增强生物大分子皮肤渗透性的新型药物策略

Zhang Luyu, Dong Zirong, Liu Wenjuan, Wu Xiying, He Haisheng, Lu Yi, Wu Wei, Qi Jianping

Key Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, China.

Pharmaceuticals (Basel). 2022 Jul 16;15(7):877. doi: 10.3390/ph15070877.

Skin delivery of biomacromolecules holds great advantages in the systemic and local treatment of multiple diseases. However, the densely packed stratum corneum and the tight junctions between keratinocytes stand as formidable skin barriers against the penetration of most drug molecules. The large molecular weight, high hydrophilicity, and lability nature of biomacromolecules pose further challenges to their skin penetration. Recently, novel penetration enhancers, nano vesicles, and microneedles have emerged as efficient strategies to deliver biomacromolecules deep into the skin to exert their therapeutic action. This paper reviews the potential application and mechanisms of novel skin delivery strategies with emphasis on the pharmaceutical formulations.

生物大分子的经皮给药在多种疾病的全身和局部治疗中具有巨大优势。然而，紧密排列的角质层和角质形成细胞之间的紧密连接是大多数药物分子穿透皮肤的巨大屏障。生物大分子的大分子量、高亲水性和易降解性对其皮肤穿透构成了进一步挑战。近年来，新型渗透促进剂、纳米囊泡和微针已成为将生物大分子深入递送至皮肤以发挥其治疗作用的有效策略。本文综述了新型皮肤给药策略的潜在应用和机制，重点关注药物制剂。