title: Buccal films of prednisolone with enhanced bioavailability.
abstract: The conventional formulation of prednisolone is considered to be low in efficacy, primarily on account of their failure in providing and maintaining effective therapeutic drug levels. This study aims to focus on development of a mucoadhesive buccal delivery system with a twofold objective of offering a rapid as well as a prolonged delivery of prednisolone coupled with enhanced therapeutic efficacy. Buccoadhesive films of prednisolone were prepared by solvent-casting method using hydroxyl propyl methyl cellulose (K100), Carbopol 940 and/or Eudragit NE 40 D. Placebo films possessing the most desirable physicomechanical properties were selected for drug loading. The effect of polymer and its content on film properties, i.e. mucoadhesive strength, swelling and hydration, in vitro drug release was studied. Based on these studies, film F7D was selected for ex vivo permeation across porcine cheek mucosa. The steady state flux of prednisolone across the buccal mucosa was found to be 105.33 ± 32.07 µg/cm(2)/h. A comparative pharmacokinetic study of prepared film (F7D) and oral suspension of prednisolone was conducted. In vivo data of buccal film show greater bioavailability (AUC0-α: 24.26 ± 4.06 µg.h/ml versus 10.65 ± 2.15 µg.h/ml) and higher Cmax (2.70 ± 0.38 µg/ml versus 2.29 ± 0.32 µg/ml) value when compared to oral suspension. The data observed from this study highlight the feasibility of the buccal route as a viable option for delivery of prednisolone.
authors.affiliation: a Swift School of Pharmacy , SGOC, Village Ghaggar Sarai , Rajpura , Punjab , India .
authors.forename: Rachna
authors.initials: R
authors.lastname: Kumria
authors.affiliation: b Department of Pharmaceutical Sciences, College of Clinical Pharmacy , King Faisal University , Al-Ahsa , KSA , and.
authors.forename: Anroop B
authors.initials: AB
authors.lastname: Nair
authors.affiliation: c M. M. College of Pharmacy , Maharishi Markandeshwar University , Mullana, Ambala , Haryana , India.
authors.forename: Garima
authors.initials: G
authors.lastname: Goomber
authors.affiliation: c M. M. College of Pharmacy , Maharishi Markandeshwar University , Mullana, Ambala , Haryana , India.
authors.forename: Sumeet
authors.initials: S
authors.lastname: Gupta
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry*; D000268:Adhesiveness; D000278:Administration, Buccal; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004304:Dosage Forms; D004337:Drug Carriers; D004339:Drug Compounding; D005240:Feasibility Studies; D005938:Glucocorticoids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D065347:Hypromellose Derivatives / Q000737:chemistry*; D008297:Male; D009061:Mouth Mucosa / Q000378:metabolism*; D065568:Oral Mucosal Absorption; D010539:Permeability; D011109:Polymethacrylic Acids / Q000737:chemistry*; D011239:Prednisolone / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013552:Swine; D013678:Technology, Pharmaceutical / Q000379:methods; D014867:Water / Q000737:chemistry
chemical_list: D000180:Acrylic Resins; D004304:Dosage Forms; D004337:Drug Carriers; C496967:Eudragit NE40D; D005938:Glucocorticoids; D011109:Polymethacrylic Acids; D014867:Water; D065347:Hypromellose Derivatives; C006903:carbopol 940; D011239:Prednisolone; C584694:hypromellose 2208 (100 MPA.S)
keywords: Buccal; drug release; mucoadhesive; permeation; pharmacokinetics; prednisolone