FORMULATION AND EVALUATION OF NOVEL IN SITU GEL OF LAFUTIDINE FOR GASTRO RETENTIVE DRUG DELIVERY

Sindhoor S M; Sneh Priya; Amala Maxwell

doi:10.22159/ajpcr.2018.v11i8.25582

Authors

Sindhoor S M Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Deralakatte, Mangalore â€‘575 018, Karnataka, India.
Sneh Priya Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Deralakatte, Mangalore â€‘575 018, Karnataka, India.
Amala Maxwell Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Deralakatte, Mangalore â€‘575 018, Karnataka, India.

DOI:

https://doi.org/10.22159/ajpcr.2018.v11i8.25582

Keywords:

Lafutidine, Gastroretentive in situ gel, pH-triggered gelation

Abstract

Objective: The aim of the present study was to formulate and evaluate the novel in situ gel of lafutidine for gastroretentive drug delivery

Methods: A gastroretentive in situ gel of lafutidine was formulated by pH-triggered ionic gelation method using different concentrations of gelling polymer such as sodium alginate, gellan gum, and xanthum gum. Prepared formulations were evaluated for viscosity, density, buoyancy lag time and buoyancy duration, and drug content. In vitro drug release studies of all formulations were also performed. In vivo fluorescence imaging study was conducted for optimized formulation and compared with control.

Results: The concentration of gelling agents and release retardant polymers significantly affected viscosity, floating behavior, and in vitro drug release of the formulations. The pH and drug content were found in the range of 6.72â€“7.20 and 88.74â€“95.33%, respectively. Floating lag time was <2 min; duration of floating was more than 12 h. Minimum and maximum in vitro drug release were found to be for formulation F9 (51.74%) and F1 (82.76%), respectively, at the end of 12 h. The drug was released from the all the formulations in a sustained manner. In vivo studies confirmed the gastroretention of the formulation in mice stomach for 8 h. Stability studies indicated that the there was no significant change in the visual appearance, floating behavior, and drug content.

Conclusion: The gastroretentive in situ gel system, prolonged the gastric residence time, thereby targeting site-specific drug release in the upper gastrointestinal tract.

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References

Madan JR, Adokar BR, Dua K. Development and evaluation of in situ gel of pregabalin. Int J Pharm Investig 2015;5:226-33.

Rohith G, Bhimagoni KS, Anegundha S. Floating drug delivery of a locally acting H2 antagonist: An approach using an in situ gelling liquid formulation. Acta Pharm 2009;59:345-54.

Shah J, Shah S, Upadhyay P, Parikh D. In situ gel: A novel approach of gastroretentive drug delivery. Asian J Biomed Pharm Sci 2012;2:1-8.

Thomas LM. Formulation and evaluation of floating oral in-situ gel of metronidazole. Int J Pharm Pharm Sci 2014;6:265-9.

Hasan MJ, Kamal BA. Formulation and evaluation of ranitidine hydrochlorideas floating in situ gel. Int J Pharm Pharm Sci 2014;6:401 5.

Swathi G, Lakshmi PK. Design and optimization of hydrodynamically balanced oral in situ gel of glipizide. J Appl Pharm Sci 2015;5:31-8.

Satish HP, Gokul ST. Formulation development and in vitro and in vivo evaluation of gastroretentive floating drug delivery system of lafutidine. Asian J Pharm 2013;7:68-74.

Sharma YR. Elementary Organic Spectroscopy. 4th ed. New Delhi: S. Chand; 2007.

Parthiban S, Shivaraju, Senthilkumar GP, Vikneswari A. Formulation and evaluation of gastroretentive drug delivery of ornidazole in situ gellingsystem using gellan gum. Int J Res Pharm Nano Sci 2013;2:747-56.

Jayswal BD, Yadav VT, Patel KN, Patel BA, Patel PA. Formulation and evaluation of floating in situ gel based gastro retentive drug delivery of cimetidine. Int J Pharm Res Scholars 2012;1:327-37.

Patel RP, Ladani R, Dadhaniya B, Prajapathi BG. In situ gel delivery systems for chlordiazepoxide using artificial neural network. Int J Pharm Health Sci 2015;1:10-22.

Pandya K, Agarwal P, Dashora A, Sahu D, Garg R, Pareta KL, et al. Formulation and evaluation of oral floatable in situ gel of ranitidine hydrochloride. J Drug Del Ther 2013;3:90-7.

Parekh KS, Shah KV. Formulation development and evaluation of oral in situ floating gel of domperidone. Int J Pharm Sci 2013;4:228-46.

Gulecha BS, Shahi S, Lahoti SR. Floating in situ gelling drug delivery system of verapamil hydrochloride. Am J Pharm Tech Res 2012;2:955 69.

Wamorkar V, Varma MM, Manjunath SY. Formulation and evaluation of Stomach specific in situ gel of metaclopramide using natural, biodegradable polymers. Int J Res Pharm Biomed Sci 2011;2:193-201.

Singhvi G, Singh M. Review: In vitro drug release characterization models. Int Pharm Sci Res 2011;2:77-84.

Dash A, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Poloniae Pharm Drug Res 2010;67:217-23.

Teng L, Wang D, Zhao J, Liu X, Sun F, Zhou L, et al. Parenteral thermo-sensitive organogel for schizophrenia therapy. Eur J Pharm Sci 2014;60:40-8.

WHO-GMP and ICH Stability Testing Guidelines for Drug Products. The Pharmaceutical Sciencesâ€“Pharma Pathway; 2.72-2.79.