Abstract

THERMOSENSITIVE GELS CONTAINING CARBAMAZEPINE MICROSPHERES FOR INTRANASAL BRAIN TARGETING

Panchaxari Mallappa Dandagi, Rohit Sharma*, Anand Panchakshari Gadad,Vinayak Mastiholimath

Abstract

Context: Carbamazepine, derived from tricyclic antidepressant drugs is one of the most widely used antiepileptic drugs. It is characterized by a considerable hepatic first-pass effect owing to the enzymatic autoinduction of its own metabolism. Objective: The objective of the present investigation was to prepare thermo-sensitive gels containing Carbamazepine microspheres for intranasal brain targeting to prolong the drug release and enhance the bioavailability. Materials and Methods: Carbamazepine loaded chitosan microspheres were prepared by emulsion cross-linking method by varying the drug: polymer ratio and evaluated. Microsphere embedded gel was prepared using Pluronic F127 and Pluronic F68 using the optimized microsphere formulation and evaluated for in vitro permeation and ex vivo permeation. Results: Microsphere formulation containing drug and polymer in the ratio 1:4 was found to be optimized. 17% PF- 127 and 1% PF-68 were found to be promising gel vehicles. The microspheres in the viscous media showed a prolonged release, in comparison to the microspheres alone. Histopathological studies proved that the optimized formulation does not produce any toxic effect on the microscopic structure of nasal mucosa during ex vivo permeation studies. Conclusion: Formulated thermo-sensitive gel can prove to be a promising formulation for the safe and effective intranasal delivery and subsequent brain targeting of Carbamazepine.

Keywords: Thermo-sensitive Gel, Carbamazepine, Chitosan, Pluronic F127, Pluronic F68, Intranasal brain delivery.