microparticles for On-Demand Vancomycin Release and Enhanced Antibacterial Efficiency.

作者信息

Pokharel Mishal, Neron Abid, Dey Amit Kumar, Siddharthan Aishwarya Raksha, Konara Menaka, Sagar Md Mainuddin, Ferreira Tracie, Park Kihan

机构信息

Department of Biongineering, University of Massachusetts Dartmouth, Dartmouth, MA 02740, USA.

Department of Mechanical Engineering, University of Massachusetts Dartmouth, Dartmouth, MA 02740, USA.

出版信息

Pharmaceutics. 2025 Aug 1;17(8):1007. doi: 10.3390/pharmaceutics17081007.

DOI:10.3390/pharmaceutics17081007
PMID:40871028
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12389631/
Abstract

A precise drug delivery system enables the optimization of treatments with minimal side effects if it can deliver medication only when activated by a specific light source. This study presents a controlled drug delivery system based on poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs) designed for the sustained release of vancomycin hydrochloride. The MPs were co-loaded with indocyanine green (ICG), a near-infrared (NIR) responsive agent, and fabricated via the double emulsion method.They were characterized for stability, surface modification, biocompatibility, and antibacterial efficacy. Dynamic light scattering and zeta potential analyses confirmed significant increases in particle size and surface charge reversal following chitosan coating. Scanning electron microscopy revealed uniform morphology in uncoated MPs (1-10 μm) and irregular surfaces post-coating. Stability tests demonstrated drug retention for up to 180 days. Among formulations, PVI1 exhibited the highest yield (76.67 ± 1.3%) and encapsulation efficiency (56.2 ± 1.95%). NIR irradiation (808 nm) enhanced drug release kinetics, with formulation PVI4 achieving over 48.9% release, resulting in improved antibacterial activity. Chitosan-coated MPs (e.g., PVI4-C) effectively suppressed drug release without NIR light for up to 8 h, with cumulative release reaching only 10.89%. Without NIR light, bacterial colonies exceeded 1000 CFU; NIR-triggered release reduced them below 120 CFU. Drug release data fitted best with the zero-order and Korsmeyer-Peppas models, suggesting a combination of diffusion-controlled and constant-rate release behavior. These results demonstrate the promise of chitosan-coated NIR-responsive PLGA MPs for precise, on-demand antibiotic delivery and improved antibacterial performance.

摘要

如果一种精确的药物递送系统能够仅在特定光源激活时才递送药物,那么它就能以最小的副作用实现治疗的优化。本研究提出了一种基于聚乳酸-乙醇酸共聚物(PLGA)微粒(MPs)的可控药物递送系统,该系统设计用于盐酸万古霉素的持续释放。这些MPs与近红外(NIR)响应剂吲哚菁绿(ICG)共同负载,并通过双乳液法制备。对它们进行了稳定性、表面改性、生物相容性和抗菌功效的表征。动态光散射和zeta电位分析证实,壳聚糖包衣后粒径显著增加且表面电荷反转。扫描电子显微镜显示未包衣的MPs形态均匀(1-10μm),包衣后表面不规则。稳定性测试表明药物保留长达180天。在各种制剂中,PVI1的产率最高(76.67±1.3%),包封效率最高(56.2±1.95%)。近红外照射(808nm)增强了药物释放动力学,制剂PVI4的释放率超过48.9%,从而提高了抗菌活性。壳聚糖包衣的MPs(如PVI4-C)在无近红外光的情况下可有效抑制药物释放长达8小时,累积释放仅达10.89%。在无近红外光的情况下,细菌菌落超过1000 CFU;近红外触发释放将其减少至120 CFU以下。药物释放数据最符合零级和Korsmeyer-Peppas模型,表明存在扩散控制和恒速释放行为的组合。这些结果证明了壳聚糖包衣的近红外响应PLGA MPs在精确、按需抗生素递送和改善抗菌性能方面的前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/b136923505f3/pharmaceutics-17-01007-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/dcab2e96dd11/pharmaceutics-17-01007-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/52fc81cc8da5/pharmaceutics-17-01007-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/739bc8beb64e/pharmaceutics-17-01007-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/ec0c4472eb4e/pharmaceutics-17-01007-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/4036991e0d7b/pharmaceutics-17-01007-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/3f413873c2bc/pharmaceutics-17-01007-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/5857a5b56ece/pharmaceutics-17-01007-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/97577e8b2613/pharmaceutics-17-01007-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/e86290934840/pharmaceutics-17-01007-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/3818ac7e1cb5/pharmaceutics-17-01007-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/bf3923d8833e/pharmaceutics-17-01007-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/c16e5961e4ad/pharmaceutics-17-01007-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/28df853f849f/pharmaceutics-17-01007-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/b136923505f3/pharmaceutics-17-01007-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/dcab2e96dd11/pharmaceutics-17-01007-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/52fc81cc8da5/pharmaceutics-17-01007-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/739bc8beb64e/pharmaceutics-17-01007-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/ec0c4472eb4e/pharmaceutics-17-01007-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/4036991e0d7b/pharmaceutics-17-01007-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/3f413873c2bc/pharmaceutics-17-01007-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/5857a5b56ece/pharmaceutics-17-01007-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/97577e8b2613/pharmaceutics-17-01007-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/e86290934840/pharmaceutics-17-01007-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/3818ac7e1cb5/pharmaceutics-17-01007-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/bf3923d8833e/pharmaceutics-17-01007-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/c16e5961e4ad/pharmaceutics-17-01007-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/28df853f849f/pharmaceutics-17-01007-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5db2/12389631/b136923505f3/pharmaceutics-17-01007-g014.jpg

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