FORMULATION AND IN VITRO EVALUATION OF OIL ENTRAPPED BUOYANT BEADS FOR STOMACH SPECIFIC DELIVERY OF METRONIDAZOLE
Keywords:
Floating beads, Metronidazole, Sunflower oil, In vitro drug release, Scanning electron microscopyAbstract
Objective: This work focused on the development of floating alginate beads for stomach specific delivery of Metronidazole towards the effective eradication of Helicobacter pylori, a major causative agent of peptic ulcers.
Methods: Different formulations of sunflower oil entrapped gel beads were prepared by emulsion gelation technique using sodium alginate as gelling agent. The prepared beads were evaluated for size, surface morphology, drug entrapment efficiency, in vitro floatuing and in vitro drug release properties.
Results: It was found that the percentage of oil plays an important role in controlling the floating of oil-entrapped alginate beads. All batches of beads floated for >24 hours with a very short lag time of 151–187 seconds. Scanning electron microscopy (SEM) revealed that the beads were spherical in shape with small pores on the surface. SEM of the cross section of the beads demonstrated minute oil globules throughout the inner portion of the beads confirming oil entrapment. The results clearly indicated that amount of polymer (% w/v) and amount of sunflower oil (% v/v) affected the bead size, floating, encapsulation efficiency and drug release of the beads. It was observed that the drug release kinetics was best fitted with the Higuchi model and drug release from the polymer matrix system was non fickian (anomalous transport) type.
Conclusion: The results provide evidence that formulated gel beads may be used to incorporate antimicrobials like Metronidazole and may be effective when administered locally in the stomach to cure Helicobacter pylori infection.
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References
Warren JR, Marshall B. Unidentified curved bacilli on gastric epithelium in active chronic gastritis. The Lancet 1983;321(8336): 1273–75.
Umamaheswari RB, Jain S, Tripathi PK, Agrawal GP, Jain NK. Floating-bioadhesive microspheres containing aceto hydroxamic acid for clearance of Helicobacter pylori. Drug Deliv 2002;9(4): 223–31.
Bayerdroffer E, Miehlke S, Mannes GA, Sommer A, Hochter W, Weingart J, et al. Double-blind trial of omeprazole and amoxicillin to cure Helicobactor pylori infection in patients with duodenal ulcers. Gastroenterology 1995;108(5):1412–7.
Bell GD, Powell KU, Burridge M, Spenceer G, Bolton G, Purser K, et al. Omeprazole plus antimalarial combination for the eradication of metronidazole-resistant Helicobactor pylori. Aliment Pharmacol Ther 1992;6(6): 751–8.
Choi BY, Park HJ, Hwang SJ, Park JB. Preparation of alginate beads for floating drug delivery system: effects of CO2 gas-forming agents. Int J Pharm 2002;239(1-2): 81-91.
Nagahara N, Akiyama Y, Nakao M, Tada M, Kitano M. Mucoadhesive Microspheres Containing Amoxicillin for Clearance of Helicobacter pylori. Antimicrob Agents Chemother 1998;42(10): 2492–4.
Cooreman MP, Krausgrill P, Hengels KJ. Local gastric and serum amoxicillin concentrations after different oral application forms. Antimicrob Agents Chemother 1993;37(7): 1506–9.
Badwan AA, Abumalooh A, Sallam E, Abukalaf A, Jawan O. A sustained release drug delivery system using calcium alginate beads. Drug Dev Ind Pharm 1985;11(2-3): 239-56.
Murata Y, Kofuji K, Kawashima S. Preparation of floating alginate beads for drug delivery to gastric mucosa. J Biomater Sci Polym Ed 2003;14(6): 581-8.
Stops F, Fell JT, Collett JH, Martini LG, Sharma HL, Smith AM. Citric acid pr longs the gastro-retention of a floating dosage form and increases bioavailability of riboflavin in the fasted state. Int J Pharm 2006;308(1-2): 14-24.