Formulation and evaluation of In-Situ gel of Diltiazem hydrochloride for nasal delivery

[摘要] The objective of present investigation was to develop a mucoadhesive in-situ gel; formulation was developed to have a controlled kinetic drug release and to minimize the toxic effects of diltiazem Hydrochloride (DTZ). DTZ was incorporated into the, blends of thermoreversible, bio adhesive polymers such as poloxamer (PLX) and Hydroxy Propyl Methyl cellulose (HPMC) in the form of in-situ gel by cold technique to reduce mucociliary clearance, and thereby it will increase the contact of formulation with nasal mucosa and hence improving the absorption of drug. The results revealed that as the increase of bio adhesive polymer HPMC concentration, decrease in the gelation temperature (T1) and increase in gel melting temperature (T2). pH of all the formulations were found to be within the range between 5.4 – 6.2 and the nasal mucosa can tolerate the above mentioned pH of the formulations. The drug content for all the prepared formulations was found to be 97% - 100%. The mucoadhesion test indicates that the level of HPMC increases, the mucoadhesive strength also increases. The developed formulations had optimum viscosity, and it was observed that an influence of diffusion on drug particles with increase in the concentration of HPMC. The optimized formulation shows the controlled drug release (86.32%) than aqueous drug solution (93.81%). The drug release performance was greatly affected by bio polymers used and their compositions in the in situ gels preparation, which allows absorption in nasal mucosa.

[学科分类] 药理学