SODIUM ALGINATEâ€“LOCUST BEAN GUM IPN HYDROGEL BEADS FOR THE CONTROLLED DELIVERY OF NIMESULIDE-ANTI-INFLAMMATORY DRUG
Keywords:Sodium alginate (NaAlg), Locust bean gum (LBG), Glutaraldehyde (GA) and nimesulide
Objective: The objective of this study was to formulate and evaluate the drug release studies using locust bean gum (LBG) and sodium alginate (NaAlg) and cross-linked with glutaraldehyde for the controlled release (CR) of nimesulide, an anti-inflammatory drug.
Methods: Locust bean gum (LBG) and sodium alginate (NaAlg) blend hydrogel beads were prepared by an extrusion method using glutaraldehyde as a crosslinker. Nimesulide an anti-inflammatory drug was encapsulation within LBG/NaAlg blend hydrogel beads. Morphology, size, encapsulation efficiency and drug release from these hydrogel beads were evaluated by different characterization techniques such as fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), x-ray diffraction (X-RD) studies.
Results: Drug-loaded hydrogel beads were analyzed by FTIR, which indicates the interaction between drug and polymers. DSC thermograms on drug-loaded microbeads confirmed the polymorphism of nimesulide and indicated a molecular level dispersion of the drug in the hydrogel beads. SEM confirmed the spherical nature and rough surface of the hydrogel beads produced. X-RD study was performed to understand the crystalline nature of drug after encapsulated into the hydrogel beads and confirmed the complete dispersion of the drug in the polymer matrix. In vitro release studies conducted in pH-7.4 which indicated a dependence of release rate on the amount of drug loading and the amount of LBG/NaAlg, but slow release rates were extended up to 48 h. The cumulative release data were fitted to an empirical equation to compute diffusion exponent (n) which indicated the non-fickian trend for drug release.
Conclusion: These results clearly demonstrated that the ability of these newly developed hydrogel beads containing nimesulide for its sustained release could possibly be advantageous to patient compliance with reduced dosing interval.
Tabata Y, Ikada Y. Synthesis of gelatin microspheres containing interferon. Pharm Res 1989;6:422-7.
Peppas N, Burns P, Leobandung W, Chikawa HI. Hydrogels in pharmaceutical formulations. Eur J Pharm Biopharm 2000;50:27-46.
Sperling LH. Interpenetrating polymer networks and related materials. Plenum Press: New York; 1981.
Dave AM, Mehta MH, Aminabhavi TM, Kulkarni AR, Soppimath KS. Review on controlled release of nitrogen fertilizers through polymeric membrane devices. Polym Plast Technol 1999;38:675-711.
Dong LC, Hoffman AS. A novel approach for the preparation of pH-sensitive hydrogels for enteric drug delivery. J Controlled Release 1991;15:141-52.
Peppas NA, Korsmeyer RW. Hydrogels in medicine and pharmacology, Boca Raton, FL: CRC Press; 1987.
Seigel RA, Firestone BA. Mechanochemical to self-regulating insulin pump design. J Controlled Release 1990;11:181-92.
Davis TP, Huglin MB. Effect of composition on properties of copolymeric N-Vinyl-2-pyrrolidone/methyl methacrylate hydrogels and organogels. Polymer 1990;31:513-9.
Desai NP, Hubbell JA. Surface physical interpenetrating networks of poly(ethylene terephthalate) and poly(ethylene oxide) with biomedical applications. Macromolecules 1992;25:226-32.
Khare AR, Peppas NA. Investigation of hydrogel water in polyelectrolyte gels using differential scanning calorimetry. Polymer 1993;34:4595-800.
Burugapalli K, Bhatia D, Koul V, Choudhary V. Interpenetrating polymer networks based on poly(acrylic acid) and gelatin, I: Swelling and thermal behavior. J Appl Polym Sci 2001;82:217-27.
Changez M, Koul V, Burugapalli K, Dinda AK. Studies on biodegradation and release of gentamicin sulphate from interpenetrating polymer networks hydrogels based on poly(acrylic acid) and gelatin: In vitro and in vivo. Biomaterials 2004;25:139-46.
Hijorth HT, Jan K. Alginate in drug delivery systems. Drug Dev Ind Pharm 2002;28:621â€“30.
Dey P, Maiti S, Sa B. Locust bean gum and its application in pharmacy and biotechnology: an overview. Int J Curr Pharm Res 2012;4:7-11.
Dea ICM, Morrison A. Chemistry and Interactions of seed galactomannans. Adv Carbohydr Chem Biochem 1975;31:242â€“312.
Davis R, Brogden RN. Nimesulide: an update of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy. Drugs 1994;48:431-54.
Meriani F, Coceani N, Sirotti C, Voinovich V, Grassi M. Characterization of a quaternary liquid system improving the bioavailability of poorly water-soluble drugs. J Colloid Interface Sci 2003;263:590-6.
Piel G, Pirotte B, Delneuveille I, Neven P, Delarge J. Study of the influence of both cyclodextrins and l-iysine on the aqueous solubility of Nimesulide: isolation and characterization of Nimesulide-L-Iysine-cyclodextrin complexes. J Pharm Sci 1997;86:475-80.
Ferreira SH. Role of interleukins and nitric oxide in the mediation of inflammatory pain and its control by peripheral analgesics. Drugs 1993;46:1-9.
Tognell S. New clinical opportunities. Drugs 1993;46:275-6.
Ravikumara NR, Madhusudhan B, Nagaraj TS, Hiremat SR, Raina G. Preparation and evaluation of nimesulide-loaded ethylcellulose and methylcellulose nanoparticles and microparticles for oral delivery. J Biomater Appl 2009;24:47-64.
Dutet J, Lahiani MS, Didier L, Jezequel S, Bounoure F, Barbot C. Nimesulide/cyclodextrin/PEG 6000 temary complexes: Physico-chemical characterization, dissolution studies and bioavailability in rats. J Inclusion Phenom Macrocyclic Chem 2007;57:203-9.
Singla AK, Chawla M, Singh A. Nimesulide: some pharmaceutical and pharmacological aspects and update. J Pharm Pharmacol 2000;52:467-86.
Paul AL, Hardman JG, Limbird LE, Molinoff PB, Ruddon WR, Gilman AG. editors. Goodman and Gilmanâ€™s The Pharmacological basis of therapeutics, chapter, Drugs Affecting Renal and Cardiovascular Function. 9th ed. New York: McGraw-Hill Companies. Inc: 1996. p. 644.
Lakshminarayana Reddy C, Yerriswamy B, Prasad CV, Subha MCS, Chowdojirao K. Control release of chlorpheniramine maleate through IPN beads of sodium alginate-g-methyl methacrylate. J Appl Polym Sci 2010;118:2342-9.
Madhusudana Rao K, Krishna Rao KSV, Ramanjaneyulu G, Chowdoji Rao K, Subha MCS, Chang-Sik Ha. Biodegradable sodium alginate-based semi-interpenetrating polymer network hydrogels for antibacterial application. J Biomed Mater Res 2014;102:3196-206.
Sudhakar K, Madhusudana Rao K, Mallikarjuna B, Prasad CV, Subha MCS, Chowdoji Rao K. Preparation and characterization of nimesulide loaded poly(methyl methacrylate)/poly(ethylene oxide) blend microspheres: in vitro release studies. Asian J Pharm 2013;7:118-24.
Kumarababu P, Maruthi Y, Veerapratap S, Sudhakar K, Rotimi Sadiku, Prabhakar MN, Jung Il Song, et al. Development and characterization of polycaprolactone (PCL)/poly ((r)-3-hydroxybutyric acid) (PHB) blend microspheres for tamoxifen drug release studies. Int J Pharm Pharm Sci 2015;7:95-100.
Siraj S, Sudhakar P, Sajankumarji Rao U, Sekharnath KV, Chowdoji Rao K, Subha MCS. Interpenetrating polymer network microspheres of poly (vinyl alcohol)/methyl cellulose for controlled release studies of 6-thioguinine. Int J Pharm Pharm Sci 2014;6:101-6.
Jain N, Kumar H, Rajpoot AK, Verma HC. Novel interpenetrating polymer network micro adhesive microspheres of locust bean gum and poly(vinyl alcohol) for the delivery of famotidine. MIT Int J Pharm Sci 2015;1:27-36.
Manjanna KM, Rajesh KS, Shiva Kumar B. Formulation and optimization of Natural polysaccharide hydrogel microbeads of aceclofenac sodium for oral controlled drug delivery. Am J Med Sci 2013;1:5-17.
Kajjari PB, Manjeswar LS, Aminabhavi TM. Nevel pH and temperature responsive blend hydrogel Microsphere of sodium alginate and PNIPAAm-g-GG for controlled release of isoniazid. AAPS PharmaSciTech 2012;13:1147-57.
Krishna Rao KS V, Vijaya Kumar Naidu B, Subha MCS, Sairam M, Aminabhavi T M. Novel chitosan-based pH sensitive interpenetrating network microgels for controlled release of cefadroxil. Carbohydr Polym 2006;66:333-44.
Patil P, Bhoskar M. Optimization and evaluation of spray dried chitosan nanoparticles containing doxorubicin. Int J Curr Pharm Res 2014;6:7-15.
Bajpai AK, Rajpoot M. Release and diffusion of sulfamethoxazole through acrylamideâ€“based hydrogel. J Appl Poly Sci 2001;81:1238-47.
Durgapal S, Mukhopadhyay S, Goswami L. Preparation, characterization and evaluation of floating microparticles of ciprofloxacin. Int J Appl Pharm 2017;9:1-8.
Jacobsen J. Buccal iontophoretic delivery of atenolol: HCl employing a new in vitro three-chamber permeation cell. J Controlled Release 2001;70:83-95.
Jana S, Gandhi A, Sheet S, Kumar Sen K. Metal ion-induced alginate-locust bean gum IPN microspheres for sustained oral delivery of aceclofenac. Int J Biol Macromol 2015;72:45-53.