Biodegradable polymeric nanocapsules based on poly(DL-lactide) for genistein topical delivery: obtention, characterization and skin permeation studies

J Biomed Nanotechnol. 2013 Mar;9(3):527-34. doi: 10.1166/jbn.2013.1555.

Abstract

The isoflavone genistein (GEN) is a natural product with potential applications for skin cancer treatment and chemoprevention; however its high lipophilicity and chemical instability limits its clinical use. Therefore, attempts towards protecting GEN against degradation and increasing its penetration in the skin might be a valid approach. In this work, GEN loaded-PLA nanocapsules (GEN-NC) were prepared by interfacial deposition of preformed polymer (nanoprecipitation); physicochemical characterization and stability studies for 90 days were conducted. GEN-NC were incorporated into semi-solid formulations and permeation experiments were carried out using porcine ear skin. GEN-NC optimized formulation presented a mean diameter of 139 +/- 7.31 nm, polydispersity index of 0.128 +/- 0.08, encapsulation efficiency of 89.63 +/- 2.27% and drug loading from 0.6 to 1.4 w/w%. Stability studies demonstrated that nanocapsules did not exhibit aggregation during the 90 days of the assay, however, a drop in encapsulation efficiency was observed in the first 10 days. Permeation experiments demonstrated that a higher amount of GEN reaches deeper layers of the skin and increased penetration was achieved when GEN-NC were incorporated in a semi-solid gel formulation, indicating that GEN-NC might be a promising nanocarrier system for skin delivery of GEN.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Animals
  • Biocompatible Materials / pharmacology*
  • Biodegradation, Environmental / drug effects
  • Chemical Phenomena
  • Chemistry, Pharmaceutical
  • Genistein / administration & dosage*
  • Genistein / pharmacology*
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • Microscopy, Atomic Force
  • Nanocapsules / chemistry*
  • Particle Size
  • Permeability / drug effects
  • Polyesters / chemistry*
  • Skin Absorption / drug effects*
  • Static Electricity
  • Sus scrofa

Substances

  • Biocompatible Materials
  • Nanocapsules
  • Polyesters
  • poly(lactide)
  • Genistein