A synergistic approach of adapalene-loaded nanostructured lipid carriers, and vitamin C co-administration for treating acne

Drug Dev Ind Pharm. 2016;42(6):897-905. doi: 10.3109/03639045.2015.1104343. Epub 2015 Nov 17.

Abstract

The present study documents the fabrication and characterization of a topically applicable gel loaded with nanostructured lipid carriers (NLCs) of adapalene (ADA) and vitamin C (ascorbyl-6-palmitate [AP]). The NLCs were prepared by high pressure homogenization (HPH) method followed by incorporation into AP loaded gel. The fabricated system was characterized for size, poly dispersity index, entrapment efficiency (EE) and in vitro drug release properties, and was further investigated for skin compliance, skin transport characteristics (skin permeation and bio-distribution), rheological behavior, texture profile analysis and anti-acne therapeutic potential against testosterone-induced acne in male Wistar rats. The NLC-based formulation improved targeting of the skin epidermal layer and reducing systemic penetration. The co-administration of vitamin C led to an adjunct effect in acne therapy in physiological conditions. In brief, the present results suggest the potential of NLCs as a novel carrier for the dermal delivery of ADA and also the synergistic effect of vitamin C in topical therapeutics.

Keywords: Acne vulgarise; adapalene; ascorbyl-6-palmitate; nanostructured lipid carriers (NLCs); rheology; topical delivery; vitamin C.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acne Vulgaris / drug therapy*
  • Adapalene / administration & dosage*
  • Adapalene / chemistry
  • Administration, Cutaneous
  • Animals
  • Ascorbic Acid / administration & dosage*
  • Ascorbic Acid / chemistry
  • Chemistry, Pharmaceutical / methods
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Drug Synergism
  • Gels / administration & dosage
  • Gels / chemistry
  • Lipids / chemistry*
  • Male
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry
  • Nanostructures / administration & dosage*
  • Nanostructures / chemistry
  • Particle Size
  • Rats
  • Rats, Wistar
  • Skin / drug effects
  • Skin Absorption

Substances

  • Drug Carriers
  • Gels
  • Lipids
  • Adapalene
  • Ascorbic Acid