FABRICATION AND EFFECT OF PROCESS VARIABLES OF SITAGLIPTIN MICROSPHERES
Â Objective: The study is to formulate and assess the effects of different variables on the release profile of sitagliptin microspheres.
Methods: The microspheres were prepared by emulsion-solvent diffusion method and ionotropic gelation method using ethyl cellulose and sodium alginate as the polymers, respectively. The formulations are optimized by applying 23 factorial design based on the drug-polymer ratio, stirring speed, and method of preparation.
Results: The drug-polymer interaction was checked by the Fourier-transform infrared spectroscopy and differential scanning calorimetry the results of which indicated no incompatibility. The formulated sitagliptin microspheres were evaluated for shape, morphology, particle size, the degree of swelling, encapsulation efficiency, in vitro drug release studies for 12 h, and kinetics of drug release.
Conclusion: The results showed that the drug-polymer ratio and stirring speed affected the particle size and drug release. The release of the drug was found to be sustained, and diffusion path is following cube root law of Hixson-Crowell kinetics. The batch F3 was found to be desirable and was further characterized by scanning electron microscope for morphology.
2. Patel A, Ray S, Thakur RS. In vitro evaluation and optimization of controlled release floating drug delivery system of metformin hydrochloride. Drug Deliv 2006;14:57-64.
3. Bardsley JK, Ratner RE. Sitagliptin: An oral agent for Glucose control. Expert Rev Endocrinol Metab 2008;3:691-7.
4. Sadashivaiah R, Dinesh BM, Patil UA, Desai BG, Raghu KS. Design and in vitro evaluation of haloperidol lactate transdermal patches containing ethyl cellulose-povidone as film polymers. Asian J Pharm 2008;2:43-9.
5. Chawla A, Sharma P, Pawar P. Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization, and in-vitro evaluation. Acta Pharm 2012;62:529-45.
6. Sahoo SK, Mallick AA, Barik BB, Senapathi PC. Formulation and in vitro evaluation of eudragit microspheres of stavudine. Trop J Pharm Res 2005;4:369-75.
7. Gupta R, Prajapati KS, Pattnaik S, Bhardwaj P. Formulation and evaluation of novel stomach specific floating microspheres bearing famotidine for treatment of gastric ulcer and their radiographic study. Asian Pac J Trop Biomed 2014;4:729-35.
8. Shruti R, Alpana R. Formulation and characterization of an intragastric floating drug delivery system of doxorubicin hydrochloride: In vitro-in vivo release study. Asian J Pharm Clin Res 2012;5:150-8.
9. Dang T, Cui Y, Chen YD, Meng XM, Tang PF, Wu JB. Preparation and characterization of colon-specific microspheres of diclofenac for colorectal cancer. Trop J Pharm Res 2015;14:1541-7.
10. Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanism of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25-35.
11. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of the rate of release of solid drug dispersed in the solid matrices. J Pharm Sci 1963;52:1145-9.
12. Ararath D, Velmurugan S. Formulation and evaluation of nevirapine mucoadhesive microspheres. Int J Pharm Pharm Sci 2015;7:342-8.
13. Sundar VD, Sathyamoorthy N, Madhuri M, Dhanaraju MD. Preparation and evaluation of ethyl cellulose microspheres of pioglitazone HCl for sustained drug delivery. Int J Pharm 2014;4:189-93.
14. El-Menshawe SF, Abdeltwab AM, Mohamed AI. Novel gastro-retentive polymeric microspheres: An approach for increased bioavailability and an once-daily dosing of terbutaline sulfate. Int J Pharm Pharm Sci 2016;8:320-9.
15. Raslan H K, Maswadeh H. In-vitro dissolution kinetic study of theophylline from mixed controlled release matrix tablets containing HPMC and glyceryl behenate. Ind J Pharm Sci 2006;68:308-12.
16. Sundar VD, Dhanaraju MD, Nandhakumar S. Preparation and characterization of anastrozole loaded magnetic poly (epsilon-caprolactone) microspheres for anticancer activity. Der Pharm Lett 2016;8:118-28.
17. Mazumder B, Sarkar MK, Dey S, Roy N. Effect of formulation and process variables on the characteristics of microspheres of an anti-viral drug prepared by a solvent evaporation technique. Int J Pharm Pharm Sci 2010;2:52-9.
18. Garud N, Garud A. Preparation and in-vitro evaluation of metformin microspheres using non-aqueous solvent evaporation technique. Trop J Pharm Res 2012;11:577-83.
19. Vinodbhai PK, Gohel MC, Parikh RK, Bariya S. Sustained release floating microspheres of Acyclovir: Formulation optimization and characterization and in-vitro evaluation. Int J Drug Dev Res 2011;3:242- 51.
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