• Santosh Gada Jawaharlal Nehru Technological University, Kukatpally, Hyderabad, Telangana, India
  • ANANDKUMAR Y. V L College of Pharmacy, Raichur, Karnataka, India
  • C. MALLIKARJUNA SETTY Oxford College of Pharmacy, Bengaluru, Karnataka. India


Objective: The objective of the present study was to investigate the possibility of obtaining a controlled, relatively constant effective level of lamivudine microspheres.

Methods: Lamivudine loaded sodium alginate (SA) and tamarind mucilage(TM) mucoadhesive microspheres were prepared by ionic gelation technique with three different proportions of SA and TM with different concentrations of CaCl2. The prepared microspheres were evaluated for drug loading, particle size distribution, surface morphology, FTIR, in vitro wash off, in vitro release and stability studies.

Results: The microspheres were found to be free flowing having diameter ranging from 769.22 to 978.56 µm, drug encapsulation efficiency (DEE) was found to be 65.28 to 92.33%. Percent drug release after 12 h were ranging from 85±1.51 to 97±1.44. In vitro release profile of all formulations shows slow controlled release up to 12 h. In vitro wash off studies shown fairly good mucoadhesivity with 20% microspheres adhered after 6h. Stability studies showed that no significant change in particle size and maximum DEE in comparison to the formulation stored at room temperature.

Results: The lamivudine loaded SA-TM mucoadhesive microspheres can be conveniently prepared which showed better result and it may be used full for controlling the drug release and improve the bioavailability.

Keywords: Microspheres, Mucoadhesive, Tamarind, Mucilage, In vitro, Lamivudine

Author Biography

Santosh Gada, Jawaharlal Nehru Technological University, Kukatpally, Hyderabad, Telangana, India

Department of Pharmaceutics

Senior Assistant Professor


1. Velmurugana S, Ali MA. Preparation and evaluation of maraviroc mucoadhesive microspheres for gastro retentive drug delivery. Int J Pharm Pharm Sci 2015;7:208-14.
2. Abdul M, Rao AS, Martha S, Sirisha Y, Chandrika PU. Development of a floating multiple unit controlled-release beads of zidovudine for the treatment of AIDS. JOPR J Pharm Res 2012;6:78–83.
3. Biswal I, Dinda A, Das D, Si S, Chowdary KA. Encapsulation protocol for highly hydrophilic drug using non-biodegradable polymer. Int J Pharm Pharm Sci 2011;3:256–9.
4. Ma N, Xu L, Wang Q, Zhang X, Zhang W, Li Y, et al. Development and evaluation of new sustained-release floating microspheres. Int J Pharm 2008;358:82–90.
5. Basak SC, Kumar KS, Ramalingam M. Design and release characteristics of sustained release tablet containing metformin HCl. Br J Pharm Sci 2008;44:477–83.
6. Patel PN, Patel MM, Rathod DM, Patel JN, Modasiya MMK. Sustain release drug delivery: a theoretical prospective. J Pharm Res 2012;5:4165–8.
7. Raffin RP, Colome LM, Schapoval EES, Pohlmann AR, Guterres SS. Increasing sodium pantoprazole photostability by microencapsulation: Effect of the polymer and the preparation technique. Eur J Pharm Biopharm 2008;69:1014–8.
8. Zyazici M, Sevgi F, Ertan G. Micromeritic studies on nicardipine hydrochloride microcapsules. Int J Pharm 1996;138:25–35.
9. Dasari A, Velmurugana S. Formulation and evaluation of nevirapine mucoadhesive microspheres. Int J Pharm Pharm Sci 2015;7:342-8.
10. Deshmukh MT, Mohite SK. Preparation and evaluation of mucoadhesive microsphere of fluoxetine Hcl. Int J Pharm Sci Res 2017;8:3776-85.
11. Vasir JK, Tambwekar K, Garg S. Bioadhesive microspheres as a controlled drug delivery system. Int J Pharm 2003;255:13–32.
12. Chowdary KPR, Srinivas Rao S. Mucoadhesive microspheres and microcapsules: current status. Indian J Pharm Sci 2005;67:141–50.
13. Chowdary KR, Rao YS. Mucoadhesive microspheres for controlled drug delivery. Biol Pharm Bull 2004;27:1717–24.
14. Jain SK, Chourasia MK, Jain AK, Jain RK, Shrivastava AK. Development and characterization of mucoadhesive microspheres bearing salbutamol for nasal delivery. Drug Delivery 2004;11:113–22.
15. Yadav SK, Khan G, Bonde GV, Bansal M, Mishra B. Design, optimization and characterizations of chitosan fortified calcium alginate microspheres for the controlled delivery of dual drugs. Artif Cells Nanomed Biotechnol 2018;46:1180-93.
16. George M, Abraham TE. Polyionic hydrocolloids for the intestinal delivery of protein drugs: alginate and chitosan–a review. J Controlled Release 2006;114:1–14.
17. Smidsrod O, Draget KI. Chemistry and physical properties of alginates. Carbohydr Eur 1996;14:6–13.
18. El-menshawe SE, Kharshoum RM, Hamad DS, Halawa A. Effect of biodegradable copolymers and divalent cations on the sustained release ability of propranolol hydrochloride loaded biomaterial microspheres. Int J Pharm Pharm Sci 2016;8:311-7.
19. Kroll E, Winnik FM, Ziolo RF. In situ preparation of nanocrystalline?-Fe2O3 in iron (II) cross-linked alginate gels. Chem Mater 1996;8:1594–6.
20. Llanes F, Ryan DH, Marchessault RH. Magnetic Nanostructured composites using alginates of different M/G ratios as the polymeric matrix. Int J Biol Macromol 2000;27:35–40.
21. Gowda DV, Nawaz M, Vishnu DM. Design and evaluation of carboxymethyl tamarind kernel polysaccharide (cmtkp) controlled release spheroids/pellets and investigating the influence of compression. Int J Pharm Pharm Sci 2014;6:103-9.
22. Jana S, Lakshman D, Sen KK, Basu SK. Development and evaluation of epichlorohydrin cross-linked mucoadhesive patches of tamarind seed polysaccharide for buccal application. Int J Pharm Sci Drug Res 2010;2:193–8.
23. Jani GK, Shah DP, Prajapati VD, Jain VC. Gums and mucilages: versatile excipients for pharmaceutical formulations. Asian J Pharm Sci 2009;4:309–23.
24. Sahoo R, Sahoo S, Nayak PL. Release behavior of anticancer drug paclitaxel from tamarind seed polysaccharide galactoxyloglucan. Eur J Sci Res 2010;47:197–206.
25. Kulkarni D, Dwivedi AK, Sarin JPS, Singh S. Tamarind seed polyose: a potential polysaccharide for sustained release of verapamil hydrochloride as a model drug. Indian J Pharm Sci 1997;59:1–7.
26. Patel B, Patel P, Bhosale A, Hardikar S, Mutha S, Chaulang G. Evaluation of tamarind seed polysaccharide (TSP) as a mucoadhesive and sustained release component of nifedipinebuccoadhesive tablet and comparison with HPMC and Na CMC. Int J Pharm Tech Res 2009;1:404–10.
27. Anumolu PD, Anusha K, Mrudula Kiran A, Monika P, Sowndarya NSKR, Sunitha G. Liquid chromatographic quantification of ternary mixture of anti-viral drugs and application to assessment of their tablet dosage form. Int J Pharm Pharm Sci 2016;8:237-40.
28. Benjamin J Eckhardt, Roy M Gulick. Drugs for HIV infection. Infectious Diseases 2017;4:1293-308.
29. Charles F. Antiretroviral agents and treatment of HIV infection. Goodman and Gilman’s, The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2011. p. 1634-5.
30. Piliero PJ. Pharmacokinetic properties of nucleoside/ nucleotide reverse transcriptase inhibitors. J Acquir Immune Defic Syndr 2004;37:S2–S12.
31. Betty JD, Jennifer C. Human immunodeficiency virus infection-antiretroviral therapy. In: Richard AH, David JQ. editors. The textbook of therapeutics: drug and disease management. 8th ed. Philadelphia: Lippincott Williams and Wilkins; 2006. p. 2137-58.
32. Moyle G. Clinical manifestations and management of antiretroviral nucleoside analog-related mitochondrial toxicity. Clin Ther 2000;22:911-36.
33. Deveswaran R, Bharath S, Furtado S, Abraham S, Basavaraj BV, Madhavan V. Isolation and evaluation of tamarind seed polysaccharide as a natural suspending agent. Int J Pharm Biol Arch 2010;1:360-3.
34. Erik AR, Angelica RG, Raquel GR, Victor VG, Cesar PA. Rheological properties of tamarind (Tamarindusindica L.) seed mucilage obtained by spray-drying as a novel source of hydrocolloid. Int J Biol Macromol 2018;107:817-24.
35. Panda BB, Mohapatra S, Mallik S, Acharya P. Effect of tamarind seed mucilage on rheological properties: evaluation of suspending properties. Int Res J Pharm Sci 2010;1:8.
36. Gada SG, Anandkumar Y, Setty CM. Preparation and evaluation of zidovudine mucoadhesive microspheres. Eur J Pharm Med Res 2017;4:570-6.
37. Tavakol M, Ebrahim VF, Sameereh HN. The effect of polymer and CaCl2 concentrations on the sulfasalazine release from alginate-N, O-carboxymethyl chitosan beads. Prog Biomater 2013;2:10.
38. Obeidat WM, Price JC. Preparation and evaluation of Eudragit S 100 microspheres as pH-sensitive release preparations for piroxicam and theophylline using the emulsion-solvent evaporation method. J Microencapsul 2006;23:195-202.
39. Sharma M, Jain K, Dev SK, Choudhury PK. Formulation and evaluation of sodium alginate beads by emulsion gelation method. Asian J Pharm 2017;11:S101-6.
40. Maiti S, Dey P, Banik A, Biswanath S, Ray S, Kaity S. Tailoring of locust bean gum and development of hydrogel beads for controlled oral delivery of glipizide. Drug Delivery 2010;17:288–300.
41. Verma S, Kumar V, Jyoti, Mishra DN. Formulation, evaluation and optimization of mucoadhesive microspheres of acyclovir. Bull Pharm Res 2014;4:14-20.
42. Nagasree K, Chowdary GV, Kumar MCB, Reddy MTR, Bhikshapathi DVRN. Design and evaluation of sodium alginate microspheres loaded with gatifloxacin. Der Pharm Lett 2016;8:361-70.
43. Pal DK, Nayak AK. Novel tamarind seed polysaccharide-alginate mucoadhesive microspheres for oral gliclazide delivery: in vitro–in vivo evaluation. Drug Delivery 2012;19:123–31.
44. Sharma VK, Bhattacharya A. Release of metformin hydrochloride from Ispaghula-sodium alginate beads adhered on cock intestinal mucosa. Indian J Pharm Educ Res 2008;42:365–72.
45. Nayaka AK, Saquib MHS, Beg S, Alam MI. Mucoadhesive beads of gliclazide: design, development, and evaluation. Sci Asia 2010;36:319–25.
46. Princely S, Saleem BN, Nandhakumar S, Dhanaraju MD. Controlled delivery of antiretroviral drug-loaded cross-linked microspheres by ionic gelation method. Asian J Pharm Clin Res 2016;9:264-71.
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How to Cite
Gada, S., Y., A., & SETTY, C. M. (2019). PREPARATION, EVALUATION AND STABILITY OF LAMIVUDINE LOADED ALGINATE-TAMARIND MUCILAGE MICROSPHERES. International Journal of Applied Pharmaceutics, 11(4), 365-370.
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