Micelles based on polyvinylpyrrolidone VA64: A potential nanoplatform for the ocular delivery of apocynin

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 & PLUSMN; 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.

Automated summary

The study demonstrates the potential feasibility of APO-VA64 nano-ophthalmic solution as a new treatment for ocular inflammatory diseases. The solution, fabricated via a simple process, exhibits valuable characteristics such as good ocular tolerance and improved drug permeation ability. It shows significant efficacy in treating ocular damage induced by benzalkonium chloride.