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Enzymatic characterization of lipid-based drug delivery systems
Authors:Ljusberg-Wahren Helena  Seier Nielsen Flemming  Brogård Mattias  Troedsson Emma  Müllertz Anette
Affiliation:1. Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia;2. Department of Microbiology and Immunology, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt;1. Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla, 90112, Thailand;2. Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla, 90112, Thailand;3. Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla, 90112, Thailand;4. Pharmacy Technician Department, Sirindhron College of Public Health of Suphanburi, 77 moo4, Tubteelek sub-district, Mueang district, Suphanburi, 72000, Thailand;5. Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla, 90112, Thailand;1. A.E. Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, 8, Arbuzov Str., Kazan 420088, Russian Federation;2. Kazan (Volga Region) Federal University, A.M. Butlerov Chemical Institute, 18, Kremlin Str., Kazan 420008, Russian Federation
Abstract:
The present work introduces a simple and robust in vitro method for enzymatic characterisation of surface properties of lipid dispersions in aqueous media. The initial lipolysis rate in biorelevant media, using pancreatic lipase and a self-microemulsifying formulation (SMEDDS) containing digestible lipids as substrate, was determined. The impact of incorporating two sparingly water soluble model drugs, probucol and halofantrine, into the SMEDDS was studied. It was found that both model drugs reduced the initial rate of lipolysis compared with the vehicle, probucol having a larger effect than halofantrine. The reduction of initial lipolysis rate indicates that probucol and halofantrine are bound in the water/emulsion interface limiting the substrate availability.
Keywords:
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