Issue

Vol. 26 No. 9 (2014): Vol 26 Issue 9

Copyright (c) 2014 AJC

Creative Commons License

This work is licensed under a Creative Commons Attribution 4.0 International License.

Development of Microparticulate Sustained Release Dosage Form of Emtricitabine: An Anti-HIV Drug

https://doi.org/10.14233/ajchem.2014.15757
A. Fathima
School of Chemical and Biotechnology, SASTRA University, Thanjavur-613 401 India
B.N. Vedha Hari
School of Chemical and Biotechnology, SASTRA University, Thanjavur-613 401 India
D. Ramya Devi
School of Chemical and Biotechnology, SASTRA University, Thanjavur-613 401 India

Corresponding Author(s) : D. Ramya Devi

ramya@scbt.sastra.edu

Asian Journal of Chemistry, Vol. 26 No. 9 (2014): Vol 26 Issue 9

Abstract

Emtricitabine is a nucleotide reverse transcriptase inhibitor used for HIV infections, with oral bioavailability of 93 %. Microparticles loaded with emtricitabine were formulated through ionotropic gelation method using sodium alginate as retardant polymer and calcium chloride as cross linker. The concentration of hydroxy propyl methyl cellulose and sodium alginate were varied as 50-300 mg and 100-900 mg respectively using 32 factorial design. The prepared microparticles were evaluated for particle size distribution (322.66 to 553.40 μm), percentage yield (96.68-98.33 %) drug content (92.85-95.23%) and drug entrapment efficiency (27.41 to 52.44 %). The FT-IR spectroscopic analysis indicated the minimum drug polymer interaction during preparation. The stability and uniform dispersion of drug in the polymeric matrix was confirmed by DSC and XRD studies. The in vitro release profile indicated that increase in intensity of cross linking decreased the rate of drug release, with showed significant sustained release effect of the dosage form for more than 8 h.

Keywords

Emtricitabine Microparticles Sodium alginate Response surface methodology
Fathima, A., Vedha Hari, B., & Ramya Devi, D. (2014). Development of Microparticulate Sustained Release Dosage Form of Emtricitabine: An Anti-HIV Drug. Asian Journal of Chemistry, 26(9), 2604–2610. https://doi.org/10.14233/ajchem.2014.15757
Download Citation
Endnote/Zotero/Mendeley (RIS)
BibTeX
References
  1. N.P. Abhay, R.S. Sadhana and W.T. Mahesh, Int. J. Pharm. Res. Dev.,3, 99 (2011).
  2. M.N.V. Satheesh and K. Shivani, Int. J. PharmTech. Res., 3, 1242 (2012).
  3. D.L. Wise, Handbook of Pharmaceutical Controlled Release Technology,CRC Press, New York, p. 271 (2000).
  4. R. Langer and J. Folkman, Nature, 263, 797 (1976).
  5. S.D. Putney and P.A. Burke, Nat. Biotechnol., 16, 153 (1998).
  6. J. Moore, The Drug Delivery Outlook to 2005, Business Insights Ltd.,(1999).
  7. J. Siepmann, Prog. Colloid Polym. Sci., 15, 133 (2006).
  8. http://www.drugs.com/sfx/atripla-side-effects.html.
  9. P. Emillio, Archive of SID, 8, 125 (2008).
  10. J.E. Gallant, E. DeJesus, J.R. Arribas, A.L. Pozniak, B. Gazzard, R.E.Campo, B. Lu, D. McColl, S. Chuck, J. Enejosa, J.J. Toole and A.K. Cheng, N. Engl. J. Med., 354, 251 (2006).
  11. K.D. Malay and C.S. Prakash, Acta Polon. Pharm. Drug Res., 64, 253 (2007).
  12. C.M. Silva,A.J. Ribeiro, M. Figueiredo, D. Ferreira and F. Veiga, AAPS J., 7, 903 (2005).
  13. R.W.J. Lencki, R.J. Neufeld and T. Spinney, US Patent 4822534 (1989).
  14. K. Nilsson, S. Bimbaum, S. Flygare, L. Linse, U. Schroder, U. Jeppsson, P.O. Larsson, K. Mosbach and P. Brodelius, Eur. J. Appl. Microbial. Biotechnol., 17, 319 (1983).
  15. L.S.C. Wan, P.W.S. Heng and L.W. Chan, J. Microencapsul., 9, 309 (1992).
  16. V. Belgamwar, V. Shah and S. Surana, Curr. Drug Deliv., 6, 113 (2009).
  17. P. Venkatesan, R. Manavalan and K. Valliappan, J. Pharm Sci. Res., 1, 26 (2009).
  18. B.N. Vedha Hari, A. Brahma Reddy and B. Samyuktha Rani, J. Young Pharmacists, 2, 350 (2010).
  19. J. Luypaert, M.H. Zhang and D.L. Massart, Anal. Chim. Acta, 478, 303 (2003).
  20. S. Roy, S.G. Panpalia, B.C. Nandy, V.K. Rai, L.K. Tyagi, S. Dey and K.C. Meena, Int. J. Pharm. Sci. Drug Res., 1, 36 (2009).
  21. B.C. Gangadhar, R.S. Sunder, M.V. Vimal Kumar, M.S. Raju and M.S. Kiran, Int. J. Drug Discovery, 2, 8 (2010).
  22. L. Pachuau and B. Mazumder, Int. J. PharmTech Res., 1, 966 (2009).
  23. L. Pachuau, S. Sarkar and B. Mazumder, Trop. J. Pharm. Res., 7, 995 (2008).
  24. H. Eroglu, R. Alpar and L. Toner, J. Pharm. Sci., 33, 144 (2008).
  25. P.D. Chudiwal, P.L. Pawar, M.A. Nagaras and S.K. Mandlik, S.V. Pandya and P. Wakte, Int. J. PharmTech Res., 1, 1366 (2009).
  26. J. Shaji and A. Shinde, Int. Res. J. Pharm., 3, 166 (2012).
  27. G. Deshmukh, D. Ruikar, A.K.Seth, T. Ghelani, H. Patel, J. Patel and J. Patel, Pharm. Sci. Monitor: Int. J. Pharm. Sci., 2, 26 (2011).
  28. S.C. Jagdale, S.A. Ghorpade, B.S. Kuchekar and A.R. Chabukswar, Int. J. Pharm. Applications, 3, 181 (2011).
  29. A.V. Pande, U.A. Nimbalkar, M.V. Dhoka and P.A. Sonawane, Int. J. Res. Pharm. Chem., 1, 448 (2011).
  30. G. Singhvi and M. Singh, Int. J. Pharm. Studies Res., 2, 77 (2011).
  31. http://www.drugbank.ca/drugs/DB00879.
  32. I.A. Kartsonakis and G. Kordas, J. Am. Ceram. Soc., 93, 65 (2010).
  33. T. Phaechamud, A. Mesnukul and K. Yodkhum, Indian J. Pharm. Sci., 71, 413 (2009).
Read More
Author biographies is not available.
Download
PDF
Statistic
Read Counter : 0 Download : 0