In vitro skin penetration enhancement techniques: A combined approach of ethosomes and microneedles

C. Bellefroid, A. Lechanteur, B. Evrard, D. Mottet, F. Debacq-Chainiaux, G. Piel

Research output: Contribution to journalArticle

Abstract

Dermal administration of different macromolecules, such as nucleic acids, remains a real challenge because of the difficulty of crossing the main skin barrier, the stratum corneum (SC). To overcome this barrier, the use of deformable lipid-based nanovectors were developed to increase topical penetration through the SC and to promote the intercellular delivery of drugs. The purpose of this study is to compare the skin penetration of different liposome formulations according to their composition. In vitro and ex vivo experiments using Franz diffusion cells were performed to highlight the effect of (i) lipid charge, (ii) edge activators (EA) and (iii) ethanol on the diffusion properties of nanovectors. We showed that all formulations were not able to cross the SC. However, on a tape stripped skin, we showed that cationic formulations containing an EA and ethanol improved the skin penetration. The use of microneedles was considered to bypass the SC. We have shown that sodium cholate and ethanol were necessary to ensure an appropriate diffusion of liposomes into the dermis when applied by means of microneedles. This could be a promising approach to further deliver efficiently macromolecules such as genes into the skin.

Original languageEnglish
Article number118793
Pages (from-to)118793
JournalInternational Journal of Pharmaceutics
Volume572
DOIs
Publication statusPublished - 15 Dec 2019

Keywords

  • Deformable liposome
  • Microneedles
  • Nucleic acids
  • Skin delivery
  • Stratum corneum

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