Volume : 12, Issue : 04, April – 2025

Title:

FORMULATION AND IN VITRO EVALUATION OF SUSTAINED RELEASE MICROSPHERE UTILIZING AN ANTIEMETIC DRUG AS A MODEL COMPOUND

Authors :

Afreen Kauser

Abstract :

Tropisetron is an antagonist of the 5-HT3 (5-hydroxytryptamine3) receptor employed to avert nausea and vomiting generated by chemotherapy. The microspheres containing ethyl-cellulose, sodium alginate, and HPMC K15M were effectively synthesized by the ionic gelation method. All formulations were assessed based on many criteria including particle size analysis, drug content, drug entrapment efficiency, compatibility evaluation, in vitro dissolution testing, release kinetics analysis, and stability assessment. The synthesized microspheres exhibited excellent spherical morphology with a smooth surface, and their particle size was assessed using optical microscopy, revealing a consistent size distribution across all batches. The in vitro dissolution investigations indicated that the Tropisetron microspheres formulation TM10 exhibited superior sustained release characteristics for a duration of 12 hours, incorporating 30% of each of the three polymers. The release mechanism was ascertained by applying various kinetic equations, including zero-order, first-order, Higuchi model, and Korsmeyer-Peppas, and analyzing the R² values; the current study revealed that the optimal formulation exhibited zero-order release kinetics, with the drug release mechanism characterized by anomalous diffusion combined with erosion. The findings of the present study unequivocally demonstrate the promising potential of tropisetron microspheres as a viable alternative to traditional dosage forms, effectively meeting patient requirements with a once-daily administration.
Keywords: Tropisetron, Microsphere, Ethyl cellulose, Sodium alginate, HPMC K15M,

Cite This Article:

Please cite this article in press Afreen Kauser et al., Formulation And In Vitro Evaluation Of Sustained Release Microsphere Utilizing An Antiemetic Drug As A Model Compound .,, Indo Am. J. P. Sci, 2025; 12(04).

Number of Downloads : 10

References:

1. Harris D, Fell JT, Sharma HL, Taylor DC: GI transit of potential bioadhesive formulations in man: a scintigraphic study. Journal of Controlled Release 1990; 12(2):45–53.
2. Sunil, Vinay K, Pavan P, Mohan Jagan S, Madhusudan Rao Y: Formulation of eplerenone mini tablets – a novel approach in designing sustained release matrix tablets. Journal of global pharma technology 2011; 09:15-21.
3. Vyas SP, Khar RK. Essentials of Controlled Drug Delivery, 1st ed. 2002:417- 457. 4. Widder KJ, Sanyci AE, Ovadia H, Paterson PQ. Clinical Immunopathology 1979; 14:395.
4. Nair R, Reddy B, Kumar C, Kumar K, Application of Chitosan microspheres as drug carrier: A Review, Journal of Pharmaceutical Science & Research 2009;12 :1-12.
5. Shu XZ, Zhu KJ. A novel approach to prepare Tripolyphospate chitosan complex beads for controlled release drug delivery. International Journal of Pharmacy 2000; 20(1):51-58.
6. Kibbe, A.H., 2003 ed. Handbook of Pharmaceutical Excipients. American Pharmaceutical Association & Pharmaceutical Press: Washington, DC & London, UK.
7. Brahmankar DM, Jaiswal SB. Biopharmaceutics and Pharmacokinetics a Treatise. 1st ed. New Delhi: Vallabh Prakashan; 1995.
8. Begum, S., Panda, N., & Praveena, C. (2025). Design Characterization Optimization Of Lenalidomide-Loaded Bovine Serum Albumin Nanoparticles For Myeloma Therapy. International Journal of Applied Pharmaceutics, 18(1). https://doi.org/10.22159/ijap.2026v18i1.55623
9. Griffiths, P.; de Hasseth, J.A. (18 May 2007). Fourier Transform Infrared Spectrometry (2nd ed.). Wiley-Blackwell. ISBN 0471194042.
10. Wunderlich, B. (1990). Thermal Analysis. New York: Academic Press. pp. 137–140. ISBN 0-12-765605-7.
11. Using Quality by Design (QbD) in Designing Efficient, FDA Compliant Pharmaceutical Manufacturing Processes and FacilitiesWhat is the Impact? by Russ Somma, Ph.D.SommaTech, LLC.
12. Biostatistics A Methodology for the Health Sciences Second Edition Gerald Van Belle, Lloyd D. Fisher, Patrick J. Heagerty, Thomas Lumley. A John Wiley & Sons, Inc., Publication.
13. Panda, N.; Jena, S.; Kumar, P.R.; Pradhan, M.A.; Satpathy, P.R.; Mishra MM, C. Evaluation and Characterization of Bioadhesive Drug Delivery Systems. J. Pharm. Negat. Results 2023, 14, 39–46.
14. Panda N, Charan Panda K, Reddy AV, Reddy GVS. Process optimization, formulation and evaluation of hydrogel {guar gum-g-poly(acrylamide)} based doxofylline microbeads. Asian J Pharm Clin Res. 2014 Jul 1;7(3):60-5.
15. Panda N, Reddy AV, Reddy GV, Sultana A. Formulation design and in vitro evaluation of bilayer sustained release matrix tablets of doxofylline. Int J Pharm Pharm Sci. 2015;7(10):74–83.
16. Panda N, Reddy AV, Reddy GVS, Panda KC, Formulation, design and in vitro evaluation of zolmitriptan immediate release tablets using Primojel and Ac-Di-Sol. J. Pharm. Sci. Res. 2015, 7, 545–553
17. Panda N, Reddy AV, Reddy GVS, Sultana A. Formulation design and in vitro evaluation of bilayer sustained release matrix tablets of doxofylline. Int J Pharm Pharm Sci 2015;7:74-83
18. Akbar M, Panda N, Reddy AV.Formulation and evaluation of doxofylline sublingual tablets using sodium starch glycolate and crosscarmellose sodium as superdisintegrant. Int. j. pharm. res. allied sci 2015; 4(2):90-100
19. Panda N, Sultana A, Reddy AV, Reddy GVS and Ansari MS. Formulation Design and Study the effect of Polyplasdone-XL and AC-Di-Sol on Release Profile of Doxofylline Immediate Release Tablets. International Journal of Pharmaceutical Sciences Review & Research 2015; 32: 67- 76.
20. Panda N, Vurathi S, Vakkalagadda RK, Formulation Design and Characterization of Pitavastatin Calcium Lipid-Based Solid Self-Emulsifying Delivery System, Journal of Clinical Otorhinolaryngology, Head, and Neck Surgery, 27 (1), 2023. 998-1008.
21. Panda N, Reddy V, Reddy G, Panda K. Effect of different grades of hpmc and eudragit on drug release profile of doxofylline sustained release matrix tablets and IVIVC studies. Int Res J Pharm. 2015;6:493–504.
22. Dandagi PM, Manvi FV, Gadad AP, Mastiholimath VS, Patil MB, Balamuralidhara V. Micro encapsulation of Verapamil hydrochloride by ionotropic gelation technique. Indian Journal of Pharmaceutical Sciences 2004; 66(5):631-635.
23. Ramchandran S, Nandhakumar N, Dhanaraju M.D. Development and in vitro evaluation of biodegradable chitosan microspheres loaded with ranitidine and cross linked with Glutaraldehyde. International journal of pharm tech research 2011; 1:488-496.
24. Thanoo BC, Sunny MC, Jayakrishnan A. cross linked chitosan microspheres preparation and evaluation as a matrix for the controlled release of pharmaceutics. Journal of Pharmacy and Pharmcology 1992; 44:283.
25. Kyonghee Park, Goo Young Jung, Myong-ki kim. Triptorelin acetate-loaded poly (lactide-co-glycolide) (PLGA) microspheres for controlled drug delivery. Macromolecula Research 2012; 20: 847-51.
26. N.Thejaswi, Prathima Srinivas, Sadanandam M., Sumit Shah. Preparation and characterization of Goserelin acetate loaded microspheres. International Journal of pharmacy and pharmaceutical science 2013; 5 suppl 1: 184-89.
27. Raju.T, Santhosh Kumar.J, Ravindra Babu D.S, Arvind G. Formulation and Evaluation of Cytarabin PLA microspheres. International Journal of pharmacy and pharmaceutical science 2013; 5 suppl 1: 87-93.
28. Yi-Yan Y, Tai-Shung C, Xin-Lia B. Effect of preparation condition on morphology and release of biodegradable polymeric microspheres containing protein fabricated by double-emulsion method. Chemical Engineering Sci 2000; 55: 2223-26.
29. Rajesh P, Jolly RP, Iieena Soni, Kishor NK. Poly (D,L- Lactide-coGlycolide) microspheres containing 5-Fluorouracil: Optimization of process parameters. AAPS 2003; 4:1-8.
30. Yoon Yeo and Kiran Park. Control of encapsulation efficiency and initial burst in polymeric microparticles systems. Arch Pharm. Res 2004; 1:1-12.
31. Igartua M, Hernandez RM, Esquisabel A. Influence of formulation variables on the in-vitro release of albumin from biodegradable microparticulate systems. J. Microencapsulation 1997; 14:349-56.
32. Sah HK, Toddywala R, Chein YW. Biodegradable microcapsules prepared by a w/o/w technique: effect of shear force to make a primary w/o emulsion on their morphology and protein release. J. Microencapsulation 1993; 12: 59-69.