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 ± 1.24 nm), narrow micelle size distribution, and high APO encapsulation efficiency.

Highlights

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.

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.

Read the article here

Article information: Yaru Li, Lei Zhou, Mengmeng Zhang, Runzhi Li, Guohu Di, Hongyun Liu, Xianggen Wu, Micelles based on polyvinylpyrrolidone VA64: A potential nanoplatform for the ocular delivery of apocynin, International Journal of Pharmaceutics, Volume 615, 2022. https://doi.org/10.1016/j.ijpharm.2022.121451.