Ramos Campos, Estefânia Vangelie [UNESP]Silva de Melo, Nathalie Ferreira [UNESP]Guilherme, Viviane Aparecidade Paula, EneidaRosa, André Henrique [UNESP]de Araújo, Daniele RibeiroFraceto, Leonardo Fernandes [UNESP]2014-05-272014-05-272013-01-01Journal of Pharmaceutical Sciences, v. 102, n. 1, p. 215-226, 2013.0022-35491520-6017http://hdl.handle.net/11449/74101The 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 449.6nm, a zeta potential of -20.1mV, 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. © 2012 Wiley Periodicals, Inc.215-226engAnalgesiaAnesthetic activityControlled releaseDrug releaseLidocaineNanoparticlesNanospheresNanotechnologyPoly(ε-caprolactone)Polymeric drug carrierlidocainenanospherepolycaprolactoneanimal experimentanimal tissueatomic force microscopycontrolled studycytotoxicitydrug formulationdrug releasedrug structurein vitro studymalemousenonhumanzeta potentialAnesthetics, LocalAnimalsBALB 3T3 CellsCell SurvivalChemistry, PharmaceuticalDelayed-Action PreparationsDose-Response Relationship, DrugDrug CarriersDrug StabilityFibroblastsHydrogen-Ion ConcentrationKineticsMaleMiceMicroscopy, Atomic ForceMotor ActivityNerve BlockPain ThresholdParticle SizePolyestersReaction TimeSciatic NerveSolubilityTechnology, PharmaceuticalArtigo10.1002/jps.23350WOS:000312145900023Acesso restrito2-s2.0-848706730400000-0002-2042-018X