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一种潜在的载药纳米粒原位凝胶,用于增强和持续眼部递送达氟沙星。

A potential nanoparticle-loaded in situ gel for enhanced and sustained ophthalmic delivery of dexamethasone.

机构信息

Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China. Guangdong Provincial Engineering Center of Topical Precise Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China. R&D Team for Formulation Innovation, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.

出版信息

Nanotechnology. 2018 Oct 19;29(42):425101. doi: 10.1088/1361-6528/aad7da. Epub 2018 Aug 3.

Abstract

Increasing the permeability of drugs across the cornea is key to improving drug absorption by the eye. This study presents a newly developed in situ gel loaded with nanoparticles, which could achieve controlled drug release and high ocular drug bioavailability by avoiding rapid precorneal clearance. The physicochemical parameters of the formulation were investigated and showed uniform size, physical stability, and favorable rheological and gelling properties. Ex vivo permeation studies revealed significantly higher drug release from the in situ gel loaded with nanoparticles compared to the conventional poloxamer in situ gel and the drug solution. When compared with a marketed formulation, the in situ gel loaded with nanoparticles provided slower controlled release and higher ocular bioavailability of dexamethasone. In conclusion, the developed nanoparticle-loaded in situ gel can successfully increase drug ocular bioavailability by enhancing contact time with the ocular surface and permeation through the cornea.

摘要

提高药物穿过角膜的通透性是提高眼部药物吸收的关键。本研究提出了一种新开发的载纳米粒原位凝胶,通过避免快速的角膜前清除,可以实现药物的控制释放和高眼部药物生物利用度。对制剂的理化参数进行了考察,结果表明其具有均匀的粒径、物理稳定性以及良好的流变学和胶凝性能。离体渗透研究表明,载纳米粒的原位凝胶与常规泊洛沙姆原位凝胶和药物溶液相比,药物释放明显增加。与市售制剂相比,载纳米粒的原位凝胶提供了更慢的控制释放和更高的地塞米松眼部生物利用度。总之,开发的载纳米粒原位凝胶可以通过增加与眼表面的接触时间和穿透角膜来成功提高药物的眼部生物利用度。

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