Optimization and Evaluation of In situ Nasal Gel of Donepezil Hydrochloride


  • Pallavi M. Chaudhari Department of Pharmaceutics, Dr. D. Y. Patil College of Pharmacy, Pune, Maharashtra, India




Factorial design, In situ gel, Nasal route, Poloxamer 407, Tragacanth


Introduction: The nasal route has been explored as a route of administration, due to the benefits it offers. The formulation in the form of in situ gel has been utilized for the local and systemic effect. This type of formulation first exists in sol form, but once they are administered, it undergoes gelation to form gel, and this approach can be used for successful drug delivery system. Methods: Thus, in the present study, formulation of in situ gel for nasal administration for donepezil hydrochloride (HCL), by the use of 32 factorial designs, to improve its nasal bioavailability, was developed by increasing its nasal retention time and arrive at an optimized formulation. The formulation was developed by the use of cold method, by incorporation of thermoreversible polymer poloxamer 407 and mucoadhesive agent tragacanth. The in situ gel was later evaluated for different parameters such as pH, gelation time gelation temperature, gel strength, drug content, mucoadhesion, viscosity, in vitro drug diffusion, and stability. Results: Based on results obtained, F5 formulation was found to be optimum. The concentration of 22.5% Poloxamer 407 with 0.07% tragacanth showed promising nasal drug delivery system for donepezil HCl, with enhanced residence time due to increase in viscosity and mucoadhesion characteristics. Conclusion: The use of in situ gel formulation thus can effectively and safely improve the nasal residence time and absorption of donepezil HCl.


Download data is not yet available.


Gu F, Fan H, Cong Z, Li S, Wang Y, Wu C. Preparation, characterization, and in vivo pharmacokinetics of thermo sensitive in situ nasal gel of Donepezil hydrochloride. Acta Pharm 2020;70:411-22.

Yang Z. Enhanced brain distribution and pharmacodynamics of rivastigmine by liposomes following intranasal administration. Int J Pharm 2013;452:344-54.

Hanson R, Frey W. Intranasal delivery bypasses the blood-brain barrier to target therapeutic agents to the central nervous system and treat neurodegenerative disease. BMC Neurosci 2008;9:S5.

Horvát S. Sodium hyaluronate as a mucoadhesive component in nasal formulation enhances delivery of molecules to brain tissue. Eur J Pharm Biopharm 2009;72:252-9.

Rogers M, Peter P. Cognitive impairment in multiple sclerosis: Evidence-based analysis and recommendations. J Clin Neurosci 2007;14:919-27.

Jaiswal J, Anantvar S. Formulation and evaluation of thermoreversible nasal in situ gel of metoprolol succinate. Int J Pharm Pharm Sci 2012;4:96-102.

Parmar V, Lumbhani N. Development and evaluation of ion dependent in-situ nasal gelling systems of metoclopramide hydrochloride as an antimigraine model drug. Int J Lat Res Sci Tech 2012;1:80-9.

Khairnar P, Walke P, Narkhede P, Nehete J. Formulation and in-vitroevaluation of thermoreversible rizatriptan benzoate nasal gel. Int J Pharm Pharm Sci 2011;3:250-6.

Miller C, Donovan D. Effect of poloxamer 407 gels on the miotic activity of pilocarpine nitrate in rabbits. Int J Pharm 1982;12:142-52.

Durgapal S, Rana M, Mukhopadhyay S, Rana AJ, Goswami L, Joshi S. Formulation and evaluation of in-situ nasal gel of montelukast sodium for the effective treatment of asthma. Int J Pharm Sci Res 2018;9:2792-9.

Yadav D, Kunjwani H, Suryawanshi S. Formulation and Evaluation of thermosensitive in situ gel of salbutamol sulphate for nasal drug delivery system. Int J Pharm Pharm Sci 2012;4:188-94.

Singh RM, Kumar A, Pathak K. Mucoadhesive in situ nasal gelling drug delivery systems for modulated drug delivery. Expert Opin Drug Deliv 2013;10:115-30.

Pund S, Rasve G, Borade G. Ex vivo permeation characteristics of venlafaxine through sheep nasal mucosa. Eur J Pharm Sci 2013;48:195-201.

Ahiwale R, Mahaparale P, Chakor R. Formulation and evaluation of nasal in situ gel bupropion hydrochloride. World J Pharm Pharm Sci 2014;4:595-614.

Majithiya R, Ghosh P, Umrethia M, Murthy R. Thermoreversible-mucoadhesive gel for nasal delivery of sumatriptan. AAPS PharmSciTech 2006;7:E80-6.

ICH Harmonized Tripartite Guideline, Federal Register. Photostability Testing of New Drug Substance and Products. London, UK: European Medicines Agency; 1997. p. 62.

Wang Y, Jiang S, Wang H, Bie H. A mucoadhesive, thermoreversible in situ nasal gel of geniposide for neurodegenerative diseases. PLoS One 2017;12:1-17.

Shelke S, Shahi S, Jalalpure S, Dhamecha D. Formulation and evaluation of thermoreversible mucoadhesive in-situ gel for intranasal delivery of Naratriptan hydrochloride. J Drug Deliv Sci Technol 2015;29:238-44.

Yong S, Choi S, Rhee D. Effect of sodium chloride on the gelation, gel strength and bioadhesive force of poloxamer gels. Int J Pharm 2001;275:195-205.




How to Cite

Pallavi M. Chaudhari. (2021). Optimization and Evaluation of In situ Nasal Gel of Donepezil Hydrochloride. Asian Pacific Journal of Health Sciences, 8(2), 104–110. https://doi.org/10.21276/apjhs.2021.8.2.20