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羟丙基-β-环糊精-伏立康唑眼用原位凝胶给药系统:体外评估、稳定性和抗真菌活性。

Hp-β-CD-voriconazole in situ gelling system for ocular drug delivery: in vitro, stability, and antifungal activities assessment.

机构信息

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

出版信息

Biomed Res Int. 2013;2013:341218. doi: 10.1155/2013/341218. Epub 2013 May 9.

DOI:10.1155/2013/341218
PMID:23762839
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3665163/
Abstract

The objective of the present study was to design ophthalmic delivery systems based on polymeric carriers that undergo sol-to-gel transition upon change in temperature or in the presence of cations so as to prolong the effect of HP- β -CD Voriconazole (VCZ) in situ gelling formulations. The in situ gelling formulations of Voriconazole were prepared by using pluronic F-127 (PF-127) or with combination of pluronic F-68 (PF-68) and sodium alginate by cold method technique. The prepared formulations were evaluated for their physical appearance, drug content, gelation temperature (T gel), in vitro permeation studies, rheological properties, mucoadhesion studies, antifungal studies, and stability studies. All batches of in situ formulations had satisfactory pH ranging from 6.8 to 7.4, drug content between 95% and 100%, showing uniform distribution of drug. As the concentration of each polymeric component was increased, that is, PF-68 and sodium alginate, there was a decrease in T gel with increase in viscosity and mucoadhesive strength. The in vitro drug release decreased with increase in polymeric concentrations. The stability data concluded that all formulations showed the low degradation and maximum shelf life of 2 years. The antifungal efficiency of the selected formulation against Candida albicans and Asperigillus fumigatus confirmed that designed formulation has prolonged effect and retained its properties against fungal infection.

摘要

本研究的目的是设计基于聚合物载体的眼科递药系统,该载体在温度变化或存在阳离子时发生溶胶-凝胶转变,从而延长 HP-β-CD 伏立康唑(VCZ)原位凝胶制剂的作用。通过冷法技术,使用泊洛沙姆 F-127(PF-127)或泊洛沙姆 F-68(PF-68)与海藻酸钠联合制备伏立康唑原位凝胶制剂。对所制备的制剂进行物理外观、药物含量、胶凝温度(T gel)、体外渗透研究、流变学性质、黏膜粘附研究、抗真菌研究和稳定性研究。所有原位制剂批次的 pH 值均在 6.8 到 7.4 之间,药物含量在 95%到 100%之间,显示出药物的均匀分布。随着每种聚合物成分的浓度增加,即 PF-68 和海藻酸钠,T gel 随着粘度和黏膜粘附强度的增加而降低。体外药物释放随着聚合物浓度的增加而减少。稳定性数据表明,所有制剂均表现出低降解和最长 2 年的保质期。所选制剂对白色念珠菌和烟曲霉的抗真菌效率证实,所设计的制剂具有延长的作用,并保留了其对抗真菌感染的特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1f2/3665163/6452b67d5cd4/BMRI2013-341218.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1f2/3665163/39c7fc5dbe75/BMRI2013-341218.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1f2/3665163/3e6f7c3c4c24/BMRI2013-341218.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1f2/3665163/af50c3955a8b/BMRI2013-341218.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1f2/3665163/6452b67d5cd4/BMRI2013-341218.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1f2/3665163/39c7fc5dbe75/BMRI2013-341218.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1f2/3665163/3e6f7c3c4c24/BMRI2013-341218.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1f2/3665163/af50c3955a8b/BMRI2013-341218.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1f2/3665163/6452b67d5cd4/BMRI2013-341218.004.jpg

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