title: Preparation and characterization of poly(ε-caprolactone) nanospheres containing the local anesthetic lidocaine.
abstract: The objective of this work was to develop a modified release system for the local anesthetic lidocaine (LDC), using poly(ε-caprolactone) (PCL) nanospheres (NSs), to improve the pharmacological properties of the drug when administered by the infiltration route. In vitro experiments were used to characterize the system and investigate the release mechanism. The NSs presented a polydispersion index of 0.072, an average diameter of 449.6 nm, a zeta potential of -20.1 mV, and an association efficiency of 93.3%. The release profiles showed that the release of associated LDC was slower than that of the free drug. Atomic force microscopy analyses showed that the spherical structure of the particles was preserved as a function of time, as well as after the release experiments. Cytotoxicity and pharmacological tests confirmed that association with the NSs reduced the toxicity of LDC, and prolonged its anesthetic action. This new formulation could potentially be used in applications requiring gradual anesthetic release, especially dental procedures.
authors.affiliation: Department of Environmental Engineering, São Paulo State University, Sorocaba, SP, Brazil.
authors.forename: Estefânia Vangelie
authors.initials: EV
authors.lastname: Ramos Campos
authors.forename: Nathalie Ferreira
authors.initials: NF
authors.lastname: Silva de Melo
authors.forename: Viviane Aparecida
authors.initials: VA
authors.lastname: Guilherme
authors.forename: Eneida
authors.initials: E
authors.lastname: de Paula
authors.forename: André Henrique
authors.initials: AH
authors.lastname: Rosa
authors.forename: Daniele Ribeiro
authors.initials: DR
authors.lastname: de Araújo
authors.forename: Leonardo Fernandes
authors.initials: LF
authors.lastname: Fraceto
mesh_terms: D000779:Anesthetics, Local / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D041702:BALB 3T3 Cells; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers; D004355:Drug Stability; D005347:Fibroblasts / Q000187:drug effects / Q000473:pathology; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008012:Lidocaine / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D008297:Male; D051379:Mice; D018625:Microscopy, Atomic Force; D009043:Motor Activity / Q000187:drug effects; D054118:Nanospheres; D036103:Nanotechnology; D009407:Nerve Block; D017288:Pain Threshold / Q000187:drug effects; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011930:Reaction Time; D012584:Sciatic Nerve / Q000187:drug effects; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000779:Anesthetics, Local; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011091:Polyesters; C016240:polycaprolactone; D008012:Lidocaine