Screening of Formulation Variables for the Preparation of Poly(epsilon-caprolactone) Nanocapsules Containing the Local Anesthetic Benzocaine

Author(s)

Moraes, Carolina Morales ^[1] ; de Matos, Angelica Prado ^[1] ; Grillo, Renato ^[2] ; de Melo, Nathalie F. S. ^{[1, 2]} ; de Paula, Eneida ^[1] ; Dias Filho, Newton Luiz ^[3] ; Rosa, Andre Henrique ^[2] ; Fraceto, Leonardo Fernandes ^{[1, 2]}

Affiliation

^[1] State Univ Campinas UNICAMP, Dept Biochem, BR-13083970 Campinas, SP - Brazil

^[2] Unesp Univ Estadual Paulista, Dept Environm Engn, BR-18087180 Sao Paulo - Brazil

^[3] Unesp Univ Estadual Paulista, Dept Phys & Chem, BR-15385000 Sao Paulo - Brazil

• Document type: Journal article
• Source: Journal of Nanoscience and Nanotechnology; v. 11, n. 3, p. 2450-2457, MAR 2011.
• Web of Science Citations: 7

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. (AU)