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Dextran-protamine coated nanostructured lipid carriers as mucus-penetrating nanoparticles for lipophilic drugs.

Abstract：

:The main objectives of the present study were (i) to evaluate the effect of the mucus layer on saquinavir-loaded nanostructured lipid carriers (SQV-NLCs) uptake and (ii) to evaluate the mucopenetrating properties of dextran-protamine (Dex-Prot) coating on NLCs as per SQV permeability enhancement. Three different NLC formulations differing on particle size and surfactant content were obtained and coated with Dex-Prot complexes. SQV permeability was then evaluated across Caco-2 cell monolayers (enterocyte-like model) and Caco-2/HT29-MTX cell monolayers (mucus model). In the Caco-2 monolayers, Dex-Prot-NLCs increased up to 9-fold SQV permeability in comparison to uncoated nanoparticles. In the Caco-2/HT29-MTX monolayers, Dex-Prot-NLCs presenting a surface charge close to neutrality significantly increased SQV permeability. Hence, Dex-Prot complex coating is a promising strategy to ensure successful nanoparticle mucus-penetration, and thus, an efficient nanoparticle oral delivery. To our knowledge, this is the first time that Dex-Prot coating has been described as a nanoparticle muco-penetration enhancer across the intestinal mucus barrier.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Beloqui A,Solinís MÁ,des Rieux A,Préat V,Rodríguez-Gascón A

doi

10.1016/j.ijpharm.2014.04.027

subject

Has Abstract

pub_date

2014-07-01 00:00:00

pages

105-11

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(14)00255-5

journal_volume

468

pub_type

杂志文章

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