American Journal of Medical Sciences and Medicine
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American Journal of Medical Sciences and Medicine. 2013, 1(1), 5-17
DOI: 10.12691/ajmsm-1-1-2
Open AccessArticle

Formulation and Optimization of Natural Polysaccharide Hydrogel Microbeads of Aceclofenac Sodium for Oral Controlled Drug Delivery

K.M. Manjanna1, , K. S. Rajesh2 and B. Shivakumar3

1Department of pharmaceutics, T.V.M.College of pharmacy, Bellary, India

2Department of pharmaceutics, Parul institute of pharmacy, Limda, India

3Department of pharmaceutical chemistry. B.L.D.E College of pharmacy, Bijapur, India

Pub. Date: February 15, 2013

Cite this paper:
K.M. Manjanna, K. S. Rajesh and B. Shivakumar. Formulation and Optimization of Natural Polysaccharide Hydrogel Microbeads of Aceclofenac Sodium for Oral Controlled Drug Delivery. American Journal of Medical Sciences and Medicine. 2013; 1(1):5-17. doi: 10.12691/ajmsm-1-1-2

Abstract

The objective of this study was to prepare and evaluate calcium alginate (CA) microbeads with calcium chloride as cross-linking agent for aceclofenac sodium by ionotropic external gelation method. Calcium alginate microbeads represent a useful tool for oral sustained/ controlled drug delivery but show several problems, mainly related to the stability, and rapid drug release at higher pH that, in most cases, is too fast due to increase porosity. To overcome such inconveniences, which was to develop CA microbeads coated with Guar gum (GG) and Locust bean gum (LBG) as drug release modifiers to improve stability and prolong the drug release. While increasing in the concentration of sodium alginate and other polymer dispersion increased size distribution, flow properties, mean particle size, swelling ratio and drug entrapment efficiency. The mean particle sizes of drug-loaded microbeads were found to be in the range 596.45±1.04 to 880.10±0.13. The drug entrapment efficiency was obtained in the range of 63.24±0.66 to 99.75±0.87. The shape and surface characteristics were determined by scanning electron microscopy (SEM). No significant drug-polymer interactions, physical changes and crystallinity of the drug in the formulations were determined by FT-IR spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction [XRD]. In-vitro drug release profiles of microbeads were pH dependent and were analyzed by different kinetic models. The mechanism of drug release from microbeads depends on swelling and erosion process resulting CA microbeads was diffusion controlled followed by First order kinetics and whereas CA microbeads coated with GG and LBG approaching to near Zero- order kinetics.

Keywords:
Sodium alginate aceclofenac sodium Natural polysaccharides Oral controlled drug delivery Zero-order kinetics

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References:

[1]  Kathleen parfitt and Martindale. The complete Drug reference part-I “Anti-inflammatory drugs and antipyretics” 32nd edn, Philadelphia Pharmaceutical Press,(1996) 1-11
 
[2]  Patric B. Deasy “Microencapsulation and related drug process” Drugs and pharmaceutical Science, 2nd edn, Marcel Dekker Inc, Newyork; (1984) 1-22.
 
[3]  Yie W. Chein. “Oral drug delivery and delivery systems” ,Novel drug delivery systems, 2nd edn Marcel Dekker- Inc, New-York,( 1992) 139
 
[4]  Covelo T, Matricardi P; Polysaccharide Hydrogels for modified release formulations. J.Control release (2007) 119; 5-24;
 
[5]  Peppas N.A, Bures P, Leobandung W, Ichikawa H; Hydrogels in pharmaceutical formulations, Eur J Biopharm. (2000) 50; 27-46
 
[6]  Hijorth HT, Jan K “Alginate in Drug Delivery Systems” Drug. dev. Ind. Pharm.(2002) 28;6; 621-630.
 
[7]  Grant, G.T.et,al, Biological interaction between polysaccharides and divalent cations: the egg-box model, FEBS, Letts; (1973) 32; 195-198;
 
[8]  Fernández-Hervás, M. J., Holgado, M. A., Fini, A. Fell, J. T. In vitro evaluation of alginate beads of a diclofenac salt. Int J Pharm, (1998) 163, 23-34.
 
[9]  Østberg, T., Lund, E. M. Graffner, C. Calcium alginate matrices for oral multiple unit administration. IV. Release characteristics in different media. Int J Pharm (1994). 112, 241-248.
 
[10]  Edith M, Mark R.K. “Microencapsulation” Encyclopedia of controlled release, I edn, Vol, II, Published by John Wiley and Sons Inc. London.(1999) 520-538;
 
[11]  Matricardi‌ P, (2001). Chiara DM , Tommasina C, Franco A Recent advances and perspectives on coated alginate microspheres for modified drug delivery; Exp opin drug deliv (2008) 5; 417-425
 
[12]  Tejal S, Chirag N, Tejal G, Chotal N.P. Development of Discriminating method for dissolution of aceclofenac marketed formulation. Dissolution Technologies. (2008) 5; 31-35
 
[13]  Thaned P and Satit P; Xanthan-alginate composite gel beads; Molecular interaction and in-vitro characterization. Int, J, Pharm; (2007) 331; 61-71.
 
[14]  Agnihotri S. A. and Aminabhavi T. M. Controlled release of clozapine through chitosan microparticles prepared by a novel method. J Control Release, (2004) 96, 245-259.
 
[15]  Malay K Das, Prakash CS. Evaluation of Furosemide loaded alginate microspheres prepared by ionotropic external gelation technique. Acta, pharm.drug Research; (2007) 64; 3; 253-262
 
[16]  Mishra B, Jayanth P, Mishra D.N. Sankar C Development of guar gum alginate based microcapsules of metranidazole for delivery to colon; Acta Pharmaceutica Turcica (2004) 46; 121-130
 
[17]  Deshmukh V.N, Sakarkar D.M Wakade RB Formulation and evaluation of controlled release alginate microspheres using locust bean gum; J Pharmacy Research (2009) 2; 42-49
 
[18]  Martin A, Swarbrick, J, and Cammarata, A. Micromeritics, Phsical Pharmacy, 4th edn, B.I. Waverly Pvt, Ltd, New-Delhi (1991) 760.
 
[19]  Dandagi P.M, Microencapsulation of Verapamil Hydrochloride by Ionotropic gelation technique, Ind. J. Pharm. Sci (2004) 66 ; 631-63.
 
[20]  Rajesh K.S., Khanrah A. Biswanath SA. Release of Ketoprofen from Alginate Microparticles Containing Film Forming polymers; J. Sci and Ind. Research; (2004) 62; 965-989;
 
[21]  Pornsak S, Ross AK. Development of polysaccharide coated pellets for oral administration: Swelling and release behavior of calcium pectinate gel. AAPS Pharma Sci Tech, (2007) 8 (3) 1-8.
 
[22]  Srinivas Mutalic, et, al Enhancement of dissolution rate and bioavailability of aceclofenac ; A chitosan based solvent change approach, Int. J. Pharm, (2008) 350;279-290
 
[23]  Matthews BR, Regulatory aspects of stability testing in Europe. Drug dev Ind Pharm (1999) 25;831-856
 
[24]  Sartori, C., Finch, D. S. Ralph, B. Determination of the cation content of alginate thin films by FTIR spectroscopy. Polymer, (1997) 38, 43–51.
 
[25]  Pralhad TT, Rajendra Kumar DK. Encapsulation of Water-Insoluble Drugs by a Cross-linking Technique, AAPS Pharm Sci; (2004) 6; 12; 1-8.
 
[26]  Rastogi R, Sultan Y, Aqil M. Alginate Microspheres of Isoniazid for Oral Sustained Drug Delivery, Int, J, Pharm, (2007) 334; 71-77.
 
[27]  Yotsuyanagi T, Ohkubo T, Ohhashi T, Ikeda Calcium induced gelation of alginic acid and pH-sensitive re-swelling of dried gels. Chem Pharm Bull (1987) 35;1555-1563
 
[28]  Sevgi T, Omer HO, Fusun A. Formulation and investigation of nicardipine HCl-alginate gel beads with factorial design-based studies. Euro, J. Pharma, Sci; (1998) 6; 241-246.
 
[29]  Bhardwaj T.R Kanwar M, Lal, M et al Natural gums and modified natural gums as sustained release carriers. Drug Dev. Ind. Pharm. (2000) 26: 1025-1038.
 
[30]  Raida. S. Controlling of systemic absorption of gliclazide through incorporation into alginate beads. J Microencapsulation (2007) 341; 230-237.
 
[31]  Rahman Z, Kanchan K, Roop KK, et al Characterization of 5-Florourocil Microspheres for colonic delivery , AAPS Pharm Sci Tech (2006); 7(2); E1-9
 
[32]  Roland Bodmeier, Omlaksana Paeratkul, “Spherical agglomerates of water insoluble drugs” J. Pharm. Sci, (1989) 78; 964-970.
 
[33]  Costa, P. Lobo, JMS. Modeling and comparison of dissolution profiles. Eur J Pharm Sci (2001). 13, 123-133.