Abstract
The purpose of the study was to develop Tizanidine HCl (TZN) and Meloxicam (MLX) loaded bilayer mucoadhesive films intended for buccal administration, aiming to enhance the bioavailability. Bilayer films were prepared by solvent evaporation technique selecting arabinoxylan (ARX) as a sustained release (SR) layer forming polymer and hydroxypropyl methylcellulose (HPMC) E-15 as an immediate release (IR) layer-forming polymer. Prepared films were subjected to in-vitro drug release, surface morphology, mechanical strength, compatibility of the ingredients, drug contents, ex-vivo mucoadhesion strength and drug permeation. Crossover study design was applied to study the in-vivo pharmacokinetics by using albino rabbits. Various pharmacokinetic parameters including AUC, Cmax, tmax and t1/2 of both drugs loaded in films were compared with standard solution/dispersion administered to the rabbits at the dose of 1mg/kg. The results unveiled instant release and permeation of MLX from IR layer, while good controlled release and permeation characteristics of TZN from SR films over 8 h. films were of uniform thickness with smooth surface and satisfactory mechanical strength. Mucoadhesion strength was sufficient to provide suitable contact time with mucosal membrane. The pharmacokinetic study exhibited prompt absorption of MLX with better AUC 0-t (6655.64 ng/ml*h vs 6538.99 ng/ml*h) and Cmax (436.98 ng/ml vs 411.33 ng/ml) from oral dispersion. Similarly buccal films has shown enhanced half-life (9.91hr vs 2.51 hr), AUC 0-t (1043.4 ng/ml*h vs 149.1 ng/ml*h) and Cmax (91.92 ng/ml vs 42.29 ng/ml) from oral solution. A statistical investigation disclosed a significantly improved pharmacokinetics of TZN and MLX after their absorption across buccal route following administration of buccal film (p<0.05). ARX proved expedient and bilayer buccal films as a drug delivery system ascertained the dual effect of providing instant release of one active agent and persistent release of another one with improved pharmacokinetics.
Highlights
Buccal films have been approved in the three major regions of the world including US, EU and Japan for prescription
Buccal films are considered suitable drug delivery system that can be used for rapid absorption of the drug across the buccal mucosa as well as avoidance of first pass metabolism and enhancing the bioavailability of the drugs
ARX was soaked in distilled water to prepare 3% w/v gel, aqueous solutions of glycerol (6%), hydroxypropyl methylcellulose (HPMC) K15M (2%), Analysis of pharmacokinetic profile polysuccralose (2%) and Tizanidine HCl (TZN) (3%) were prepared
Summary
Buccal films have been approved in the three major regions of the world including US, EU and Japan for prescription. Buccal adhesive films are new drug delivery system, which are made by using mucoadhesive polymer. They have been recently interested due to avoidance of the first pass effect and ability to sustain release for topical and oral therapy. Bi-layer films can be a carrier of more than one drug at a time and serve as a drug delivery system with potential of providing diversity and adaptations. TZN is a myotonolytic agent and considered an effective agent for the treatment of spasticity It has to face the extensive hepatic metabolism when administered through oral route due to which its bioavailability is limited only to 30 to 40%. MLX is a non-steroidal anti-inflammatory drug and is effective in the treatment of various pain disorders. Buccal films are considered suitable drug delivery system that can be used for rapid absorption of the drug across the buccal mucosa as well as avoidance of first pass metabolism and enhancing the bioavailability of the drugs
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