Bioavailability of oral drug formulations and methods for its improvement

Ipatova O.M.1, Torkhovskaya T.I.1 , Medvedeva N.V.1, Prozorovskiy V.N.1, Ivanova N.D.1, Shironin A.V.1, Baranova V.S.1, Archakov A.I.1

1. Institute of Biomedical Chemistry RAMS
Section: Experimental/Clinical Study
DOI: 10.18097/PBMC20105601101      PubMed Id: 21328915
Year: 2010  Volume: 56  Issue: 1  Pages: 101-119
The recent studies in nanotechnology resulted in the development of novel formulations with improved bioavailability. This is especially important for oral administered drugs as the most convenient formulations. The current review deals with the processes occurring at the gastro-intestinal (GI) tract and their influence on the drug form. The increase of bioavailability of the drug may be achieved through designing novel formulations according to the specific drug properties. They include capsules that release pharmaceutical agents at various parts of the GI tract, floating systems that prolong the presence of the drug in the GI tract, dispersed forms with surface-active soluble polymers, micelles that carry poor-soluble drugs inside their non-polar core, agents that facilitate tight junction opening, such as caprate and chitosan, and lipid-based formulations. The own data show the stimulating influence of phospholipid nanoparticles on peroral absorption of drug indomethacin in rats and on passage of transport marker and drugs through Caco-2 cell monolayer in vitro. The review summarizes current understanding of factors that influence the bioavailability of the oral drug forms, currently used models for pharmacokinetic studies, and various approaches to developing novel pharmaceutical forms that increase the bioavailability of the drugs.
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Keywords: drug bioavailability, intestinal absorption, enterocytes, drug formulations, paracellular absorption, lymphatic transport, phospholipid nanoparticles

Ipatova, O. M., Torkhovskaya, T. I., Medvedeva, N. V., Prozorovskiy, V. N., Ivanova, N. D., Shironin, A. V., Baranova, V. S., Archakov, A. I. (2010). Bioavailability of oral drug formulations and methods for its improvement. Biomeditsinskaya Khimiya, 56(1), 101-119.
This paper is also available as the English translation: 10.1134/S1990750810010117
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