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

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Abstract

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.

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Acknowledgements

The authors acknowledge the kind support of Lipoid GmBH, Ludwigshafen, Germany, for providing the gift sample Phospholipon® 90 G.

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Authors and Affiliations

  1. Department of Pharmaceutics, Maratha Mandal’s College of Pharmacy, Belagavi, Karnataka, 590010, India

    Arzoo Toyeba Jamadar, Malleswara Rao Peram, Nagesh Chandrasekhar & Ankita Kanshide

  2. Central Research Laboratory, Maratha Mandal’s NGH Institute of Dental Sciences and Research Centre, Belagavi, Karnataka, 590010, India

    Malleswara Rao Peram, Vijay M. Kumbar & Prakash V. Diwan

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  1. Arzoo Toyeba Jamadar
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Correspondence to Malleswara Rao Peram.

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Jamadar, A.T., Peram, M.R., Chandrasekhar, N. et al. Formulation, Optimization, and Evaluation of Ultradeformable Nanovesicles for Effective Topical Delivery of Hydroquinone. J Pharm Innov 18, 506–524 (2023). https://doi.org/10.1007/s12247-022-09657-7

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