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多元醇修饰的可变形脂质体强化隐形眼镜以提高眼部通透性。

Polyol-modified deformable liposomes fortified contact lenses for improved ocular permeability.

作者信息

Dave Jeel, Jani Harshilkumar, Patel Yashkumar, Mohite Popat, Puri Abhijeet, Chidrawar Vijay R, Datta Deepanjan, Bandi Sony Priyanka, Ranch Ketan, Singh Sudarshan

机构信息

Department of Pharmaceutics and Pharmaceutical Technology, L. M. College of Pharmacy, Ahmedabad, India.

Research Scholar, Gujarat Technological University, Chandkheda, Ahmedabad, India.

出版信息

Nanomedicine (Lond). 2025 Apr;20(7):649-662. doi: 10.1080/17435889.2025.2463867. Epub 2025 Feb 18.

DOI:10.1080/17435889.2025.2463867
PMID:39963803
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11970793/
Abstract

AIM

To develop a glycerol modified liposomes to effectively deliver active agents into posterior segment of the eye for the management of posterior uveitis.

MATERIALS AND METHODS

The modified liposome enhanced with glycerol as an edge activator was fabricated using a 3 experimental design with independent variables being soya lecithin (mg) (X) and glycerol (%) (X) and vesicle size (nm) (Y), deformability index (%) (Y), and entrapment efficiency (%) (Y) as dependent variable with improve permeability and entrapment efficacy. These modified liposomes were then integrated into pHEMA-based contact lenses via free radical polymerization using different monomer mixture, co-polymer, crosslinker, and photo-initiator to extend drug release.

RESULTS AND CONCLUSIONS

Nano-vesicles resulted in size and deformability index of 200.5 ± 15 nm and 11.58, respectively, with entrapment efficiency of 80.98% of the drug. Moreover, the optimized lenses demonstrated 71%) of swelling and transmittance of 87%). In addition, release of active component from the therapeutic contact lens demonstrated sustained drug release over 24 h. Whereas studies displayed a 5-fold increase in drug permeation, compared to tested conventional eye drops. The results suggested that glycerosomes-loaded contact lens can be a promising alternative for regulated delivery of dexamethasone sodium phosphate in the management of posterior uveitis.

摘要

目的

研发一种甘油修饰的脂质体,以有效地将活性剂递送至眼后段,用于治疗后葡萄膜炎。

材料与方法

以甘油作为边缘活化剂增强的修饰脂质体,采用三因素实验设计制备,自变量为大豆卵磷脂(毫克)(X1)和甘油(%)(X2),因变量为囊泡大小(纳米)(Y1)、变形性指数(%)(Y2)和包封率(%)(Y3),以提高渗透性和包封效果。然后,通过自由基聚合,使用不同的单体混合物、共聚物、交联剂和光引发剂,将这些修饰脂质体整合到基于聚甲基丙烯酸羟乙酯的隐形眼镜中,以延长药物释放。

结果与结论

纳米囊泡的大小和变形性指数分别为200.5±15纳米和11.58,药物包封率为80.98%。此外,优化后的隐形眼镜显示出71%的溶胀率和87%的透光率。另外,治疗性隐形眼镜中活性成分的释放显示药物在24小时内持续释放。与测试的传统眼药水相比,研究显示药物渗透增加了5倍。结果表明,载有甘油脂质体的隐形眼镜有望成为在治疗后葡萄膜炎时调节地塞米松磷酸钠递送的一种替代方法。

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