• Santosh Gada JNTU Hyderabad and KCT College of Pharmacy, Gulbarga, Karnataka India
  • ANANDKUMAR Y. Department of Pharmaceutics, V L College of Pharmacy, Raichur, Karnataka, India
  • C. MALLIKARJUN SETTY Department of Pharmaceutics, Oxford College of Pharmacy, Bengaluru, Karnataka, India




Lamivudine, Optimization, Drumstick, Sodium Alginate, Model fitting


Objective: The objective of this study was to design and evaluate controlled release mucoadhesive microspheres of lamivudine using mucoadhesive polymers and mucilage.

Methods: Mucoadhesive microspheres of lamivudine were formulated by ionic gelation method. The response surface methodology was adapted for optimization of formulation using central composite design (CCD) for two factors at three levels each was employed to study the effect of independent variables, Sodium alginate-drumstick mucilage (X1) and calcium chloride (CaCl2) concentration (X2) on dependent variables, namely drug encapsulation efficiency (DEE) and particle size (PS). Optimized drumstick mucilage mucoadhesive microspheres of lamivudine were obtained by using numerical optimization of desirability approach. The observed microspheres were coincided well with the predicted values by the experimental design.

Results: The microspheres formed were spherical in shape, and Particle size (PS) ranged between 681.63-941.57μm. Drug encapsulation efficiency (DEE) was ranged between 69.63-94.56 %. The drug release for an optimized formulation was 96.58 %. The mechanism of drug release from microspheres followed Korsemeyer’s-Peppas and exponential ‘n’ value was greater than 0.45, indicating the drug release was non-fickian i.e., swelling followed by erosion mechanism.

Conclusion: This work suggests that mucoadhesive microspheres, an effective drug delivery system for lamivudine, can be prepared using drumstick mucilage in improving the bioavailability of the drug.


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Hardenia A, Gupta AK. Development and optimization of gastroretentive mucoadhesive microspheres using 33 factorial design. Int J Pharm Sci Res 2016;7:2020-30.

Gedam S, Jadhav P, Talele S, Jadhav A. Effect of crosslinking agent on the development of gastroretentive mucoadhesive microspheres of risedronate sodium. Int J Appl Pharm 2018;10:133-40.

Panda S, Pattnaik S, Maharana L, Botta GB, Mohapatra P. Formulation and evaluation of zidovudine loaded olibanum resin microcapsules: exploring the use of natural resins as biodegradable polymeric materials for controlled release. Asian J Pharm Clin Res 2013;6:191-6.

Yoo SH, Song YB, Chang PS, Lee HG. Microencapsulation of ????-tocopherol using sodium alginate and its controlled release properties. Int J Biol Macromol 2006;38:25-30.

Sriamornsak P, Sungthongjeen S. Modification of theophylline release with alginate gel formed in hard capsules. AAPS Pharm Sci Tech 2007;8:E1-8.

Malakar J, Nayak Ak, Pal D. Development of cloxacillin loaded multiple-unit alginate-based floating system by an emulsion-gelation method. Int J Biol Macromol 2012;50:138-47.

Nayak AK, Khatua S, Hasnain MS, Sen KK. Development of alginate-PVP K30 microbeads for controlled diclofenac sodium delivery using central composite design. DARU J Pharm Sci 2011;19:356-66.

Han J, Zhou Z, Yin R, Yang D, JNie J. Alginate chitosan/hydroxyapatite polyelectrolyte complex porous scaffolds: preparation and characterization. Int J Biol Macromol 2010;46:199–205.

Patel YL, Sher P, Pawar AP. The effect of drug concentration and curing time on processing and properties of calcium alginate beads containing metronidazole by response surface methodology. AAPS Pharm Sci Tech 2006;7:E24-30.

Pal D, Nayak AK. Development, optimization, and antidiabetic activity of gliclazide-loaded alginate-methyl cellulose mucoadhesive microcapsules. AAPS Pharm Sci Tech 2011; 12:1431-41.

Llanes F, Ryan DH, Marchessault RH. Magnetic nanostructured composites using alginates of different M/Gratios as a polymeric matrix. Int J Biol Macromol 2000;27:35-40.

Pal D, Nayak Ak. Novel tamarind seed polysaccharide alginate mucoadhesive microspheres for oral gliclazide delivery: in vitro-in vivo evaluation. Drug Delivery 2012;19:123-31.

Borra SP, Eswaraiah MC, Reddy GK. Evaluation of different synthetic and natural polymers as a protective layer on highly soluble and high dose drug metoprolol succinate for manufacturing of control release multi-unit pellets tablets. Int J Appl Pharm 2018;10:69-76.

Panda D, Swain S, Gupta R, S Si, Kanungo SK. Preparation and evaluation of gels from gum of Moringa oleifera. Indian J Pharm Sci 2006;68:777-80.

Panda D, Choudhury NSK, Yedukondalu M, S Si, Gupta R. Evaluation of gum of Moringa oleifera as a binder and release retardant in tablet formulation. Indian J Pharm Sci 2008;70:614-8.

Katlama C, Valantin MA, Matheron S, Coutellier A, Calvez V, Diane D, et al. Efficacy and tolerability of stavudine plus lamivudine in treatment-naive and treatment-experienced patients with HIV-1 infection. Ann Intern Med 1998;129:525-31.

Princely S, Saleem Basha N, 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.

Furman PA, Fyfe JA, St Clair MH, Richards CA, Spector T. Phosphorylation of 3?-azido-3?-eoxythymidine and selective interaction of the 5?-triphosphate with human immunodeficiency virus reverse transcriptase. Proc Natl Acad Sci USA 1986;83:8333-7.

Moore KH, Barrett JE, Shaw S, Pakes GE, Churchus R, Kapoor A, et al. The pharmacokinetics of lamivudine phosphorylation in peripheral blood mononuclear cells from patients infected with HIV-1. AIDS 1999;13:2239-50.

Becher F, Landman R, Mboup S, Kane CN, Canestri A, Liegeois F, et al. Monitoring of didanosine and stavudine intracellular trisphosphorylated anabolite concentrations in HIV-infected patients. AIDS 2004;18:181-7.

Himadrisen, Surva Kumar J. Long-acting composition containing zidovudine and lamivudine. US patent publication US20050175694A1; 2005. p. 1-32.

Lewis GA, Matieu D, Phan-Tan-Lu R. Pharmaceutical Experiment Design, Marcel Dekker, New York, NY, USA; 1999.

Singh B, Kapil R, Nandi M, Ahuja N. Developing oral drug delivery systems using formulation by design: vital precepts retrospect and prospects. Expert Opin Drug Delivery 2011; 8:1341–60.

Singh B, Garg B, Chaturvedi SC, Arora S, Mandsaurwale R, Kapil R, et al. Formulation development of gastroretentive tablets of lamivudine using floating bioadhesive potential of optimized polymer blends. J Pharm Pharmacol 2012;64:654–69.

Singh B, Kumar R, Ahuja N. Optimizing drug delivery systems using systematic “design of experiments”, part I: fundamental aspects. Crit Rev Ther Drug Carrier Syst 2005;22:27-105.

Singh B, Dahiya M, Saharan V, Ahuja N. Optimizing drug delivery systems using systematic “design of experiments”, part II: retrospect and prospects. Crit Rev Ther Drug Carrier Syst 2005;22:215-94.

Joshi SA, Chavhan SS, Sawant KK. Rivastigmine loaded PLGA and PBCA nanoparticles: preparation, optimization, and characterization, in vitro and pharmacodynamic studies. Eur J Pharm Biopharm 2010;76:189–99.

Ashish, Singh RB. Nature of gum polysaccharide extracted from Moringa oleifera Lam. (Sainjna) plant. Adv Appl Sci Res 2014;5:1-3.

Chin CY, Jalil J, Ng PY, Ng SF. Development and formulation of Moringa oleifera standardised leaf extract film dressing for wound healing application. J Etnopharmacol 2018;212:188-199.

Prajapati SK, Tripathi P, Ubaidulla U, Anand V. Design and development of gliclazide mucoadhesive microcapsules: in vitro and in vivo evaluation. AAPS Pharm Sci Tech 2008;9:224-30.

Nayak AK, Pal D. Development of pH-sensitive tamarind seed polysaccharide-alginate composite beads for controlled diclofenac sodium delivery using response surface methodology. Int J Biol Macromol 2011;49:784-93.

Shaji J, Shah A. Optimization of tenoxicam loaded niosomes using quadratic design. Int J Curr Pharm Res 2016;8:62-7.



How to Cite

Gada, S., A. Y., and C. M. SETTY. “DRUMSTICK MUCILAGE MICROSPHERES FOR CONTROLLED RELEASE OF LAMIVUDINE: DESIGN, OPTIMIZATION AND IN VITRO EVALUATION”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 11, no. 4, Apr. 2019, pp. 60-68, doi:10.22159/ijpps.2019v11i4.30733.



Original Article(s)