title: Biodegradable polymeric nanocapsules based on poly(DL-lactide) for genistein topical delivery: obtention, characterization and skin permeation studies.
abstract: The isoflavone genistein (GEN) is a natural product with potential applications for skin cancer treatment and chemoprevention; however its high lipophilicity and chemical instability limits its clinical use. Therefore, attempts towards protecting GEN against degradation and increasing its penetration in the skin might be a valid approach. In this work, GEN loaded-PLA nanocapsules (GEN-NC) were prepared by interfacial deposition of preformed polymer (nanoprecipitation); physicochemical characterization and stability studies for 90 days were conducted. GEN-NC were incorporated into semi-solid formulations and permeation experiments were carried out using porcine ear skin. GEN-NC optimized formulation presented a mean diameter of 139 +/- 7.31 nm, polydispersity index of 0.128 +/- 0.08, encapsulation efficiency of 89.63 +/- 2.27% and drug loading from 0.6 to 1.4 w/w%. Stability studies demonstrated that nanocapsules did not exhibit aggregation during the 90 days of the assay, however, a drop in encapsulation efficiency was observed in the first 10 days. Permeation experiments demonstrated that a higher amount of GEN reaches deeper layers of the skin and increased penetration was achieved when GEN-NC were incorporated in a semi-solid gel formulation, indicating that GEN-NC might be a promising nanocarrier system for skin delivery of GEN.
authors.affiliation: Faculdade de Farmácia, Lab. Tecnologia Farmacêutica e Sistemas de Liberação de Fármacos, Universidade Federal de Goiás, Goiânia, GO, 74.605-220, Brasil.
authors.forename: Ana Lúcia Teixeira de Carvalho
authors.initials: AL
authors.lastname: Zampieri
authors.forename: Fabrícia Saba
authors.initials: FS
authors.lastname: Ferreira
authors.forename: Erica Crispim
authors.initials: EC
authors.lastname: Resende
authors.forename: Marilisa Pedroso Nogueira
authors.initials: MP
authors.lastname: Gaeti
authors.forename: Danielle Guimarães Almeida
authors.initials: DG
authors.lastname: Diniz
authors.forename: Stephânia Fleury
authors.initials: SF
authors.lastname: Taveira
authors.forename: Eliana Martins
authors.initials: EM
authors.lastname: Lima
mesh_terms: D000287:Administration, Topical; D000818:Animals; D001672:Biocompatible Materials / Q000494:pharmacology*; D001673:Biodegradation, Environmental / Q000187:drug effects; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D019833:Genistein / Q000008:administration & dosage* / Q000494:pharmacology*; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D018625:Microscopy, Atomic Force; D053769:Nanocapsules / Q000737:chemistry*; D010316:Particle Size; D010539:Permeability / Q000187:drug effects; D011091:Polyesters / Q000737:chemistry*; D012869:Skin Absorption / Q000187:drug effects*; D055672:Static Electricity; D034421:Sus scrofa
chemical_list: D001672:Biocompatible Materials; D053769:Nanocapsules; D011091:Polyesters; C033616:poly(lactide); D019833:Genistein