In vitro lipolysis has emerged as a powerful tool in the development of in vitro in vivo correlation
for Lipid-based Drug Delivery System (LbDDS). In vitro lipolysis possesses the ability to mimic
the assimilation of LbDDS in the human biological system. The digestion medium for in vitro lipolysis
commonly contains an aqueous buffer media, bile salts, phospholipids and sodium chloride. The concentrations
of these compounds are defined by the physiological conditions prevailing in the fasted or fed
state. The pH of the medium is monitored by a pH-sensitive electrode connected to a computercontrolled
pH-stat device capable of maintaining a predefined pH value via titration with sodium hydroxide.
Copenhagen, Monash and Jerusalem are used as different models for in vitro lipolysis studies.
The most common approach used in evaluating the kinetics of lipolysis of emulsion-based encapsulation
systems is the pH-stat titration technique. This is widely used in both the nutritional and the pharmacological
research fields as a rapid screening tool. Analytical tools for the assessment of in vitro lipolysis
include HPLC, GC, HPTLC, SEM, Cryo TEM, Electron paramagnetic resonance spectroscopy, Raman
spectroscopy and Nanoparticle Tracking Analysis (NTA) for the characterization of the lipids and colloidal
phases after digestion of lipids. Various researches have been carried out for the establishment of
IVIVC by using in vitro lipolysis models. The current publication also presents an updated review of
various researches in the field of in vitro lipolysis.
Keywords: In vitro lipolysis, IVIVC, lipase, pH stat, lipid based drug delivery systems, lipid digestion, biorelevant media.
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Xiao, L.; Yi, T. Liu, Zhou, H. The in vitro lipolysis of lipid-based drug delivery systems: A newly identified relationship between drug release and liquid crystalline phase. BioMed Res. Int., 2016, 20(16), 1-9.
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