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Formulation and transport properties of tenofovir loaded liposomes through Caco-2 cell model
Faculty
Pharmacy
Year:
2013
Type of Publication:
Article
Pages:
318-326
Authors:
Zidan, Ahmed S, Spinks, Crystal B, Habib, Muhammad J, Khan, Mansoor A
DOI:
10.3109/08982104.2013.810645
Journal:
JOURNAL OF LIPOSOME RESEARCH INFORMA HEALTHCARE
Volume:
23
Research Area:
Biochemistry \& Molecular Biology; Pharmacology \& Pharmacy
ISSN
ISI:000325522500007
Keywords :
Caco-2, cytotoxicity, permeability, proliposomes, tenofovir
Abstract:
The aim was to investigate the potential of proliposomes to improve the permeability of tenofovir, anti-HIV, for oral delivery. Tenofovir was incorporated into phosphatidylcholine proliposomes and their absorption was determined in Caco-2 cell cultures grown on Transwell inserts using aqueous drug solutions as reference. Five batches of proliposomes were prepared with different stearylamine levels and characterized in terms of vesicular morphology, drug encapsulation efficiency (EEF), drug leakage, vesicular sizing and surface charges. Cytotoxicity of the reconstituted liposomes was evaluated by the MTT assay. The obtained results showed that increasing the incorporated percentage of stearylamine led to an increase in drug encapsulation, a slower drug leakage and larger liposomes formed. Compared to the drug solutions at corresponding concentrations, the proposed formulations showed a positive relationship (R-2 = 0.9756) for the influence of increasing the stearylamine percentage on reduction of mitochondrial activity. Regarding the drug permeability, enhancements of apparent permeability by 16.5- and 5.2-folds were observed for proliposomes formulations with 5\% and 15\% stearylamine, respectively. A good correlation was observed between the Caco-2 and dialysis models that might indicate passive diffusion as well as paracellular transport as suggested mechanisms for drug absorption. Cationic proliposomes offered a potential formulation to improve the permeation of tenofovir.
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