3-Acetyl-11-keto-beta-boswellic acid loaded-polymeric nanomicelles for topical anti-inflammatory and anti-arthritic activity

J Pharm Pharmacol. 2010 Feb;62(2):273-8. doi: 10.1211/jpp.62.02.0016.

Abstract

Objectives: The aim of this study was to develop 3-acetyl-11-keto-beta-boswellic acid (AKBA)-loaded polymeric nanomicelles for topical anti-inflammatory and anti-arthritic activity.

Methods: Polymeric nanomicelles of AKBA were developed by a radical polymerization method using N-isopropylacrylamide, vinylpyrrolidone and acrylic acid. The polymeric nanomicelles obtained were characterized by Fourier transform infrared (FTIR), transmission electron microscopy (TEM) and dynamic light scattering (DLS). In-vitro and in-vivo evaluations of AKBA polymeric nanomicelles gel were carried out for enhanced skin permeability and anti-inflammatory and anti-arthritic activity.

Key findings: TEM and DLS results demonstrated that polymeric nanomicelles were spherical with a mean diameter approximately 45 nm. FTIR data indicated a weak interaction between polymer and AKBA in the encapsulated system. The release of drug in aqueous buffer (pH 7.4) from the polymeric nanomicelles was 23 and 55% after 2 and 8 h, respectively, indicating sustained release. In-vitro skin permeation studies through excised abdominal skin indicated a threefold increase in skin permeability compared with AKBA gel containing the same amount of AKBA as the AKBA polymeric nanomicelles gel. The AKBA polymeric nanomicelle gel showed significantly enhanced anti-inflammatory and anti-arthritic activity compared with the AKBA gel.

Conclusions: This study suggested that AKBA polymeric nanomicelle gel significantly enhanced skin permeability, and anti-inflammatory and anti-arthritic activity.

MeSH terms

  • Administration, Topical
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / adverse effects
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use*
  • Arthritis, Experimental / drug therapy*
  • Edema / drug therapy
  • Gels
  • In Vitro Techniques
  • Light
  • Male
  • Mice
  • Micelles
  • Microscopy, Electron, Transmission
  • Nanoparticles / chemistry*
  • Particle Size
  • Rats
  • Rats, Wistar
  • Scattering, Radiation
  • Skin / drug effects*
  • Skin / metabolism
  • Skin Absorption / drug effects*
  • Skin Irritancy Tests
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Surface Properties
  • Triterpenes / administration & dosage
  • Triterpenes / adverse effects
  • Triterpenes / chemistry
  • Triterpenes / pharmacokinetics
  • Triterpenes / therapeutic use*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Gels
  • Micelles
  • Triterpenes
  • acetyl-11-ketoboswellic acid