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Mechanism of transport of saquinavir-loaded nanostructured lipid carriers across the intestinal barrier

Beloqui, Ana ; Solinís, María Ángeles ; Gascón, Alicia R. ; del Pozo-Rodríguez, Ana ; des Rieux, Anne ; Préat, Véronique

Journal of controlled release, 2013-03, Vol.166 (2), p.115-123 [Peer Reviewed Journal]

Netherlands: Elsevier B.V

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Title:
Mechanism of transport of saquinavir-loaded nanostructured lipid carriers across the intestinal barrier
Author: Beloqui, Ana ; Solinís, María Ángeles ; Gascón, Alicia R. ; del Pozo-Rodríguez, Ana ; des Rieux, Anne ; Préat, Véronique
Subjects: Anti-HIV Agents - administration & dosage ; Anti-HIV Agents - chemistry ; Anti-HIV Agents - pharmacokinetics ; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism ; bioavailability ; Biological Availability ; Biological Transport, Active ; Caco-2 ; Caco-2 Cells ; Chemistry, Pharmaceutical ; Chromatography, High Pressure Liquid ; Coculture Techniques ; Drug Carriers ; Drug Compounding ; drugs ; Endocytosis ; Endocytosis - drug effects ; Enterocytes ; Humans ; Intestinal Absorption ; Lipids - chemistry ; M cell ; Nanoparticle ; Nanoparticles ; P-gp substrate ; Particle Size ; permeability ; physicochemical properties ; physiological transport ; Saquinavir - administration & dosage ; Saquinavir - chemistry ; Saquinavir - pharmacokinetics ; Solubility ; Surface-Active Agents ; surfactants ; Suspensions ; Transcytosis
Is Part Of: Journal of controlled release, 2013-03, Vol.166 (2), p.115-123
Notes: http://dx.doi.org/10.1016/j.jconrel.2012.12.021
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Description: The aims of this work were (i) to evaluate the potential of nanostructured lipid carriers (NLCs) as a tool to enhance the oral bioavailability of poorly soluble compounds using saquinavir (SQV), a BCS class IV drug and P-gp substrate as a model drug, and (ii) to study NLC transport mechanisms across the intestinal barrier. Three different NLC formulations were evaluated. SQV transport across Caco-2 monolayers was enhanced up to 3.5-fold by NLCs compared to SQV suspension. M cells did not enhance the transport of NLCs loaded with SQV. The size and amount of surfactant in the NLCs influenced SQV's permeability, the transcytosis pathway and the efflux of SQV by P-gp. An NLC of size 247nm and 1.5% (w/v) surfactant content circumvented P-gp efflux and used both caveolae- and clathrin-mediated transcytosis, in contrast to the other NLC formulations, which used only caveolae-mediated transcytosis. By modifying critical physicochemical parameters of the NLC formulation, we were thus able to overcome the P-gp drug efflux and alter the transcytosis mechanism of the nanoparticles. These findings support the use of NLCs approaches for oral delivery of poorly water-soluble P-gp substrates. [Display omitted]
Publisher: Netherlands: Elsevier B.V
Language: English

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Mechanism of transport of saquinavir-loaded nanostructured lipid carriers across the intestinal barrier

Beloqui, Ana ; Solinís, María Ángeles ; Gascón, Alicia R. ; del Pozo-Rodríguez, Ana ; des Rieux, Anne ; Préat, Véronique

Netherlands: Elsevier B.V

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