Electrostatically optimized adapalene-loaded emulsion for the treatment of acne vulgaris

Yun Bae Ji; Hye Yun Lee; Soyeon Lee; Young Hun Kim; Kun Na; Jae Ho Kim; Sangdun Choi; Moon Suk Kim

doi:10.1016/j.mtbio.2022.100339

Electrostatically optimized adapalene-loaded emulsion for the treatment of acne vulgaris

Mater Today Bio. 2022 Jun 24:16:100339. doi: 10.1016/j.mtbio.2022.100339. eCollection 2022 Dec.

Authors

Yun Bae Ji¹, Hye Yun Lee¹, Soyeon Lee¹, Young Hun Kim¹, Kun Na², Jae Ho Kim¹, Sangdun Choi¹, Moon Suk Kim^{1

3}

Affiliations

¹ Department of Molecular Science and Technology, Ajou University, Suwon, 443-749, South Korea.
² Department of Biotechnology, The Catholic University of Korea, Bucheon, 420-743, South Korea.
³ Research Institute, Medipolymers, Suwon, 16522, South Korea.

Abstract

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-b-poly(ε-caprolactone) (MC) as an anionic emulsifier coupled with a newly synthesized MC with different contents of an amine pendant-group (MC-[NH₂]_x) as a cationic emulsifier. The AD emulsion prepared using MC-[NH₂]_x 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-[NH₂]_x 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-[NH₂]_x emulsifier provides a promising therapeutic strategy for acne vulgaris.

Keywords: Acne vulgaris; Adapalene; Electrostatic emulsifier; Electrostatic interaction; Emulsion.