Formulation, Optimization, and Evaluation of Ultradeformable Nanovesicles for Effective Topical Delivery of Hydroquinone.

Purpose: The present study aimed to develop, statistically optimize, and characterize hydroquinone-loaded transfersomes (HQ-TFs) for effective topical delivery by mitigating the problems associated with HQ. Methods: HQ-TFs were prepared by the thin-film hydration method and characterized for particle size, zeta potential (ZP), entrapment efficiency (EE), in vitro drug release, and skin penetration potential. The optimized hydroquinone-loaded transfersome (OPT-HQ-TF) was incorporated in a gel and evaluated for ex vivo skin permeation and deposition profile, in vitro antioxidant activity, in vitro cytotoxicity study, in vitro tyrosinase inhibition assay, and dermal skin irritation study. Results: The OPT-HQ-TF showed a particle size of 210 nm, ZP of − 15.10 mV, and EE% of 67.61. The cumulative drug release % from transfersomal formulations ranged from 54.39 ± 1.92 to 76.05 ± 1.18%. The fluorescence microscopy investigation revealed the penetration of transfersomes into deeper skin layers. The skin permeation and deposition studies indicated that the OPT-HQ-TF gel improved permeation and drug retention in the skin compared to the HQ plain gel. The antioxidant assay revealed that HQ retained its antioxidant activity after encapsulation. The cytotoxicity study demonstrated that the OPT-HQ-TF gel significantly decreased the cytotoxicity towards L-929 mouse fibroblast. The tyrosinase inhibition assay specified that the OPT-HQ-TF gel has the potential to treat hyperpigmentation. The dermal skin irritation study indicated that the OPT-HQ-TF gel is safe and non-irritant. Conclusion: The present study findings suggested the potential application of deformable nanovesicles as an innovative topical drug delivery system of HQ in the treatment of hyperpigmentation. [ABSTRACT FROM AUTHOR]