Synthesis of lidocaine-loaded PLGA microparticles by flow focusing. Effects on drug loading and release properties.
In the present work, two methods for the preparation of lidocaine-loaded PLGA microparticles are compared. The differences between the polymeric particles obtained by solvent evaporation (SEVM) or flow focusing (FF) were studied by means of scanning electron microscopy and surface thermodynamics determinations. A detailed investigation of the capabilities of the polymer particles to load this drug is described. The physical state of the drug in the polymeric particles and the existence of interactions between both entities were studied by differential scanning calorimetry. The main factors determining the lidocaine incorporation and the release kinetics were the synthesis procedure followed, the amount of drug dissolved in the organic phase during the synthesis routine, the type of polymer (molecular weight and end chemical groups) and the size and the hydrophobic/hydrophilic properties of the particles. The FF technology allowed higher drug incorporations and slower release kinetics. The release studies showed a biphasic profile probably due to diffusion-cum-degradation mediated processes.
Holgado
M A
MA
Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, c/Profesor García González 2, Seville, Spain. holgado@us.es
Arias
J L
JL
Cózar
M J
MJ
Alvarez-Fuentes
J
J
Gañán-Calvo
A M
AM
Fernández-Arévalo
M
M
D000465:Algorithms; D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000138:chemical synthesis*; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D004339:Drug Compounding; D019344:Lactic Acid; D008012:Lidocaine / Q000008:administration & dosage* / Q000138:chemical synthesis*; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D010316:Particle Size; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012995:Solubility; D013816:Thermodynamics
D000779:Anesthetics, Local; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D008012:Lidocaine