Silica-lipid hybrid microcapsules: influence of lipid and emulsifier type on in vitro performance

Int J Pharm. 2011 May 16;409(1-2):297-306. doi: 10.1016/j.ijpharm.2011.02.038. Epub 2011 Mar 1.

Abstract

This study reports on the physicochemical characterisation and in vitro investigations of macro-porous silica-lipid hybrid (SLH) microcapsules when formulated using various lipids: long-chain triglycerides (LCT), medium-chain triglycerides (MCT), medium-chain mono-, diglycerides (MCMDG); and emulsifiers: anionic lecithin and cationic oleylamine. For the lipophilic compound coumarin 102 (logP=4.09), a complete and immediate in vitro release was attained for the SLH microcapsules under simulated intestinal sink conditions. The in vitro digestion study of various types of SLH microcapsules demonstrates: (i) reduced variability and enhanced lipid digestibility for the MCMDG-based microcapsules (i.e. 90-100% lipolysis) in comparison with an equivalent lipid solution and emulsion (50-90% lipolysis); and (ii) more controllable digestion kinetics for the LCT-based microcapsules which produce a lipolysis rate higher than that of a lipid solution but lower than that of a lipid emulsion. The drug phase partition results show approximately 5- to 17-fold increase in the drug solubilisation degree resulting from the digestion of MCT and MCMDG-based microcapsules (116 μg/mL), and LCT-based microcapsules (416 μg/mL) in comparison with the blank micellar medium (24 μg/mL). In conclusion, the SLH microcapsules could be tailored to manipulate the digestion patterns of both medium- and long-chain lipids in order to maximise the drug solubilisation capacity.

Publication types

  • Comparative Study

MeSH terms

  • Amines / chemistry
  • Capsules
  • Coumarins / administration & dosage*
  • Coumarins / chemistry
  • Diglycerides / chemistry*
  • Drug Delivery Systems
  • Emulsions
  • Excipients / chemistry
  • Intestinal Mucosa / metabolism
  • Lecithins / chemistry
  • Lipolysis
  • Porosity
  • Silicon Dioxide / chemistry*
  • Solubility
  • Triglycerides / chemistry*

Substances

  • Amines
  • Capsules
  • Coumarins
  • Diglycerides
  • Emulsions
  • Excipients
  • Lecithins
  • Triglycerides
  • Silicon Dioxide
  • oleylamine