Tamoxifen-loaded lecithin organogel (LO) for topical application: Development, optimization and characterization

Int J Pharm. 2013 Feb 28;444(1-2):47-59. doi: 10.1016/j.ijpharm.2013.01.029. Epub 2013 Jan 24.

Abstract

Lecithin organogels (LOs) are semi-solid systems with immobilized organic liquid phase in 3-D network of self-assembled gelators. This paper attempts to study the various attributes of LOs, starting from selection of materials, optimization of influential components to LO specific characterization. After screening of various components (type of gelators, organic and aqueous phase) and construction of phase diagrams, a D-optimal mixture design was employed for the systematic optimization of the LO composition. The response surface plots were constructed for various response variables, viz. viscosity, gel strength, spreadability and consistency index. The optimized LO composition was searched employing overlay plots. Subsequent validation of the optimization study employing check-point formulations, located using grid search, indicated high degree of prognostic ability of the experimental design. The optimized formulation was characterized for morphology, drug content, rheology, spreadability, pH, phase transition temperatures, and physical and chemical stability. The outcomes of the study were interesting showing high dependence of LO attributes on the type and amount of phospholipid, Poloxamer™, auxillary gelators and organic solvent. The optimized LO was found to be quite stable, easily applicable and biocompatible. The findings of the study can be utilized for the development of LO systems of other drugs for the safer and effective topical delivery.

MeSH terms

  • Administration, Topical
  • Drug Carriers / chemistry*
  • Drug Design
  • Drug Stability
  • Estrogen Antagonists / chemistry*
  • Gels
  • Lecithins / chemistry*
  • Tamoxifen / chemistry*
  • Transition Temperature
  • Viscosity

Substances

  • Drug Carriers
  • Estrogen Antagonists
  • Gels
  • Lecithins
  • Tamoxifen