Polyvinylpyrrolidone (PVP) is capable of forming complexes in aqueous solutions with poorly soluble drugs, dramatically increasing their aqueous solubility and formulating stable aqueous solutions. These self-assembled complexes could potentially be explored as an ocular drug delivery system. This study assumes that these PVP medicine complexes can improve ocular permeation and strengthen the drugs' therapeutic effects. PVP K-17PF (17PF) and naringenin (NAR) could formulate into self-assembly nanocomplexes (17PF-NAR). The optimal formulation featured a 17PF/NAR weight ratio 20:1 with a complexation efficiency of 98.51 ± 0.86 percent, a mean diameter 6.73 ± 0.42 nm, and a polydispersity index 0.254 ± 0.019. This 17PF-NAR nanocomplex ophthalmic solution was stable in well storage at both 4° and 25 °C for 12 weeks. The 17PF-NAR nanocomplexes were observed to significantly improve in vitro antioxidant activity and membrane permeation of NAR. The 17PF-NAR nanocomplex ophthalmic solution had good in vitro cellular tolerance and well in vivo tolerated in rabbits. The 17PF-NAR nanocomplexes also demonstrated significant improvement in in vivo intraocular permeation of NAR and in vivo anti-inflammatory efficacy. These results indicated that nanocomplexes based on 17PF have great potential as novel nanoformulations to improve the ocular bioavailability and therapeutic efficacy of poorly water-soluble agents such as NAR.
Keywords: Nanocomplex; Naringenin; Ocular drug delivery; PVP K-17PF.
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