Formulation and Evaluation of Microspheres for Colon Targeted Drug Delivery Using Anthelminthics Drugs
Abstract
The objective of this study was to develop sustained release microspheres for colon-targeted drug delivery system to enhance therapeutic efficacy while minimizing systemic side effects. The controlled and prolonged release of drugs in the colon can significantly improve the treatment outcomes for various colon-related diseases. Microspheres, small spherical particles with sizes ranging from 1 to 1000 micrometers, were formulated using biodegradable polymers and natural materials to ensure biocompatibility and controlled drug release. The formulation process involved the selection of appropriate polymers, such as poly lactic acid and polyglycolic acid, and the incorporation of the drug within the microspheres. Various techniques, including solvent evaporation, coacervation, and spray drying, were employed to prepare the microspheres with the desired drug-loading efficiency and particle size distribution.The formulated microspheres were extensively evaluated to assess their suitability for sustained release colon-targeted drug delivery. Evaluation parameters included drug encapsulation efficiency, particle size distribution, surface morphology and in vitro.In vitro drug release studies were conducted using simulated gastrointestinal fluids to mimic the conditions in the gastrointestinal tract. The sustained release microspheres exhibited controlled drug release over an extended period, specifically in the colon region. This sustained release profile was achieved by optimizing the polymer composition and formulation parameters, which allowed for the gradual degradation of the microspheres and subsequent release of the drug.
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References
2. Leuva VR, Patel BG, Chaudhary DJ, Patel JN, Modasiya MMK. Oral colon-specific drug delivery system. J Pharm Res. 2012;5(4):2293–7.
3. Kumar M, Ali A, Kaldhone P, Shirode A, Kadam VJ. Report on pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Res. 2010;3(3).
4. Philip AK, Philip B. Colon targeted drug delivery systems: a review on primary and novel approaches. Oman Med J. 2010;25(2):79–87.
5. VyasSP,KharRK.Gastro retentive systems. In: VyasSP,KharRK,editors. Controlled drug delivery: concepts and advances. New Delhi, VallabhPrakashan,2005;218-253.
6. Vinaykumar K.V, Sivakumar T, Tamizhmani T. Colon targeted drug delivery system: A review on recent approaches, Int J Pharm Biomed Sci 2011, 2(1), 11-19.
7. TarakJayraj Mehta et al., Need of colon specific drug delivery system: Review on primary and novel approaches, Int J Pharm Research Dev 2011, 3(1), 134-153.
8. Sangeetha G, Begum J M, Reddemma S, Rajendra Y, Colon targeted drug delivery system:A review, International Journal of Pharmacy& Technology. 2011;3(4):1657-72
9. Coupe AJ, Davis SS, Wilding IR. Variation in gastrointestinal transit of pharmaceutical dosage forms in healthy subjects. Pharm Res. 1991;8(3):360–4.
10. Jain NK, Controlled and Novel drug delivery, 04 Edition, CBS Publishers New Delhi, India; 21, 236-237.
11. Thakur D, M.pharm, presentation on introduction, advantage, disadvantage, and ideal properties of microsphere, slideshare. Published on Oct 17, 2016.
12. Sree Giri P B, Gupta V.R.M, Devanna N, Jayasurya K. Microspheres as drug delivery system - A review. JGTPS. 2014; 5(3):1961 -72.
13. Ghulam M., Mahmood A., Naveed A., Fatima R.A., Comparative study of various microencapsulation techniques. Effect of polymer viscosity on microcapsule charecterestics, Pak.J.Sci. 2009; 22(3):291-300.
14. Li, S.P., Kowalski C.R., Feld K.M., Grim W.M., Recent Advances in Microencapsulation Technology and Equipment, Drug Dev Ind Pharm. 14, 1988, 353-376. https://doi.org/10.3109/03639048809151975
15. Alagusundaram. M, Madhu SudanaChetty.C, Umashankari.K, Attuluri Venkata Badarinath, Lavanya.C and Ramkanth.S. Microspheres as a Novel Drug Delivery System - A Review. International Journal of ChemTech Research. 2009; 1(3):526-534.
16. Kushwaha N, Jain A, Jain PK, Khare B, Jat YS, An Overview on Formulation and Evaluation Aspects of Tablets. Asian Journal of Dental and Health Sciences 2022; 2(4):35-39
17. Bodmeier R, Chen H. Preparation and characterization of microspheres containing the anti- inflammatory agents, indomethacin, ibuprofen and ketoprofen. Journal of controlled release. 1989; 10(1989):167-175
18. Gavhane P, Deshmukh M, Khopade AN, Kunjir VV, Shete RV. A review on microsphere. Journal of Drug Delivery and Therapeutics. 2021 Jan 15; 11(1):188-94
19. Bijaya G., Laboratory Manual for Pharmaceutical Technology and Biopharmaceutics Experiments.

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