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.

中文翻译：

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用于有效局部递送氢醌的超变形纳米囊泡的配方、优化和评估

目的

本研究旨在通过减轻与 HQ 相关的问题来开发、统计优化和表征负载氢醌的传递体 (HQ-TF)，以实现有效的局部给药。

方法

HQ-TFs 采用薄膜水化法制备，并对其粒径、zeta 电位 (ZP)、包封率 (EE)、体外药物释放和皮肤渗透电位进行了表征。将优化的氢醌负载转移体 (OPT-HQ-TF) 掺入凝胶中并评估离体皮肤渗透和沉积曲线、体外抗氧化活性、体外细胞毒性研究、体外酪氨酸酶抑制测定和皮肤皮肤刺激研究.

结果

OPT-HQ-TF 的粒径为 210 nm，ZP 为 - 15.10 mV，EE% 为 67.61。转移体制剂的累积药物释放百分比范围为 54.39 ± 1.92 至 76.05 ± 1.18%。荧光显微镜研究揭示了转移体渗透到更深的皮肤层中。皮肤渗透和沉积研究表明，与 HQ 普通凝胶相比，OPT-HQ-TF 凝胶改善了皮肤中的渗透和药物保留。抗氧化试验表明，HQ 在封装后保留了其抗氧化活性。细胞毒性研究表明，OPT-HQ-TF 凝胶显着降低了对 L-929 小鼠成纤维细胞的细胞毒性。酪氨酸酶抑制试验表明 OPT-HQ-TF 凝胶具有治疗色素沉着过度的潜力。

结论

本研究结果表明可变形纳米囊泡作为 HQ 的创新局部药物递送系统在治疗色素沉着过度方面的潜在应用。