title: 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.
authors.affiliation: National Facilities in Engineering and Technology with Industrial Collaboration Centre, University College of Pharmaceutical Sciences, Kakatiya University, Warangal- 506 009, Andhra Pradesh, India.
authors.forename: Chinna Reddy
authors.initials: CR
authors.lastname: Palem
authors.forename: Ramesh
authors.initials: R
authors.lastname: Gannu
authors.forename: Narender
authors.initials: N
authors.lastname: Doodipala
authors.forename: Vamshi Vishnu
authors.initials: VV
authors.lastname: Yamsani
authors.forename: Madhusudan Rao
authors.initials: MR
authors.lastname: Yamsani
mesh_terms: D000268:Adhesiveness; D000269:Adhesives; D000327:Adsorption; D000328:Adult; D000465:Algorithms; D000818:Animals; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004294:Domperidone / Q000008:administration & dosage* / Q000493:pharmacokinetics; D018492:Dopamine Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D065127:Dopamine D2 Receptor Antagonists; D016503:Drug Delivery Systems; D004355:Drug Stability; D005079:Excipients; D006801:Humans; D006813:Humidity; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D009061:Mouth Mucosa / Q000378:metabolism; D009092:Mucous Membrane / Q000378:metabolism; D012463:Saliva / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013552:Swine; D013718:Tensile Strength; D055815:Young Adult
chemical_list: D000269:Adhesives; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D005079:Excipients; D004294:Domperidone