化学
胶束
聚乙烯吡咯烷酮
药物输送
药理学
体内
体外
泊洛沙姆
核化学
纳米载体
毒品携带者
纳米颗粒
作者
Yaru Li,Lei Zhou,Mengmeng Zhang,Runzhi Li,Guohu Di,Hongyun Liu,Xianggen Wu
标识
DOI:10.1016/j.ijpharm.2022.121451
摘要
• • VA64 micelles was the first time to be formulated into ophthalmic preparation. • • APO-VA64 showed soaring increasement in APO aqueous solubility. • • This ophthalmic solution exhibited good ocular tolerance. • • This ophthalmic solution demonstrated strengthened in vivo treatment efficacies. • • The inhibition of HMGB1 signaling was involved in therapeutic effect. Purpose of this work was to determine the feasibility of a nano-ophthalmic solution consisting of the nanocarrier polyvinylpyrrolidone VA64 (VA64) and encapsulated apocynin (APO) as treatment for ocular inflammatory diseases. Results showed the solution, termed APO-VA64 ophthalmic solution, could be fabricated via a simple process. This solution was clear, colorless, and possessed valuable characteristics, such as small micelle size (14.12 ± 1.24 nm), narrow micelle size distribution, and high APO encapsulation efficiency. Encapsulated APO was also found to have high aqueous solubility and in vitro release and antioxidant activities. APO-VA64 ophthalmic solution showed good ocular tolerance and demonstrated improved corneal permeation ability in mouse eyes. In an in vivo mice model, topically administered APO-VA64 ophthalmic solution was found to be significantly more effective against benzalkonium chloride-induced ocular damage than APO, VA64, and a mix of APO and VA64. Blockage of high mobility group box 1 signaling and its related proinflammatory cytokines were involved in this therapeutic effect. In conclusion, these in vitro and in vivo findings demonstrate that VA64 micelles are a potential nanoplatform for ocular drug delivery, and that the nanoformulation APO-VA64 ophthalmic solution may be a promising candidate for the efficacious treatment of ocular inflammatory diseases.
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