Ji Yun Bae, Lee Hye Yun, Lee Soyeon, Kim Young Hun, Na Kun, Kim Jae Ho, Choi Sangdun, Kim Moon Suk
Department of Molecular Science and Technology, Ajou University, Suwon, 443-749, South Korea.
Department of Biotechnology, The Catholic University of Korea, Bucheon, 420-743, South Korea.
Mater Today Bio. 2022 Jun 24;16:100339. doi: 10.1016/j.mtbio.2022.100339. eCollection 2022 Dec.
Adapalene (AD) is an FDA-approved drug that shows good therapeutic efficacy for the treatment of acne vulgaris. However, due to its negative charge, AD cannot efficiently penetrate across the also negatively-charged skin membrane. This study is the first to assess the treatment of acne vulgaris using electrostatically optimized AD emulsions prepared using anionic AD with methoxy polyethylene glycol--poly(ε-caprolactone) (MC) as an anionic emulsifier coupled with a newly synthesized MC with different contents of an amine pendant-group (MC-[NH]) as a cationic emulsifier. The AD emulsion prepared using MC-[NH] with high cationic charge potential was significantly stable in the short-term studies compared with anionic MC or no emulsifier. Furthermore, the AD emulsion prepared with the cationic MC-[NH] emulsifier provided a two or three times stronger therapeutic effect against acne vulgaris than the AD emulsion prepared with the anionic MC emulsifier or no emulsifier in an animal study. Additionally, the AD emulsion with high cationic charge potential exerted a remarkable inhibition of macrophage expression, as confirmed by histological analysis. Therefore, the electrostatic interaction between the negatively-charged skin membrane and the AD emulsion prepared with the cationic MC-[NH] emulsifier provides a promising therapeutic strategy for acne vulgaris.
阿达帕林（AD）是一种经美国食品药品监督管理局（FDA）批准的药物，对寻常痤疮的治疗显示出良好的疗效。然而，由于其带负电荷，AD不能有效地穿透同样带负电荷的皮肤膜。本研究首次评估了使用静电优化的AD乳液治疗寻常痤疮，该乳液是用阴离子型AD与甲氧基聚乙二醇-聚（ε-己内酯）（MC）作为阴离子乳化剂，再结合新合成的带有不同胺侧基含量的MC（MC-[NH]）作为阳离子乳化剂制备而成。在短期研究中，与阴离子型MC或无乳化剂相比，使用具有高阳离子电荷电位的MC-[NH]制备的AD乳液具有显著的稳定性。此外，在一项动物研究中，用阳离子型MC-[NH]乳化剂制备的AD乳液对寻常痤疮的治疗效果比用阴离子型MC乳化剂或无乳化剂制备的AD乳液强两到三倍。另外，组织学分析证实，具有高阳离子电荷电位的AD乳液对巨噬细胞表达有显著抑制作用。因此，带负电荷的皮肤膜与用阳离子型MC-[NH]乳化剂制备的AD乳液之间的静电相互作用为寻常痤疮提供了一种有前景的治疗策略。
