title: Nanoencapsulation improves the in vitro antioxidant activity of lipoic acid.
abstract: Lipoic acid is a widely studied substance, whose therapeutic effects are related to its antioxidant activity. Our objective was to develop lipoic acid-loaded lipid-core nanocapsules and evaluate their in vitro antioxidant effect against lipid peroxidation induced by ascorbyl free radicals, using soybean lecithin liposomes as the substrate. The nanocapsule suspensions were prepared by interfacial deposition of poly(epsilon-caprolactone) and characterized by particle size and polydispersion index (photon correlation spectroscopy), zeta potencial (eletrophoretic mobility), drug content and encapsulation efficiency (HPLC). The extent of lipid peroxidation was determined (TBARS). The nanostrucutures presented mean diameters of between 191 and 349 nm, zeta potential values from -14.1 +/- 4.5 to -10.4 +/- 0.6, and high lipoic acid encapsulation. A significant increase in the antioxidant activity of lipoic acid was achieved through nanoencapsulation or by increasing its concentration in the formulation. The protection results ranged from 48.9 +/- 3.4 to 57.4 +/- 9.1% for lipoic acid-loaded lipid-core nanocapsules. The lipoic acid release from nanostrucutures significantly decreased with increasing polymer concentration. Also, it was observed an increasing in the antioxidant activity as the lipoic acid release time decreased. The co-encapsulation of lipoic acid with melatonin in lipid-core nanocapsules did not improve the protection against lipid peroxidation. The results obtained demonstrate the optimal concentrations of polymer and lipoic acid in the formulations in terms of enhancing the antioxidant activity. Furthermore, by the strategy applied, it was verified that nanoencapsulation is an efficient alternative to increase the antioxidant effect of lipoic acid, representing a potential approach for therapeutic applications.
authors.affiliation: Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752, 90610-000, Porto Alegre, RS, Brazil.
authors.forename: Irene C
authors.initials: IC
authors.lastname: Külkamp
authors.forename: Bruna D
authors.initials: BD
authors.lastname: Rabelo
authors.forename: Simone J
authors.initials: SJ
authors.lastname: Berlitz
authors.forename: Mateus
authors.initials: M
authors.lastname: Isoppo
authors.forename: Mariana D
authors.initials: MD
authors.lastname: Bianchin
authors.forename: Scheila R
authors.initials: SR
authors.lastname: Schaffazick
authors.forename: Adriana R
authors.initials: AR
authors.lastname: Pohlmann
authors.forename: Sílvia S
authors.initials: SS
authors.lastname: Guterres
mesh_terms: D000975:Antioxidants / Q000008:administration & dosage* / Q000494:pharmacology*; D066298:In Vitro Techniques; D015227:Lipid Peroxidation / Q000187:drug effects; D008081:Liposomes; D008550:Melatonin / Q000008:administration & dosage; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry / Q000648:ultrastructure; D036103:Nanotechnology; D010316:Particle Size; D011091:Polyesters; D008063:Thioctic Acid / Q000008:administration & dosage* / Q000494:pharmacology*
chemical_list: D000975:Antioxidants; D008081:Liposomes; D053769:Nanocapsules; D011091:Polyesters; C016240:polycaprolactone; D008063:Thioctic Acid; D008550:Melatonin