Development, Optimization and Characterization of Innovative Buccal Delivery System of Zolmitriptan

Naman      Raval; Punit      Parejiya; Pragna      Shelat; Anita      Lalwani

doi:10.2174/2210304x11202040007

Abstract

The aim of proposed research work was to develop a bioadhesive sustained release matrix tablets of zolmitriptan for treatment of migrane. Compression coating technology was used for preparing the tablets that released the drug unidirectionally. Drug loaded core tablets were prepared with mucoadhesive and sustained release polymers like Noveon AA1 Polycarbophil and hydroxypropyl methylcellulose (HPMC K4M) while unloaded coat tablets, that covered the three surfaces of the core tablet, were prepared using ethyl cellulose and Compritol ATO 888. A two factor, three level, face centred, central composite design (CCD) was used to optimize amount of Noveon AA1 and amount of HPMC so as to get required mucoadhesion and rate of drug release. Higher levels of HPMC K4M in the experimental design batches exhibited higher in vitro drug release in the initial hour while the NoveonAA1 levels could be related to increase in mucoadhesive strength. Overlay plot comprising a region that satisfied the constraints for all the selected attributes was generated. Formulation containing 10% w/w of Noveon AA1 and 10% w/w of HPMC K4M was found to be optimum. Checkpoint batches were also prepared to validate the evolved mathematical models. Korsmeyer-Peppas release kinetic model best fitted the optimized batch release profile which showed anomalous diffusion mechanism. The In Vitro drug release could be correlated with the Ex vivo drug permeation. It can be concluded that buccal route can be one of the alternatives available for administration of zolmitriptan.

Keywords: Unidirectional buccal delivery, zolmitriptan, design of experiment, mucoadhesive delivery, compression coating, allergens, URBT, ANOVA, Mucoadhesion, interpenetration, Korsmeyer-Peppas model, receptor compartment, mucosa, mucoadhesion, saliva