title: Benzocaine-loaded polymeric nanocapsules: study of the anesthetic activities.
abstract: This paper describes a comparison of different polymeric nanocapsules (NCs) prepared with the polymers poly(D,L-lactide-co-glycolide), poly(L-lactide) (PLA), and poly(ε-caprolactone) and used as carrier systems for the local anesthetic (LA) benzocaine (BZC). The systems were characterized and their anesthetic activities investigated. The results showed particle size distributions with polydispersity indices below 0.135, average diameters up to 120 nm, zeta potentials up to -30 mV, and entrapment efficiencies around 70%. Formulations of BZC using the polymeric NCs presented slower release profiles, compared with that of free BZC. Slowest release (release constant, k = 0.0016 min(-1)) was obtained using the PLA NC system. Pharmacological evaluation showed that encapsulation of BZC in PLA NCs prolonged its anesthetic action. This new formulation could potentially be used in future applications involving the gradual release of local anesthetics (LAs).
authors: Department of Biochemistry, State University of Campinas, Campinas, São Paulo, Brazil.
authors: Nathalie Ferreira Silva
authors: NF
authors: De Melo
authors: Daniele Ribeiro
authors: DR
authors: De Araújo
authors: Renato
authors: R
authors: Grillo
authors: Carolina Morales
authors: CM
authors: Moraes
authors: Angélica Prado
authors: AP
authors: De Matos
authors: Eneida
authors: E
authors: de Paula
authors: André Henrique
authors: AH
authors: Rosa
authors: Leonardo Fernandes
authors: LF
authors: Fraceto
mesh_terms: D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000494:pharmacology*; D000818:Animals; D001566:Benzocaine / Q000008:administration & dosage* / Q000494:pharmacology*; D019344:Lactic Acid / Q000737:chemistry; D008297:Male; D051379:Mice; D053769:Nanocapsules / Q000737:chemistry*; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012584:Sciatic Nerve / Q000187:drug effects
chemical_list: D000779:Anesthetics, Local; D053769:Nanocapsules; D011091:Polyesters; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; C016240:polycaprolactone; D011100:Polyglycolic Acid; D019344:Lactic Acid; C033616:poly(lactide); D001566:Benzocaine