title: Hydrogel containing adapalene- and dapsone-loaded lipid-core nanocapsules for cutaneous application: development, characterization, in vitro irritation and permeation studies.
abstract: Lipid-core polymeric nanocapsule suspensions containing adapalene and dapsone (AD-LCNC) were developed and incorporated in a Carbopol 940® hydrogel (AD-LCNC HG). A nanoemulsion (AD-NE), similarly prepared but omitting the polymer, was developed and also incorporated in a Carbopol 940®hydrogel (AD-NE HG) to evaluate the polymer effect. Physicochemical characteristics were evaluated. AD-LCNC suspensions containing 0.07% of dapsone and 0.025% of adapalene presented an average size of 194.9 ± 0.42 nm, zeta potential of -15 ± 1.2 mV and polydispersity index of 0.12 ± 0.02, using electrophoretic light scattering (n = 3). The granulometric profiles showed unimodal size distributions for AD-LCNC suspensions, demonstrating that no microscopic population is present in the formulation. No instability phenomena were observed by multiple light-scattering analysis. Photomicrographs obtained by TEM showed homogeneous- and spherical-shaped particles. The encapsulation efficiency was 99.99% for dapsone and 100% for adapalene. The pH values for AD-LCNC suspensions were 5.1 and 7.6 for AD-LCNC HG. Formulations were classified as nonirritant in the HET-CAM test. Rheological analysis demonstrated a non-Newtonian pseudoplastic profile. The in vitro skin permeation studies showed a higher amount of adapalene in epidermis (130.52 ± 25.72 ng/mg) and dermis (4.66 ± 2.5 ng/mg) for AD-NE HG. The AD-LCNC HG presented higher amount of dapsone in both the skin layers (73.91 ± 21.64 ng/mg in epidermis and 4.08 ± 0.85 ng/mg in dermis). The assay showed significant difference between AD-LCNC HG and AD-NE HG (p < 0.05), and drug was not found in the receptor medium.
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre - RS , Brazil.
authors.forename: Rubia L
authors.initials: RL
authors.lastname: Pereira
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre - RS , Brazil.
authors.forename: Fernanda I
authors.initials: FI
authors.lastname: Leites
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre - RS , Brazil.
authors.forename: Karina
authors.initials: K
authors.lastname: Paese
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre - RS , Brazil.
authors.forename: Rafaela M
authors.initials: RM
authors.lastname: Sponchiado
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre - RS , Brazil.
authors.forename: Cecília B
authors.initials: CB
authors.lastname: Michalowski
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre - RS , Brazil.
authors.forename: Silvia S
authors.initials: SS
authors.lastname: Guterres
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre - RS , Brazil.
authors.forename: Elfrides E S
authors.initials: EE
authors.lastname: Schapoval
keywords: Acne; franz cells; het-cam; nanotechnology; rheology