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用于眼科应用的莫西沙星负载型聚乳酸-羟基乙酸共聚物纳米混悬液的制备及体外/离体评价

Preparation and In Vitro/Ex Vivo Evaluation of Moxifloxacin-Loaded PLGA Nanosuspensions for Ophthalmic Application.

作者信息

Mudgil Meetali, Pawar Pravin K

机构信息

Chitkara College of Pharmacy, Chitkara University, Chandigarh-Patiala Highway, Rajpura, Patiala, Punjab, 140401, India.

出版信息

Sci Pharm. 2013 Apr-Jun;81(2):591-606. doi: 10.3797/scipharm.1204-16. Epub 2013 Feb 4.

DOI:10.3797/scipharm.1204-16
PMID:23833723
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3700085/
Abstract

The aim of the present investigation was to prepare a colloidal ophthalmic formulation to improve the residence time of moxifloxacin. Moxifloxacin-loaded poly(dl-lactide-co-glycolide) (PLGA) nanosuspensions were prepared by using the solvent evaporation technique. The nanosuspensions were characterised physically by using different techniques like particle size, zeta potential, FTIR, DSC, and XRD analysis. In vitro and ex vivo studies of nanosuspensions were carried out using a modified USP dissolution apparatus and all-glass Franz diffusion cells, respectively. The antibacterial activities of the nanosuspension and marketed formulations were performed against S. aureus and P. aeroginosa. The moxifloxacin-loaded PLGA nanosuspensions showed uniform particle size, ranging between 164-490 nm with negative zeta potential for all batches. The percentage entrapment efficiency of the drug-loaded nano-suspension was found to be between 84.09 to 92.05%. In vitro drug release studies suggest that all of the formulations showed extended drug release profiles and follow Korsemeyer-Peppas release kinetics. In vitro corneal permeability was found to be comparable with that of the marketed formulation across isolated goat cornea, indicating the suitability of the nanosuspension formulation in the ophthalmic delivery of moxifloxacin. The optimised nano-suspension was found to be more active against S. aureus and P. aeruginosa compared to the marketed eye drops.

摘要

本研究的目的是制备一种胶体眼科制剂，以提高莫西沙星的驻留时间。采用溶剂蒸发技术制备了载莫西沙星的聚（dl-丙交酯-共-乙交酯）（PLGA）纳米混悬液。通过使用不同的技术，如粒径、zeta电位、傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和X射线衍射（XRD）分析，对纳米混悬液进行了物理表征。分别使用改良的美国药典溶出装置和全玻璃Franz扩散池对纳米混悬液进行了体外和离体研究。对纳米混悬液和市售制剂针对金黄色葡萄球菌和铜绿假单胞菌进行了抗菌活性测试。载莫西沙星的PLGA纳米混悬液显示出均匀的粒径，所有批次的粒径在164-490nm之间，zeta电位为负。载药纳米混悬液的包封率在84.09%至92.05%之间。体外药物释放研究表明，所有制剂均显示出延长的药物释放曲线，并符合Korsemeyer-Peppas释放动力学。在离体山羊角膜上，发现纳米混悬液的体外角膜渗透率与市售制剂相当，表明纳米混悬液制剂适用于莫西沙星的眼部给药。与市售眼药水相比，优化后的纳米混悬液对金黄色葡萄球菌和铜绿假单胞菌更具活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/9f2448e66afa/scipharm-2013-81-591f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/df3b291a8f03/scipharm-2013-81-591f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/a51671dcd307/scipharm-2013-81-591f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/acbc10179eef/scipharm-2013-81-591f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/b988ba17da3c/scipharm-2013-81-591f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/528e3744e1e3/scipharm-2013-81-591f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/9f2448e66afa/scipharm-2013-81-591f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/df3b291a8f03/scipharm-2013-81-591f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/a51671dcd307/scipharm-2013-81-591f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/acbc10179eef/scipharm-2013-81-591f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/b988ba17da3c/scipharm-2013-81-591f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/528e3744e1e3/scipharm-2013-81-591f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/316f/3700085/9f2448e66afa/scipharm-2013-81-591f6.jpg

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