FORMULATION AND CHARACTERISATION OF SUSTAINED RELEASE MICROBEADS LOADED WITH ZALTOPROFEN
Objective: The main aim of the present investigation was to formulate and evaluate microbeads of zaltoprofen. Zaltoprofen, a BCS class II drug used in the treatment of rheumatoid arthritis. Zaltoprofen has a shorter half-life of 2.8 h, and it is administered at a dose of 80 mg thrice a day. By encapsulating the drug into microbeads, it is expected that the release of the drug would be prolonged and thereby, it reduces the frequency of administration and better patient compliance may be improved.
Methods: Gellan-chitosan and calcium chloride beads of zaltoprofen were prepared employing ionotropic gelation method using different concentrations of gellan, chitosan, calcium chloride and zaltoprofen. The microbeads were evaluated for its various Physico-chemical parameters such as particle size determination, drug entrapment efficiency, infrared spectroscopy study, differential scanning calorimetry, X-ray diffraction analysis, scanning electron microscopy, in vitro drug release study and in vivo oral bioavailability studies.
Results: The results suggested that the batch FG-II exhibited higher drug entrapment efficiency (72.42±0.013), a sustained drug release for a period of 24 h. The pharmacokinetic profile of the drug from microbeads exhibited an enhanced oral bioavailability (2.4 times higher than that of pure drug), lower elimination rate (1.14 times lesser for the drug in microbeads) with prolonged elimination half-life (2.561 times higher than pure zaltoprofen).
Conclusion: Zaltoprofen entrapped microbeads demonstrated as a better delivery system for the sustained release of drug and also to circumvent the drawbacks associated with conventional therapy.
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 tartrate 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. Hirate K, Uchida A, Ogawa Y, Arai T, Yoda K. Zaltoprofen, a non-steroidal anti-inflammatory drug, inhibits bradykinin-induced pain responses without blocking bradykinin receptors. Neurosci Res 2006;54:288.
9. 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.
10. 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.
11. 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.
12. 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.
13. 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.
14. Sawyer M, Ratain MJ, Body surface area as a determinant of pharmacokinetics and drug dosing. Invest New Drugs 2001;19:171-7.
This work is licensed under a Creative Commons Attribution 4.0 International License.