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Lipid Architectonics for Superior Oral Bioavailability of Nelfinavir Mesylate: Comparative in vitro and in vivo Assessment
T. Belubbi, S. Shevade, V. Dhawan, V. Sridhar, A. Majumdar, R. Nunes, F. Araújo, B. Sarmento, K. Nagarsenker, F. Steiniger, A. Fahr, A. Magarkar, A. Bunker, M. Nagarsenker,
Jazyk angličtina Země Spojené státy americké
Typ dokumentu srovnávací studie, časopisecké články
Perzistentní odkaz
https://www.medvik.cz/link/bmc19012384
- MeSH
- biologická dostupnost MeSH
- Caco-2 buňky MeSH
- inhibitory HIV-proteasy chemie MeSH
- krysa rodu rattus MeSH
- lidé MeSH
- lipidy chemie MeSH
- nelfinavir chemie farmakokinetika MeSH
- potkani Sprague-Dawley MeSH
- rozpustnost MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- lidé MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- srovnávací studie MeSH
Nelfinavir mesylate (NFV), a human immunodeficiency virus (HIV) protease inhibitor, is an integral component of highly active anti retro viral therapy (HAART) for management of AIDS. NFV possesses pH-dependent solubility and has low and variable bioavailability hampering its use in therapeutics. Lipid-based particulates have shown to improve solubility of poorly water soluble drugs and oral absorption, thereby aiding in improved bioavailability. The current study compares potential of vesicular and solid lipid nanocarriers of NFV with drug nanocrystallites and microvesicular systems like cochleates in improving bioavailability of NFV. The paper outlines investigation of systems using in vitro models like in vitro lipolysis, in vitro release, and permeation through cell lines to predict the in vivo potential of nanocarriers. Finally, in vivo pharmacokinetic study is reported which provided proof of concept in sync with results from in vitro studies. Graphical Abstract ᅟ.
Citace poskytuje Crossref.org
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- $a Belubbi, Tejashree $u Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai, Maharashtra, 400098, India.
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- $a Nelfinavir mesylate (NFV), a human immunodeficiency virus (HIV) protease inhibitor, is an integral component of highly active anti retro viral therapy (HAART) for management of AIDS. NFV possesses pH-dependent solubility and has low and variable bioavailability hampering its use in therapeutics. Lipid-based particulates have shown to improve solubility of poorly water soluble drugs and oral absorption, thereby aiding in improved bioavailability. The current study compares potential of vesicular and solid lipid nanocarriers of NFV with drug nanocrystallites and microvesicular systems like cochleates in improving bioavailability of NFV. The paper outlines investigation of systems using in vitro models like in vitro lipolysis, in vitro release, and permeation through cell lines to predict the in vivo potential of nanocarriers. Finally, in vivo pharmacokinetic study is reported which provided proof of concept in sync with results from in vitro studies. Graphical Abstract ᅟ.
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- $a Shevade, Sukhada $u Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai, Maharashtra, 400098, India.
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