Abstract
Objective: The main objective of the present investigation was to develop microbeads of tenofovir. Tenofovir, a BCS class III drug has a poor bioavailability of 25%, and it is administered 300 mg once a day. By incorporating the drug into a microparticulate carrier, it is expected that the dissolution profile and the oral bioavailability may be increased.
 Methods: Reinforced gellan-chitosan and calcium chloride beads of tenofovir were prepared by ionotropic gelation method employing various different concentrations of gellan, chitosan, calcium chloride and tenofovir. The beads were evaluated for various physico-chemical parameters such as particle size determination, drug entrapment efficiency, swelling studies, infra red spectroscopy study, differential scanning calorimetry, x-ray diffraction analysis, scanning electron microscopy, in vitro drug release study, cytotoxicity study and in vivo oral bioavailability studies.
 Results: From the results, it can be concluded that the formulation TB-III exhibited higher drug entrapment efficiency (46.09±0.21), a higher swelling index, sustained drug release for a period of 24 h. The pharmacokinetic profile of the drug from microbeads exhibited an increased oral bioavailability (1.25 times higher than that of pure drug), decreased elimination rate (1.32 times lesser for drug in microbeads) with prolonged elimination half-life (1.32 times higher than pure tenofovir).
 Conclusion: Tenofovir loaded microbeads demonstrated as a better delivery system for the modified release of drug and also to navigate the drawbacks associated with the conventional therapy.
Highlights
Sustained release drug delivery system is an ideal approach that provides a uniform concentration of drug available at the site of absorption
In the past few decades, scientists have given a greater effort in the development of novel drug delivery systems, which assures the targeting of drug to a particular area and to and maintain the required concentration to exhibit better therapeutic response [2]
A nucleotide reverse transcriptase inhibitors (NtRTI’s) approved by USFDA in 2001 for the treatment of human immunodeficiency virus infection (HIV), has oral bioavailability was reported to be in the range of 25-30% [8]
Summary
Sustained release drug delivery system is an ideal approach that provides a uniform concentration of drug available at the site of absorption. Due to this unique property, the system tends to maintain appropriate plasma concentrations in the therapeutic range [1]. Sustained release formulations are gained importance for the oral administration of drug owing to their maintenance of consistent blood levels. The main purpose of this study was to formulate and evaluate tenofovir microbeads for improving the sustained the release of the drug, which in turn improve the oral bioavailability. Various parameters such as particle size determination, drug entrapment efficiency, swelling studies, infrared spectroscopy study, differential scanning calorimetry, x-ray diffraction analysis, scanning electron microscopy, in vitro drug release study, cytotoxicity study and in vivo bioavailability studies were systematically investigated
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