Design, evaluation and optimization of microcapsules of leflunomide with Eudragit® RL100 and Eudragit® RS. 100 by solvent evaporation technique

Rabindranath Pal, Bijan Kumar Gupta, Manas Chakraborty, Rabindra Debnath

Abstract


Leflunomide, an immune modulatory prodrug that is rapidly converted to its active metabolite possibly in the gut wall, plasma and in the liver was microencapsulated by the solvent evaporation technique using a nonaqueous solution of polymethacrylate polymer to achieve its release from the microcapsules at a slower rate. At the optimal condition of process
variables such as stirring speed, temperature of the medium, drug polymer ratio and ratio of light liquid paraffin and heavy liquid paraffin, maximum encapsulation efficiency was obtained. These microspheres were free-flowing in nature, discrete and uniform spherical in size, as evident by scanning electron microscopy. The in vitro release experiments were carried out in the simulated intestinal fluid (pH 7.2 phosphate buffer) using united States Pharmacopoeia (USP) XXII apparatus II. The data obtained from the dissolution profiles were compared using different kinetics models and the regression coefficients
were compared.


Full Text:

PDF

References


Bianco D, Hardy RM. Treatment of Evans’ syndrome with human

intravenous immunoglobulin and leflunomide in a diabetic dog.

J Am Anim Hosp Assoc 2009;45:147-50.

Jacckson RL, Morrow JD. Analgesic-antiptretic and antiinflammatory

agents and treatment of gout. In: Joel GH, Lee EL, editors. Goodman

and Gilman’s The Pharmacological Basis of Therapeutics, 11th ed.

New Delhi: McGraw Hill; 2005. p. 1415.

Bhalerao SS, Lalla JK, Rane MS. A study of electro kinetic and stability

property of suspension of diltiazem hydrochloride micro spheres.

Indian Drugs 2001;38:464-7.

Yeo Y, Park K. Characterization of reservoir-type microcapsules made

by the solvent exchange method. AAPS Pharmscitech 2004;5:52.

Fery A, Dubreuil F, Mohwal H. Mechanics of artificial microcapsules.

New J. Phys. Doi:10.1088/1367-2630/6/1/018.

Trapani A, Laquintana V, Denora N, Lopedota A, Cutrignelli A, Franco M,

et al. Eudragit RS. 100 microparticles containing 2-hydroxypropyl-b-

cyclodextrin and glutathione: Physicochemical characterization, drug

release and transport studies. Eur J Pharma Sci 2007;30:64-74.

Tirosh B, Baluom M, Nassar T, Friedman M, Abraham R. The effect of

Eudragit RL-100 on the mechanical and mucoadhesion properties of

polycarbophil dosage forms. J Control Release 2007;45:57-64.

Basu SK, Adhiyaman R. Preparation and characterization of

nitrendipine‐loaded Eudragit RL 100 microspheres prepared by an

emulsion-solvent evaporation. Trop J Pharma Res 2008;7:1033-41.

Chowdary KP, Ramesh KV. Studies on micro capsulation of diltiazem.

J Pharm Sci 1993;55:52-4.

Baidya S, Bedi S, Gupta BK. Design and evaluation of microcapsules of

diltiazem hydrochlodide. Boll Chim Farmac Anno 2001;14:l.

USPXXII. The United States Pharmacopoeia, United States Pharma

copoeia Convention INC. Rockville:2002. p. 449.




DOI: http://dx.doi.org/10.22377/ajp.v3i4.285

Refbacks

  • There are currently no refbacks.