Tacrolimus-loaded nanostructured lipid carriers for oral delivery-in vivo bioavailability enhancement

[Display omitted] The aim of the present study was to assess the Tacrolimus (TL) loaded nanostructured lipid carrier for enhancement in solubilisation potential, pharmacokinetic parameters and lymphatic distribution profile. The solubilisation potential of TL-NLC was determined via application of dy...

Full description

Saved in:
Bibliographic Details
Published in:European journal of pharmaceutics and biopharmaceutics 2016-12, Vol.109, p.149-157
Main Authors: Khan, Saba, Shaharyar, M., Fazil, Mohammad, Hassan, Md Quamrul, Baboota, Sanjula, Ali, Javed
Format: Article
Language:English
Subjects:
Administration, Oral
Albino wistar rats
Animals
Area Under Curve
Bioavailability
Biological Availability
Chromatography, High Pressure Liquid
Drug Carriers - chemistry
Drug Compounding - methods
Drug Design
Drug Stability
Fatty Acids - chemistry
Female
Immunosuppressive Agents - administration & dosage
Immunosuppressive Agents - chemistry
Immunosuppressive Agents - pharmacokinetics
In vitro lipolysis
Kinetics
Lipids - chemistry
Lipolysis
Lymph Nodes - drug effects
Lymphatic distribution
Male
Nanostructured lipid carrier
Nanostructures - chemistry
Particle Size
Rats
Rats, Wistar
Software
Solubility
Tacrolimus
Tacrolimus - administration & dosage
Tacrolimus - pharmacokinetics
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] The aim of the present study was to assess the Tacrolimus (TL) loaded nanostructured lipid carrier for enhancement in solubilisation potential, pharmacokinetic parameters and lymphatic distribution profile. The solubilisation potential of TL-NLC was determined via application of dynamic lipolysis models, which simulate the GIT environment and the intestinal conditions. The in vitro lipolysis studies revealed significantly high solubilisation (***p0.99). The in vivo, lymphatic and organ distribution studies were performed in albino wistar rats. There was marked increase of 7.2 folds in relative bioavailability of TL-NLC in comparison to TL suspension. Furthermore, study findings demonstrated that the lymphatic distribution of TL-NLC was enhanced by 19.25 folds in comparison to TL suspension. The results of dynamic lipolysis, bioavailability, lymphatic and other organ distribution studies confirmed that incorporation of TL in hybrid of lipids with different fatty acid chain length could substantially improve its in vivo prospect.
ISSN:0939-6411
1873-3441
DOI:10.1016/j.ejpb.2016.10.011