Abstract:
The aim of the study was to formulate and develop Thermoreversible nasal in situ gel of
Cyclobenzaprine hydrochloride by cold method which may improving the bioavailability and
avoidance of the first pass metabolism. Drug excipient compatibility study was carried out
using Fourier transform infrared spectroscopy which shows that neither drug decomposition
nor drug-excipients and excipients-excipients interactions occurred in the formulation.
Thermoreversible nasal in situ gel of Cyclobenzaprine hydrochloride containing Poloxamer
407 was used as the gelling agent gives excellent thermo sensitive gelling effect and
Hydroxyl Propyl Methyl Cellulose K4M was used as a mucoadhesive Polymer gives good
mucoadhesivity to the formulation and increase nasal residence time of the formulation.
Quick release of drug was achieved by PEG 400 used as a permeation enhancer. 32 Factorial
designs were apply for optimization of the concentration of HPMCK4M and PEG400. In situ
gel based formulation of Cyclobenzaprine Hydrochloride was evaluated for clarity, pH ,Drug
Content ,Gelling Temperature, mucoadhesive force,% drug release ,histopathological study
and stability study. An optimized formulation containing 18% poloxamer 407 , 0.4 %
HPMCK4M and 1% PEG was found to be good in terms of clarity, pH (5.8), gelation
temperature (320C), mucoadhesive force (736 Dyne/cm2), Drug content (96.87),%
Cumulative drug released (94.05% in 5 hr with a flux of 0.122 mg/cm2/min) and had no
cellular damage as indicated by histopathological study. The optimized formulation was
stable for 21 days in accelerated conditions.
