FORMULATION AND EVALUATION OF FLOATING IN SITU GEL OF CIPROFLOXACIN
Objective: The objective of the study was to develop floatingÂ in situÂ gel formulations of Ciprofloxacin that has a narrow absorption window and mainly absorbed in the proximal areas of GIT. These formulations increases the targeted action on bacteria for a longer time that can be used in the treatment of Helicobacter pyloriÂ (H.Â pylori) infections and urinary tract infections.
Methods: In situ gel formulations were prepared by varying concentrations of sodium alginate asÂ in situÂ gel forming bio-degradable polymer and calcium carbonate as a cross-linking agent. The formulations were evaluated for Physical appearance, pH, in vitro drug release, viscosity, in vitro floating behaviour, in vitro gelling capacity and drug content. FTIR was conducted for Ciprofloxacin, excipients used and optimized formulation.
Results: All the formulations showed an optimum viscosity that will allow ease of administration and swallowing. Floating lag time of all formulations was between 32-70 seconds and floated for>12 h. The in vitro gelling capacity increased with increasing the polymer and gelling agent concentrations. Increase in polymer concentration decreased the rate and extent of the drug release. Among all the formulations, F4Â containing 4% w/v of sodium alginate and 4% w/v of calcium carbonate showed sustainedÂ in vitro drug release (95.6%) over an extended period of 12 h. FTIR studies revealed no interaction between drug and excipients used. Drug release from the formulations followed First order kinetics with Fickian diffusion.
Conclusion: Ciprofloxacin was successfully formulated as a pH-triggered floating in situÂ gelling system using sodium alginate.
2. Miyazaki S, Endo K, Kawasaki N, Kubo W, Watanabe H, Attwood D, et al. Oral sustained delivery of paracetamol from in situ gelling xyloglucan formulations. Drug Dev Ind Pharm 2003;29:113-9.
3. Peppas N, Langer R. New challenges in biomaterials. Science 1994;263:15-20.
4. Rajinikanth S, Mishra B. Floating in situ gelling systems of acetohydroxamic acid for clearance of H. pylori. J Drug Dev Ind Pharm 2008;34:577-87.
5. Lena MT. Formulation and evaluation of floating oral in-situ gel of metronidazole. Int J Pharm Pharm Sci 2014;6:265-9.
6. Naik SB, Venkateswarlu K, Chandrasekhar KB. Formulation and in vitro evaluation of orodispersible tablets of olanzapine for the improvement of dissolution rate. J Chem Pharm Res 2016;8:177-81.
7. Varshosaz J, Tavakoli N, Roozbahani F. Formulation and in vitro characterization of ciprofloxacin floating and bioadhesive extended-release tablets. Drug Delivery 2006;13:277-85.
8. Rao S, Ratnam BV. Formulation and optimization of sustained release tablets of rosuvastatin using HPMC K4M, HPMC K100M, and carrageenan. Int J ChemTech Res 2018;11:376-86.
9. Nelson JM, Chiller TM, Powers JH, Angulo FJ. Fluoroquinolone-resistant campylobacter species and the withdrawal of fluoroquinolones from use in poultry. Clin Infect Dis 2007;44:977-80.
10. Drlica K, Zhao X. DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev 1997;61:377-92.
11. Mulagada S, Baratam SR. Design and evaluation of ondansetron fast disintegrating tablets using natural polymers and modified starches as super disintegrants for the enhancement of dissolution. J Young Pharm 2017;9:519-24.
12. Maheswaran A, Padmavathy J, Nandhini V, Saravanan D, Angel P. Formulation and evaluation of floating oral in situ gel of diltiazem hydrochloride. Int J Appl Pharm 2017;9:50-3.
13. Patel MJ, Patel KR, Patel MR, Patel NM. Strategy for development of pH-triggered floating in-situ gel of levetiracetam. Am J Pharm Tech Res 2012;2:828-41.
14. Vipul V, Basu B. Formulation and characterization of the novel floating in-situ gelling system for controlled delivery of ramipril. Int J Drug Delivery 2013;5:43-55.
15. Rao BS, Vijayaratna J, Ramarao CT. Optimization of matrix tablets containing alfuzosin HCl employing HPMC K4M. Eur J Pharm Med Res 2016;3:529-33.
16. Thomas LM. Formulation and evaluation of floating oral in-situ gel of metronidazole. Int J Pharm Pharm Sci 2014;6:265-9.
17. Patel DM, Patel CN. Formulation and evaluation of floating oral in-situ gelling system of amoxicillin. ISRN Pharm 2011;1:1-8.
18. Baratam SR, V RatnaJ. Formulation and evaluation of floating matrix tablets of levofloxacin hemihydrate using hydroxyl-propyl methylcellulose k4m to treat Helicobacter pylori infection. Asian J Pharm Clin Res 2018;11:148-51.
19. Reddy RK, Srinivas M, Srinivas R. Once-daily sustained-release matrix tablets of nicorandil: formulation and in vitro evaluation. AAPS PharmSciTech 2003;4:480-8.
20. Hasan MJ, Kamal BA. Formulation and evaluation of ranitidine hydrochloride are floating In situ gel. Int J Pharm Pharm Sci 2014;6:401-5.
21. Nayak A, Maji R, Das B. Gastroretentive drug delivery system: a review. Asian J Pharm Clin Res 2010;3:1-10.