Combination and efficiency: preparation of dissolving microneedles array loaded with two active ingredients and its anti-pigmentation effects on guinea pigs

• Published in: European journal of pharmaceutical sciences Vol. 160; p. 105749
• Main Authors: Wang, Yu-shuai, Yang, Wei-han, Gao, Wei, Zhang, Lu, Wei, Fang, Liu, Hang, Wang, Shu-ya, Li, Ying-ying, Zhao, Wei-man, Ma, Tao, Wang, Qingqing
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.05.2021
• Subjects: Anti-pigmentation; Arbutin; Dissolving microneedles array; Synergistic effect; Vitamin C; Dissolving microneedles array; Synergistic effect; Arbutin; Anti-pigmentation; Vitamin C
• ISSN: 0928-0987; 1879-0720
• DOI: 10.1016/j.ejps.2021.105749

Hyperpigmentation is a common skin disorder caused by excessive melanogenesis and uneven dispersion of melanin in the skin. To combine multiple active agents with an efficient transdermal drug delivery system is an effective strategy to combat UV induced skin pigmentation. In this work, Arbutin (Arb) and Vitamin C (Vc) mixed in 1:1 were found to have the greatest inhibition effects on melanogenesis and tyrosinase activity in B16 murine melanoma cells. And hyaluronic acid (HA) based dissolving microneedles array (DMNA) was employed to overcome the skin barriers for improved topical drug delivery, which exhibited the most desirable features, including morphology, mechanical properties, dissolving ability, and the highest drug loading. Furthermore, DMNA could greatly increase the stability of Vc during storage without adding any antioxidant which is an important issue for Vc administration. Pharmacodynamics study showed that DMNA loaded with Arb and Vc could synergistically suppress UVB-induced hyperpigmentation in guinea pig skin. This work provides a promising treatment strategy and solution for skin pigmentation and other skin problems. [Display omitted]