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

[Display omitted] 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 phosphatidylc...

Full description

Saved in:
Bibliographic Details
Published in:International journal of pharmaceutics 2016-03, Vol.500 (1-2), p.154-161
Main Authors: Guada, Melissa, Lasa-Saracíbar, Beatriz, Lana, Hugo, Dios-Viéitez, Maria del Carmen, Blanco-Prieto, Maria J.
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Bioavailability
Biological Availability
Caco-2 Cells
Cyclosporine - administration & dosage
Cyclosporine - chemistry
Cyclosporine - pharmacokinetics
Cyclosporine A
Diglycerides - chemistry
Female
Gastrointestinal stability
Humans
Immunosuppressive Agents - administration & dosage
Immunosuppressive Agents - chemistry
Immunosuppressive Agents - pharmacokinetics
Intestinal Absorption
Lipid nanoparticles
Mice, Inbred BALB C
Nanoparticles - administration & dosage
Nanoparticles - chemistry
Oral route
Phosphatidylcholines - chemistry
Poloxamer - chemistry
Polysorbates - chemistry
Taurocholic Acid - chemistry
Tissue distribution
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] 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.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2016.01.037