Transmucosal delivery of domperidone from bilayered buccal patches: In Vitro, Ex Vivo and In Vivo characterization

Abstract

Bilayered mucoadhesive buccal patches for systemic administration of domperidone (DOM), a dopamine-receptor (D(2)) antagonist, were developed using hydroxy propyl methyl cellulose and PVPK30 as a primary layer and Eudragit RLPO and PEO as a secondary layer. Ex vivo drug permeation through porcine buccal membrane was performed. Bilayered buccal patches were developed by solvent casting technique and evaluated for in vitro drug release, moisture absorption, mechanical properties, surface pH, in vitro bioadhesion, in vivo residence time and ex vivo permeation of DOM through porcine buccal membrane from a bilayered buccal patch. Formulation DB4 was associated with 99.5% drug release with a higuchi model release profile and 53.9% of the drug had permeated in 6 h, with a flux of 0.492 mg/h/cm(2) through porcine buccal membrane. DB4 showed 5.58 N and 3.28 mJ peak detachment force and work of adhesion, respectively. The physicochemical interactions between DOM and the polymer were investigated by differential scanning calorimetry (DSC) and fourier transform infrared (FTIR) Spectroscopy. DSC and FTIR studies revealed no interaction between drug and polymer. Stability studies for optimized patch DB4 was carried out at 40°C/75% relative humidity. The formulations were found to be stable over a period of 3 months with respect to drug content, in vitro release and ex vivo permeation through porcine buccal membrane. The results indicate that suitable bilayered mucoadhesive buccal patches with desired permeability could be prepared.

Fenugreek gum derivatives with improved bioadhesion and controlled drug release: In vitro and in vivo characterization

“…Optimized films were wrapped in aluminum foil and stored in a glass bottle for 6 months in the stability chamber, thereafter; they were evaluated for mass uniformity, thickness, folding endurance, drug content and % drug release [32].…”

The Influence of Recrystallized Caffeine on Water-Swellable Polymethacrylate Mucoadhesive Buccal Films

“…However, the polymer system that controls the release of the active is one of the most prominent areas of development of films. Most recent reports on the use of polymethacrylates as film-forming polymers feature them mainly as a drug-controlling materials in the formulation (13)(14)(15). In these studies, Eudragit ® polymers have either been part of the drug-containing layer or as part of the release ratecontrolling layer.…”

Bioadhesive vaginal drug delivery of nystatin using a derivatized polymer: Development and characterization

“…A carboxymethyl derivative of fenugreek gum (CMFG) was prepared, and 34 characterized by DSC, FTIR and X-ray diffraction studies. The derivatized gum was found to possess 35 bioadhesive and film forming properties. A 3 2 factorial design was employed to formulate vaginal films 36 and a response surface methodological approach was used to study the effect of formulation variables on 37 film properties.…”