title: Thermosetting microemulsions and mixed micellar solutions as drug delivery systems for periodontal anesthesia.
abstract: In the present study, thermosetting microemulsions and mixed micellar solutions were investigated as drug delivery systems for anesthetizing the periodontal pocket. The structure of the systems, consisting of the active ingredients lidocaine and prilocaine, as well as two block copolymers (Lutrol F127 and Lutrol F68), was investigated by NMR spectroscopy and photon correlation spectroscopy (PCS). The results obtained for dilute (1-3% w/w) solutions show discrete micelles with a diameter of 20-30 nm and a critical micellization temperature of 25-35 degrees C. Gel permeation chromatography (GPC) was used to study the distribution of the active ingredients, and indicates a preferential solubilization of the active components in micelles over unimers. Analogous to the Lutrol F127 single component system these formulations display an abrupt gelation on increasing temperature. The gelation temperature was found to depend on both the drug ionization and concentration. These systems have several advantages over emulsion-based formulations including good stability, ease of preparation, increased drug release rate, and improved handling due to the transparency of the formulations.
authors.affiliation: AstraZeneca R&D, SE-151 85, S]odert]alje, Sweden.
authors.forename: M
authors.initials: M
authors.lastname: Scherlund
authors.forename: M
authors.initials: M
authors.lastname: Malmsten
authors.forename: P
authors.initials: P
authors.lastname: Holmqvist
authors.forename: A
authors.initials: A
authors.lastname: Brodin
mesh_terms: D000766:Anesthesia, Dental / Q000379:methods*; D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000737:chemistry*; D002850:Chromatography, Gel; D004058:Diffusion; D016503:Drug Delivery Systems; D004655:Emulsions; D006358:Hot Temperature; D008012:Lidocaine / Q000008:administration & dosage* / Q000737:chemistry*; D008823:Micelles; D010514:Periodontal Pocket; D017785:Photons; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D011318:Prilocaine / Q000008:administration & dosage* / Q000737:chemistry*; D011409:Propylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D012212:Rheology; D012996:Solutions; D013057:Spectrum Analysis / Q000379:methods
chemical_list: D000779:Anesthetics, Local; D004655:Emulsions; D008823:Micelles; C116176:PEO-PPO-PEO; D011409:Propylene Glycols; D012996:Solutions; D011318:Prilocaine; D011092:Polyethylene Glycols; D008012:Lidocaine