Biodegradable Ingredient-Based Emulgel Loaded with Ketoprofen Nanoparticles

AAPS PharmSciTech. 2018 May;19(4):1869-1881. doi: 10.1208/s12249-018-0997-0. Epub 2018 Apr 12.

Abstract

Biodegradable materials are extensively employed to design nanocarriers that mimic extracellular environment in arthritis. The aim of this study was to formulate and characterize biocompatible, biodegradable ketoprofen-loaded chitosan-chondroitin sulfate (CHS-CS) nanoparticles with natural ingredients for transdermal applications. Polymers used in the design of nanocarriers are biodegradable and produce synergistic anti-inflammatory effect for the treatment of arthritis. For transdermal application, argan oil-based emulgel is utilized to impart viscosity to the formulation. Furthermore, naturally occurring argan oil synergizes anti-inflammatory effect of formulation and promotes skin penetration. CHS and CS form nanoparticles by polyelectrolyte complex formation or complex coacervation at pH 5.0. These particles were loaded into argan oil-based emulgel. Employing this method, nanoparticles were formulated with particle size in the range of 300-500 nm. These nanocarriers entrapped ketoprofen and showed more than 76% encapsulation efficiency and 77% release of the ketoprofen at pH 7.4 within 72 h. Drug releases from CHS-CS nanoparticles by mechanism of simple diffusion. Nanoparticle-loaded argan oil emulgel significantly enhanced skin penetration of ketoprofen as compared to marketed gel (p < 0.05). Nanocarriers prepared successfully delivered drug through transdermal route using natural ingredients. Graphical abstract ᅟ.

Keywords: arthritis; biocompatible; chitosan; chondroitin sulfate; transdermal drug delivery system.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / metabolism
  • Chitosan / administration & dosage
  • Chitosan / chemistry
  • Chitosan / metabolism
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry
  • Drug Carriers / metabolism*
  • Ketoprofen / administration & dosage
  • Ketoprofen / chemistry
  • Ketoprofen / metabolism*
  • Mice
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry
  • Nanoparticles / metabolism*
  • Particle Size
  • Polymers / administration & dosage
  • Polymers / chemistry
  • Polymers / metabolism
  • Skin / drug effects
  • Skin / metabolism*
  • Skin Absorption / drug effects
  • Skin Absorption / physiology

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Polymers
  • chitosan sulfate
  • Chitosan
  • Ketoprofen