Topical gel based nanoparticles for the controlled release of oleanolic acid: design and in vivo characterization of a cubic liquid crystalline anti-inflammatory drug

BMC Complement Med Ther. 2021 Sep 4;21(1):224. doi: 10.1186/s12906-021-03399-8.

Abstract

Background: Oleanolic acid (OA) has multiple pharmaceutical applications including anti-inflammatory activity, but low permeability of the molecule limits its widespread use.

Methods: A cubic liquid crystalline nanoparticle (LCNP)-based gel was prepared as a potential topical delivery system for OA. The LCNP-based gel was optimized using rheological, drug release kinetic, and ex vivo permeation studies.

Results: The studies showed that the OA was trapped in the interior of the LCNP with a crystal form of Pn3m space. The optimized LCNP formulation performed well using in vitro release studies for up to 12 h (85.49 ± 0.21%). Ex vivo permeation studies showed that the LCNP-based gel formulation was superior to a standard gel formulation. The r2 value from the Peppas equation indicated good linearity, but showed irregular (non-Fickian) diffusion, suggesting that drug release was controlled by multiple processes.

Conclusions: In this study, OA-loaded LCNPs were prepared by the precursor method, resulting in a well-characterized OA-LCNP gel preparation. The gel was shown to be effective in a rodent carrageenan-induced hind paw inflammation model with sustained efficacy after a single application.

Keywords: Anti-inflammatory; LCNP-based gel; Oleanolic acid; Permeation studies.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Delayed-Action Preparations
  • Gels / pharmacology*
  • Inflammation / drug therapy*
  • Liquid Crystals / chemistry
  • Oleanolic Acid / pharmacology*
  • Plant Extracts / pharmacology*
  • Rats
  • Rats, Wistar
  • Skin Absorption / drug effects*

Substances

  • Anti-Inflammatory Agents
  • Delayed-Action Preparations
  • Gels
  • Plant Extracts
  • Oleanolic Acid