title: A novel oromucosal prolonged release mucoadhesive suspension by one step spray coagulation method.
abstract: An oromucosal mucoadhesive suspension (OMS) able to combine the peculiarities of prolonged release mucoadhesive microparticles with those of an immediate release oromucosal solution is described. Microparticles were obtained by ionotropic gelation of alginate blended with another mucoadhesive material in a one step process where the cross-linking bath constituted the suspension vehicle. The effects of formulation and processing conditions on OMS performances were measured in-vitro determining the enhancement of drug penetration in buccal porcine mucosa and inhibition of tooth plaque formation using flurbiprofen and delmopinol as model drugs, respectively. Well-formed and spherical microparticles were obtained combining alginate with carbomer; linear dependence of particle size from the feed composition, viscosity and atomization pressure was found. As demonstrated by using FITC-labelled microparticles, the system remained onto the buccal mucosa at least for a six hour period. As a consequence, 0.1% flurbiprofen OMS guaranteed a concentration of flurbiprofen into buccal porcine mucosa over 6 hours comparable to 0.25% flurbiprofen reference solution, allowing a potential reduction of the 60% administered dose. The use of in-house made artificial mouth revealed that the once-a-day administration of 0.1% delmopinol OMS was as effective in plaque inhibition as the 0.2% delmopinol reference solution product given twice-a-day. These results suggested that the development of bioadhesive oromucosal suspensions, localizing the drug into buccal cavity, can reduce regimen and administrated dose.
authors: Department of Pharmaceutical Sciences, Università degli Studi di Milano, Via G. Colombo, 71-20133 Milan, Italy. francesco.cilurzo@unimi.it
authors: Francesco
authors: F
authors: Cilurzo
authors: Chiara G M
authors: CG
authors: Gennari
authors: Francesca
authors: F
authors: Selmin
authors: Umberto M
authors: UM
authors: Musazzi
authors: Cristiano
authors: C
authors: Rumio
authors: Paola
authors: P
authors: Minghetti
mesh_terms: D000180:Acrylic Resins; D000268:Adhesiveness; D000278:Administration, Buccal; D000464:Alginates / Q000737:chemistry; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry; D003773:Dental Plaque / Q000378:metabolism; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems; D016650:Fluorescein-5-isothiocyanate / Q000737:chemistry; D005456:Fluorescent Dyes / Q000737:chemistry; D005480:Flurbiprofen / Q000008:administration & dosage* / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D009025:Morpholines / Q000008:administration & dosage* / Q000737:chemistry; D009061:Mouth Mucosa; D009067:Mouthwashes / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D011145:Polyvinyls / Q000737:chemistry; D013535:Suspensions; D013552:Swine; D014783:Viscosity
chemical_list: D000180:Acrylic Resins; D000464:Alginates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D005456:Fluorescent Dyes; D006603:Hexuronic Acids; D009025:Morpholines; D009067:Mouthwashes; D011145:Polyvinyls; D013535:Suspensions; C006912:carboxypolymethylene; D005480:Flurbiprofen; D020723:Glucuronic Acid; C073738:delmopinol; D016650:Fluorescein-5-isothiocyanate