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Simulating the digestion of lipid-based drug delivery systems (LBDDS): overview of in vitro lipolysis models
Bolko, Katarina (Author), Zvonar Pobirk, Alenka (Author), Gašperlin, Mirjana (Author)

URLURL - Presentation file, Visit http://acta.chem-soc.si/61/61-1-1.pdf This link opens in a new window

Abstract
One of the greatest challenges in the pharmaceutical science is the improvement of oral bioavailability of poorly solub- le drugs. Lately, one of the most attractive approaches has been formulation of lipid based drug delivery systems. Howe- ver, the emerging popularity of these systems in the last decade has brought to light the need for efficient methods for their in vitro evaluation that would serve as their in vivo behaviour prediction tool. Because lipids are subject to lipid di- gestion and multiple absorption pathways in vivo , simple dissolution tests are not predictive enough when testing lipid based delivery systems. To assert these needs, the in vitro lipolysis model has been developed, utilizing pancreatic enzy- mes, bile and phospholipids in a temperature controlled chamber to simulate in vivo digestion. However, with very va- riable physiological conditions in gastrointestinal tract, this model has not been yet standardised and experiments vary among different laboratories. This review discusses in vivo events following oral application of lipid based delivery, in vitro lipolysis models to emulate them and their future perspectives.

Language:English
Keywords:pH stat method, self-microemulsifying systems, lipid digestion, triglyceride, bioavailability prediction
Work type:Not categorized (r6)
Tipology:1.02 - Review Article
Organization:FFA - Faculty of Pharmacy
Year:2014
Publisher:Slovensko kemijsko društvo
Number of pages:str. 1-10
Numbering:Vol. 61, no. 1
UDC:543.2/.9:615.014
ISSN on article:1318-0207
COBISS.SI-ID:3630193 Link is opened in a new window
Views:364
Downloads:161
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Record is a part of a journal

Title:Acta chimica slovenica
Shortened title:Acta chim. slov.
Publisher:Slovensko kemijsko društvo, =Slovenian Chemical Society
ISSN:1318-0207
COBISS.SI-ID:14086149 This link opens in a new window

Secondary language

Language:Slovenian
Abstract:
Enega največjih izzivov na področju farmacevtskih znanosti predstavlja izboljšanje biološke uporabnosti peroralno vnesenih učinkovin, ki so slabo vodotopne. Z namenom zagotavljanja tega cilja raziskovalci v zadnjem času veliko pozornosti namenjajo razvoju na lipidih osnovanih dostavnih sistemov. Z uveljavljanjem teh sistemov in širjenjem njihove uporabe v zadnjih dvajsetih letih se je razkrila tudi nujnost razvoja novih in vitro metod, ki bi omogočile učinkovito napovedovanje njihovega obnašanja in vivo. Slednje otežuje predvsem dejstvo, da se na lipidih osnovani dostavni sistemi v prebavnem traktu vključujejo v proces prebave, ki lahko spremeni njihove lastnosti. Z vgradnjo v na lipidih osnovani sistem lahko vplivamo tudi na pot absorpcije učinkovine iz prebavnega trakta. Ker enostavni testi sproščanja učinkovine in vitro nimajo ustrezne napovedne moči za in vivo obnašanje teh dostavnih sistemov, se razvijajo novi modeli in vitro lipolize. Slednji posnemajo fiziološke pogoje prebave z izpostavitvijo testiranega vzorca pankreatičnim encimom, žolču in fosfolipidom v termostatirani reakcijski posodi. Zaradi spremenljivosti pogojev v prebavnem traktu model in vitro lipolize še ni standardiziran, kar se odraža v veliki variabilnosti rezltatov,pridobljenih med različnimi laboratoriji. V preglednem članku smo se osredotočili predvsem na predstavitev fizioloških procesov, ki sledijo peroralnemu vnosu na lipidih osnovanih sistemov ter pregledu in perspektivnosti obstoječih modelov in vitro lipolize.

Keywords:biološka uporabnost, trigliceridi, samo-mikroemulgirajoči sistem, lipidna presnova, pH vrednosti

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