title: Screening of formulation variables for the preparation of poly(epsilon-caprolactone) nanocapsules containing the local anesthetic benzocaine.
abstract: In this work we describe the screening of four parameters in the preparation, by nanoprecipitation, of poly(epsilon-caprolactone) nanocapsules, used as a drug carrier system for the local anesthetic, benzocaine. A 2(4-1) factorial experimental design was used to study the influence of four different independent variables (polymer, oily phase, Span 60 and Tween 80) on nanocapsule characteristics (size, polydispersion index, zeta potential) and drug loading capability. Best results were obtained using an aqueous formulation comprising 100 mg of polymer, 200 mg of oily phase, 40 mg of Span 60 and 60 mg of Tween 80 in a final volume of 10 mL which produced a colloidal system with particle size of 188 nm, zeta potential -32 mV, polydispersion index 0.07, and benzocaine association efficiency > 87%. These findings open the way for future clinical studies using such formulations.
authors: Department of Biochemistry, State University of Campinas (UNICAMP), Cidade Universitària "Zeferino Vaz", Barão Geraldo, CEP 13083-970, Campinas, São Paulo, Brazil.
authors: Carolina Morales
authors: CM
authors: Moraes
authors: Angélica Prado
authors: AP
authors: de Matos
authors: Renato
authors: R
authors: Grillo
authors: Nathalie F S
authors: NF
authors: de Melo
authors: Eneida
authors: E
authors: de Paula
authors: Newton Luiz
authors: NL
authors: Dias Filho
authors: André Henrique
authors: AH
authors: Rosa
authors: Leonardo Fernandes
authors: LF
authors: Fraceto
mesh_terms: D001566:Benzocaine / Q000008:administration & dosage / Q000737:chemistry*; D020650:Combinatorial Chemistry Techniques; D004339:Drug Compounding / Q000379:methods*; D008422:Materials Testing; D053769:Nanocapsules / Q000737:chemistry* / Q000648:ultrastructure; D011091:Polyesters / Q000737:chemistry*; D013499:Surface Properties
chemical_list: D053769:Nanocapsules; D011091:Polyesters; C016240:polycaprolactone; D001566:Benzocaine