Milind P. Wagh*, Rohit R. Patil, Dhananjay M. Patwardhan, Nikhil N. Kadam


Tizanidine hydrochloride is an antispasmodic agent which acts by relaxing muscle tone. It is well absorbed from the gastrointestinal tract but its oral bioavailability is low due to first pass metabolism which makes it a possible candidate for buccal delivery. It also suffers from short half-life that necessitates frequent administration. Therefore, the objective of this study was to formulate and develop buccoadhesive patch as a potential delivery system for tizanidine hydrochloride. Various formulations were prepared by using chitosan/ thiolated chitosan as film formers and propylene glycol as plasticizer by solvent casting method. A 32 full factorial design was applied to the formulations containing different concentration of polymer and plasticizer combination. Thiolated chitosan was developed by using thioglycolic acid and chitosan in presence of 1-ethyl-3-3(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) as a catalyst. The prepared buccal patches were evaluated for physicochemical and mechanical parameters like surface pH, thickness and weight uniformity, drug content uniformity, folding endurance, in-vitro drug release, in-vitro permeation and mucoadhesive strength. The in-vitro drug release for optimised formulation containing chitosan and thiolated chitosan was 96.8 % and 84.6 %, mucoadhesive strength was 30.14 g and 56.17 g, in-vitro permeation was 83.11 % and 94.22 % respectively. The results of in-vitro study indicates that the formulation containing thiolated chitosan exhibits gradual release of drug, increased mucoadhesive strength and improved in-vitro permeation than the formulation containing unmodified chitosan for buccal delivery of tizanidine.

Keywords: Tizanidine hydrochloride, Chitosan, Thiolated chitosan, In-vitro drug release, In-vitro permeation, Mucoadhesive strength.

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