Nanostructuring Biomaterials with Specific Activities towards Digestive Enzymes for Controlled Gastrointestinal Absorption of Lipophilic Bioactive Molecules.
This review describes the development of novel lipid-based biomaterials that modulate fat digestion for the enhanced uptake of encapsulated lipophilic bioactive compounds (e.g. drugs and vitamins). Specific focus is directed towards analysing how key material characteristics affect the biological function of digestive lipases and manipulate lipolytic digestion. The mechanism of lipase action is a complex, interfacial process, whereby hydrolysis can be controlled by the ability for lipase to access and adsorb to the lipid-in-water interface. However, significant conjecture exists within the literature regarding parameters that influence the activities of digestive lipases. Important findings from recent investigations that strategically examined the interplay between the interfacial composition of the lipid microenvironment and lipolysis kinetics in simulated biophysical environments are presented. The correlation between lipolysis and the rate of solubilisation and absorption of lipophilic compounds in the gastrointestinal tract (GIT) is detailed. Greater insights into the mechanism of lipase action have provided a new approach for designing colloidal carriers that orally deliver poorly soluble compounds, directly impacting the pharmaceutical and food industries.
School of Pharmacy and Medical Sciences, University of South Australia, City East Campus, Adelaide, South Australia 5001, Australia.
Paul
P
Joyce
Institute of Fundamental Sciences, Massey University, Private Bag 11222, Palmerston North 4442, New Zealand.
Catherine P
CP
Whitby
School of Pharmacy and Medical Sciences, University of South Australia, City East Campus, Adelaide, South Australia 5001, Australia. Electronic address: clive.prestidge@unisa.edu.au.
Clive A
CA
Prestidge
D000284:Administration, Oral; D004337:Drug Carriers / Q000008:administration & dosage / Q000138:chemical synthesis*; D045703:Emulsifying Agents / Q000737:chemistry; D065569:Gastrointestinal Absorption / Q000187:drug effects* / Q000502:physiology; D041981:Gastrointestinal Tract / Q000187:drug effects / Q000502:physiology; D006801:Humans; D008049:Lipase / Q000737:chemistry*; D050356:Lipid Metabolism / Q000187:drug effects; D008055:Lipids / Q000737:chemistry*; D008066:Lipolysis; D008958:Models, Molecular; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D055553:Prescription Drugs / Q000493:pharmacokinetics*; D000072417:Protein Domains; D012822:Silicon Dioxide / Q000737:chemistry; D014815:Vitamins / Q000493:pharmacokinetics
D004337:Drug Carriers; D045703:Emulsifying Agents; D008055:Lipids; D055553:Prescription Drugs; D014815:Vitamins; D012822:Silicon Dioxide; D008049:Lipase
lipase; lipid digestion; lipid-based drug delivery; lipolysis; nanostructure