SUSTAINED RELEASE MICROBEADS OF RITONAVIR: IN VITRO AND IN VIVO EVALUATION
DOI:
https://doi.org/10.22159/ijap.2019v11i4.33149Keywords:
Ritonavir, Gellan, Chitosan, Ionotropic gelation, Oral bioavailabilityAbstract
Objective: The main aim of the present investigation was to develop sustained release microbeads of ritonavir that has a shorter half-life (3-5 h) and requires twice a day administration. These formulations exhibit a sustained release of ritonavir that would expect to improve the therapy, better drug utilization, and patient compliance.
Methods: Gellan-chitosan and calcium chloride reinforced beads of ritonavir were prepared by ionotropic gelation method employing different concentrations of gellan, chitosan, calcium chloride and drug. The prepared beads were evaluated for various physicochemical 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 and in vivo bioavailability studies.
Results: From the results, formulation GC-II exhibited higher drug entrapment efficiency (79.65±0.012), higher swelling index, sustained drug release over a period of 24 h, increased oral bioavailability (2.07 times higher than that of pure drug) and decreased elimination rate (2.15 times lesser for ritonavir microbeads) with prolonged elimination half-life (2.15 times more than pure drug) as compared to pure drug.
Conclusion: Ritonavir microbeads have demonstrated as a better delivery system for the sustained release of the drug; which may in turn circumvent the drawbacks associated with the conventional therapy.
Downloads
References
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.
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.
Vaizoglu O, Speiser P. Intelligent drug delivery systems. Trends Pharmacol Sci 1982;3:28-30.
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.
Rajinikanth PS, Sankar C, Mishra B. Sodium alginate microspheres of metoprolol tartarate for intranasal systemic delivery. Drug Delivery 2003;10:21-8.
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.
Odeku OA, Lamprecht A, Okunlola A. Characterization and evaluation of four natural gums as polymers in the formulations of diclofenca sodium microbeads. Int J Biol Macromol 2013;58:113-20.
Prakash 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.
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.
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.
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.
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.
Sawyer M, Ratain MJ. Body surface area as a determinant of pharmacokinetics and drug dosing. Invest New Drugs 2001;19:171-7.
Published
How to Cite
Issue
Section
