Lipid nanoparticles enhance the absorption of cyclosporine A through the gastrointestinal barrier: In vitro and in vivo studies

International Journal of Pharmaceutics
Melissa GuadaMaría J Blanco-Prieto

Abstract

In the present work, the feasibility of cyclosporine A lipid nanoparticles (CsA LN) for oral administration was investigated. Three CsA LN formulations were developed using Precirol as lipid matrix, one stabilized with Tween(®) 80 (Tw) and the other two with mixtures of phosphatidylcholine or Pluronic(®) F127 with taurocholate (Lec:TC and PL:TC, respectively). The physical characteristics of the LN were studied under gastrointestinal pH and their integrity was found to be dependent on the stabilizers. The in vitro intestinal permeability was assessed with a human colon adenocarcinoma cell model and in vivo pharmacokinetic and biodistribution studies were performed in Balb/c mice using Sandimmune Neoral(®) as reference. In vitro results showed the highest CsA permeability with the LN containing Lec:TC. In contrast, the best in vivo performance was achieved from the LN containing Tw. The bioavailability of CsA was matched and even enhanced with Precirol nanoparticles. This study suggests the suitability of LN as promising vehicles for CsA oral delivery.

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Citations

Feb 16, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Melissa GuadaMaria J Blanco-Prieto
Feb 2, 2016·Journal of Controlled Release : Official Journal of the Controlled Release Society·Melissa GuadaMaria J Blanco-Prieto
Mar 15, 2016·International Journal of Pharmaceutics·Melissa GuadaMaria J Blanco-Prieto
Dec 21, 2017·Expert Opinion on Drug Delivery·Hanan Al-LawatiAfsaneh Lavasanifar
Oct 24, 2019·Nanomedicine·Amber Nagy, Nicholas L Robbins
Jan 16, 2021·Pharmaceutics·Amandine GendronMariana Varna
Dec 29, 2020·Colloids and Surfaces. B, Biointerfaces·Pallavi ChandVikas Jain
Mar 18, 2021·International Journal of Nanomedicine·Salma M MohyeldinNazik A Elgindy
Oct 17, 2021·Biopharmaceutics & Drug Disposition·Hui QiuWenming Wu

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