Abstract

FORMULATION AND EVALUATION OF NASAL IN-SITU GEL OF BUPROPION HYDROCHLORIDE

Ahiwale Raj*,  Mahaparale Paresh, Chakor Rishikesh

ABSTRACT

Bupropion Hydrochloride is widely used antidepressant in a world community of which 10% of its population ageing from 20 to 29 suffer from depression. Bupropion hydrochloride is available in oral dosage form. As drug administered through oral route undergoes first pass metabolism, only 5-20% of bupropion hydrochloride is bioavailable. The present study’s objective was to fulfil the need to overcome deficiency of bioavailability and other problems associated with administration with oral route. Accordingly the study commenced with the aim to formulate and evaluate nasal in-situ gel of bupropion hydrochloride, study completed with accessing the safety and stability of formulation. For the said purpose excipients like Poloxamer 407, Carbopol 940, and Methyl paraben were used for their thermosensetive, mocoadhesive and antimicrobial property respectively. The experimental method started with preliminary studies, based on result of same, 32 factorial design was employed. Nine batches were formulated and were subjected for evaluation such as Appearance, pH, Drug Content, Gelation Time, Gelation Temperature, Gel Melting Temperature, Gel Strength, Mucoadhesion, Viscosity, Ex vivo Permeability & Histopathology. On basis of the results obtained F8 formulation was found to be good in terms of gelation temperature, gelation time, drug content, mucoadhesion, gel strength, rheological studies. Ex-vivo studies revealedthe sustain effect of gel andfinally safety parameter was confirmed by the histopathological studies. The formulation was found to be stable by accessing its stability over 6 months.

Keywords: Bupropion Hydrochloride, in-situ gel, bioavailability, poloxamer 407, carbopol 940. Intranasal delivery.