Comparison of penetration-enhancing ability of laurocapram, N-methyl-2-pyrrolidone and dodecyl-L-pyroglutamate

Pharm Weekbl Sci. 1988 Oct 14;10(5):189-92. doi: 10.1007/BF01956869.

Abstract

The study reports on penetration enhancers used to improve drug absorption through the skin. All experiments were carried out in permeation cells in vitro. Insulin (2.5 mg/ml) and Brilliant Blue (50.0 mg/ml) served as model drugs. They were formulated into a 40% solution of propylene glycol with increasing concentrations of N-methyl-2-pyrrolidone (NMP) (0.0 to 20.0%), dodecylazacycloheptan-2-one (laurocapram) and a new compound dodecyl-L-pyroglutamate (DLP; 0.0 to 0.5%). The maximum amount of insulin permeated within 24 h was almost 200 microU/ml in the case of 0.1% laurocapram, while in the case of 0.1% DLP it was approximately half of that. The optimum concentration of NMP was 12.0%. Experiments performed with Brilliant Blue showed no significant difference among formulations containing either 6.0, 12.0 or 20.0% of NMP. When NMP was omitted, flux, permeability as well as the maximum concentration estimated after 26 h reached 50% of the values obtained with NMP. The lag time was twice as long in this case in comparison with the formulations containing NMP.

Publication types

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

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Azepines / pharmacology*
  • Benzenesulfonates
  • Coloring Agents
  • In Vitro Techniques
  • Insulin / administration & dosage
  • Insulin / pharmacokinetics*
  • Pyrrolidinones / pharmacology*
  • Pyrrolidonecarboxylic Acid / analogs & derivatives
  • Pyrrolidonecarboxylic Acid / pharmacology*
  • Rats
  • Rats, Inbred Strains

Substances

  • Azepines
  • Benzenesulfonates
  • Coloring Agents
  • Insulin
  • Pyrrolidinones
  • laurocapram
  • dodecyl pyroglutamate
  • brilliant blue
  • N-methylpyrrolidone
  • Pyrrolidonecarboxylic Acid