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

Zhiqi Shi,Luolin Wang,Sha Li,Shugang Pan

doi:10.1186/s12906-021-03399-8

Abstract

BackgroundOleanolic acid (OA) has multiple pharmaceutical applications including anti-inflammatory activity, but low permeability of the molecule limits its widespread use.MethodsA 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.ResultsThe 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.ConclusionsIn 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.

Highlights

Many plants in nature have been proven to have a variety of pharmacological activities, prompting scientists to find ingredients with specific activities in them for better treatment of various diseases
The results showed that the oral bioavailability of liquid crystal nanoparticles (LCNP)-curcumin was significantly improved [26]
Based on our previous work and referenced evidence, in this study we explored the possibility of LCNP as a carrier system for a topical formulation of Oleanolic acid (OA)

Summary

Introduction

Many plants in nature have been proven to have a variety of pharmacological activities, prompting scientists to find ingredients with specific activities in them for better treatment of various diseases. Many triterpenoids including OA have been shown to have a wide range of pharmacological activities [1] including being an antioxidant, hypoglycemic, anti-inflammatory, antibacterial, and. Cubic liquid crystal nanoparticles (LCNP) are being investigated as a universal carrier for drug delivery [20,21,22,23,24] to improve the oral bioavailability of the drug because of high encapsulation efficiency, drug loading and bio-affinity [25]. We prepared curcumin and piperine-loaded LCNP using a precursor injection method. The results showed that the oral bioavailability of LCNP-curcumin was significantly improved [26]. Oleanolic acid (OA) has multiple pharmaceutical applications including anti-inflammatory activity, but low permeability of the molecule limits its widespread use

Methods

Results

Conclusion