Thermosetting microemulsions and mixed micellar solutions as drug deliverysystems for periodontal anesthesia

Citation
M. Scherlund et al., Thermosetting microemulsions and mixed micellar solutions as drug deliverysystems for periodontal anesthesia, INT J PHARM, 194(1), 2000, pp. 103-116
Citations number
49
Categorie Soggetti
Pharmacology & Toxicology
Journal title
INTERNATIONAL JOURNAL OF PHARMACEUTICS
ISSN journal
03785173 → ACNP
Volume
194
Issue
1
Year of publication
2000
Pages
103 - 116
Database
ISI
SICI code
0378-5173(20000120)194:1<103:TMAMMS>2.0.ZU;2-H
Abstract
In the present study, thermosetting microemulsions and mixed micellar solut ions were investigated as drug delivery systems for anesthetizing the perio dontal pocket. The structure of the systems, consisting of the active ingre dients lidocaine and prilocaine. as well as two block copolymers (Lutrol(R) F127 and Lutrol(R) F68), was investigated by NMR spectroscopy and photon c orrelation spectroscopy (PCS). The results obtained for dilute (1-3% w/w) s olutions 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 in dicates a preferential solubilization of the active components in micelles over unimers. Analogous to the Lutrol(R) F127 single component system these formulations display an abrupt gelation on increasing temperature. The gel ation temperature was found to depend on both the drug ionization and conce ntration. These systems have several advantages over emulsion-based formula tions including good stability, ease of preparation. increased drug release rate, and improved handling due to the transparency of the formulations. ( C) 2000 Elsevier Science B.V, All rights reserved.