Decylglucoside-based microemulsions for cutaneous localization of lycopene and ascorbic acid

Int J Pharm. 2012 Sep 15;434(1-2):420-8. doi: 10.1016/j.ijpharm.2012.06.016. Epub 2012 Jun 9.

Abstract

Cutaneous delivery of combinations of antioxidants offers the possibility of enhanced protection against UV-radiation. In this study, we investigated the potential of sugar-based microemulsions containing monoglycerides to promote simultaneous cutaneous delivery of lycopene and ascorbic acid, and increase tissue antioxidant activity. Lycopene and ascorbic acid were incorporated (0.04% and 0.2% (w/w), respectively) in decylglucoside-based microemulsions containing isopropyl myristate mixed with monocaprylin (ME-MC), monolaurin (ME-ML) or monoolein (ME-MO) as oil phase. The microemulsions increased lycopene delivery into porcine ear skin by 3.3- to 8-fold compared to a drug solution. The effect of microemulsions on ascorbic acid cutaneous delivery was more modest (1.5-3-fold), and associated with an approximately 2-fold increase in transdermal delivery. According to their penetration-enhancing ability, the microemulsions were ranked ME-MC>ME-MO>ME-ML. This superiority of ME-MC coincided with a stronger effect in decreasing skin electrical resistance. After 18 h of treatment, the viability of bioengineered skin treated with ME-MC was 2.2-times higher compared to Triton-X100 (moderate irritant), demonstrating that ME-MC is less cytotoxic. Skin treatment with ME-MC containing both antioxidants increased the tissue antioxidant activity by 10.2-fold, but no synergism between the antioxidants was observed.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Antioxidants / administration & dosage*
  • Antioxidants / pharmacokinetics
  • Antioxidants / pharmacology
  • Ascorbic Acid / administration & dosage*
  • Ascorbic Acid / pharmacokinetics
  • Ascorbic Acid / pharmacology
  • Caprylates / chemistry
  • Carotenoids / administration & dosage*
  • Carotenoids / pharmacokinetics
  • Carotenoids / pharmacology
  • Drug Delivery Systems*
  • Emulsions
  • Excipients / chemistry
  • Glucosides / chemistry
  • Glycerides / chemistry
  • Laurates / chemistry
  • Lycopene
  • Monoglycerides / chemistry
  • Myristates / chemistry
  • Skin / metabolism
  • Skin Absorption
  • Swine

Substances

  • Antioxidants
  • Caprylates
  • Emulsions
  • Excipients
  • Glucosides
  • Glycerides
  • Laurates
  • Monoglycerides
  • Myristates
  • isopropyl myristate
  • monolaurin
  • Carotenoids
  • monoolein
  • Ascorbic Acid
  • Lycopene
  • monooctanoin