Publication

Abstract : The present study was aimed to develop a mucoadhesive in-situ gel of Carvedilol for improved bioavailability by circumventing the hepatic first pass metabolism and patient compliance. Carvedilol was incorporated into the blends of thermoreversible polymer pluronic F 188(PF 188) and bioadhesive polymer Carbopol 940 in the form of in-situ gel by cold technique to reduce the muco ciliary clearance, and thereby it will increase the contact of formulation with nasal mucosa and hence improving drug absorption. The prepared gels were characterized by Gelation temp, pH, Drug content, Gel strength, permeation studies, Histopathological evaluation, stability study etc. The results revealed that as the concentration of Carbopol increases there was a decrease in the gelation temperature. pH of all the formulations were found to be within the range between 4.5-6.0 and the nasal mucosa can tolerate the above mentioned pH of the formulations. The drug content of all formulations was found to be 97.44 to 99.17%. Tests also revealed that as the level of carbopol increases mucoadhesive strength also increase. Viscosity measurement of the formulations at temperatures 25°C 37°C, shows that there was increase in viscosity with increase in the temperature and it was found that all formulations were in liquid state at room temperature and were converted into gel at nasal physiological temperature. The optimized formulation showed a drug release of 93.98% in 480 min. The biopolymers used and their compositions in the in-situ gels preparation greatly affected the drug release which allows absorption in the nasal mucosa.