ENHANCED ORAL BIOAVAILABILITY OF TENOFOVIR FROM IONOTROPICALLY GELLED MICROBEADS

  • DHANDAPANI NAGASAMY VENKATESH Department of Pharmaceutics, JSS College of Pharmacy, Udhagamandalam 643001
  • PREETY RAO Department of Pharmaceutical Biotechnology, JSS College of Pharmacy, Udhagamandalam 643001
  • RAMAN RAJESHKUMAR Department of Pharmaceutical Biotechnology, JSS College of Pharmacy, Udhagamandalam 643001

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.

Keywords: Tenofovir, Gellan, Chitosan, Ionotropic gelation, Oral bioavailability

References

1. Shefrin S, Sreelaxmi CS, Vishnu V, Sreeja CN. Enzymosomes: a rising effectual tool for targeted drug delivery system. Int J Appl Pharm 2017;9:1-9.
2. Revathy BM, Lakshmi VS, Aishwarya MU, Keerthana R, Sreeja CN. Porphysomes: a paradigm shift in targeted drug delivery. Int J Appl Pharm 2018;10:1-6.
3. Vaizoglu O, Speiser P. Intelligent drug delivery systems. Trends Pharmacol Sci 1982;3:28-30.
4. Oluwatoyin AO, Adenike O, Alf L. Formulation and in vitro evaluation of natural gum-based microbeads for delivery of ibuprofen. Trop J Pharm Res 2014;13:1577-83.
5. Rajinikanth PS, Sankar C, Mishra B. Sodium alginate microspheres of metoprolol tartarate for intranasal systemic delivery. Drug Delivery 2003;10:21-8.
6. Zhang J, XU S, Zhang S, Du Z. Preparation and characterization of tamarind gum/sodium alginate composite gel beads. Iranian Polym J 2008;17:899-906.
7. Odeku OA, Lamprecht A, Okunlola A. Characterization and evaluation of four natural gums as polymers in the formulations of diclofenac sodium microbeads. Int J Biol Macromol 2013;58:113-20.
8. Praksah S, Vidyadhara S, Sasidhar RL, Abhijit D, Akhilesh D. Development and characterization of ritonavir nanosuspension for oral use. Der Pharm Lett 2013;5:48-55.
9. Patil JS, Kamalapur MV, Marapur SC, Shiralshetti SS. Ionotropically gelled novel hydrogel beads: preparation, characterization and in vitro evaluation. Ind J Pharm Sci 2011;73:504-9.
10. Higuchi T. Mechanism of sustained action medication: theoretical analysis of rate of solid drugs dispersed in solid matrices. J Pharm Sci 1963;52:1145-9.
11. Koresmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanism of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25-35.
12. Ritger PL, Peppas NA. A simple equation for description of solute release, I: fickian and non-fickian release from non-swellable devices in the form of slabs, spheres, cylinders (or) discs. J Controlled Release 1985;5:23-35.
13. Sawyer M, Ratain MJ. Body surface area as a determinant of pharmacokinetics and drug dosing. Invest New Drugs 2001;19:171-7.
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VENKATESH, D. N., RAO, P., & RAJESHKUMAR, R. (2019). ENHANCED ORAL BIOAVAILABILITY OF TENOFOVIR FROM IONOTROPICALLY GELLED MICROBEADS. International Journal of Applied Pharmaceutics, 11(4), 242-250. https://doi.org/10.22159/ijap.2019v11i4.32281
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