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Oral bioavailability enhancement of a hydrophilic drug delivered via folic acid-coupled liposomes in rats

Ling, S.S.N., Yuen, K.H., Magosso, E., Barker, S.A. (2009) Oral bioavailability enhancement of a hydrophilic drug delivered via folic acid-coupled liposomes in rats. Journal of Pharmacy and Pharmacology, 61 (4). pp. 445-449. ISSN 0022-3573. (doi:10.1211/jpp.61.04.0005) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided. (Contact us about this Publication)
Official URL
https://doi.org/10.1211/jpp.61.04.0005

Abstract

Objectives: A liposome preparation that is amenable to receptor-mediated endocytosis has been developed to enhance the oral bioavailability of poorly absorbable peptidomimetic drugs by use of folic acid as the mediator of liposomal uptake. Methods: Folic acid was physically coupled to the surface of the liposomes and cefotaxime was used as the model drug. In-vivo evaluation was carried out on eight Sprague-Dawley rats in a two-way crossover study to compare the oral bioavailability of cefotaxime loaded in folic acid-free liposomes and folic acid-coupled liposomes. Blood samples were collected from the tail vein and plasma cefotaxime levels were determined using an HPLC method. Key findings: Enhanced oral bioavailability (AUC 0‐∞) of cefotaxime was observed when administered via folic acid-coupled liposomes. The peak plasma concentration (Cmax) of cefotaxime was increased when administered via folic acid-coupled liposomes as compared with folic acid-free liposomes. At 90% confidence interval, the value for AUC 0‐∞ was 1.4-2-times higher and the value for Cmax was 1.2-1.8-times higher for the folic acid-coupled liposomes compared with folic acid-free liposomes. Conclusions: Folic acid could enhance the uptake of liposomally entrapped drug. It could be a useful candidate to supplement liposome delivery systems.

Item Type: Article
DOI/Identification number: 10.1211/jpp.61.04.0005
Uncontrolled keywords: Cefotaxime, Folic acid, Liposomes, cefotaxime, folic acid, liposome, peptidomimetic agent, cefotaxime, folic acid, liposome, animal experiment, area under the curve, article, blood sampling, controlled study, drug absorption, drug bioavailability, drug blood level, drug delivery system, drug uptake, endocytosis, high performance liquid chromatography, hydrophilicity, in vivo study, male, nonhuman, rat, Sprague Dawley rat, animal, bioavailability, chemistry, crossover procedure, drug delivery system, drug effect, endocytosis, oral drug administration, randomization, Administration, Oral, Animals, Biological Availability, Cefotaxime, Cross-Over Studies, Drug Delivery Systems, Endocytosis, Folic Acid, Liposomes, Male, Random Allocation, Rats, Rats, Sprague-Dawley
Divisions: Faculties > Sciences > Medway School of Pharmacy
Depositing User: Susan Barker
Date Deposited: 27 Nov 2019 10:56 UTC
Last Modified: 27 Nov 2019 10:56 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/78857 (The current URI for this page, for reference purposes)
Barker, S.A.: https://orcid.org/0000-0003-4880-0253
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