title: Mixture designs in the optimisation of PLGA nanoparticles: influence of organic phase composition on β-aescin encapsulation.
abstract: The objective of this study was to enhance the encapsulation of the antileishmanial saponin aescin in poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles (NPs). We prepared the NPs by the O/W and W/O/W combined emulsification solvent evaporation/salting-out technique and investigated the influence of organic phase composition on the NPs' size, zeta potential and entrapment efficiency (EE%) using mixture designs. The obtained NPs were monodispersed with Z(ave)<300 nm and exhibited negative zeta potentials. For the single emulsion, the co-solvent concentration was shown to be the primary determinant of drug entrapment. The EE% increased from 14% to 22% by decreasing the amount of DMSO from 80% to 25% (v/v) in the organic polymer solution. For the double emulsion, EE% was 22% on average and independent of the organic phase composition. The double-emulsion technique did not enhance the aescin encapsulation as expected due to its amphiphilic nature. The optimised aescin-loaded NPs meet the requirements for further in vitro activity tests.
authors: Laboratory of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp, Antwerpen, Belgium. helene.vandeven@ua.ac.be
authors: H Van de
authors: HV
authors: Ven
authors: J
authors: J
authors: Vandervoort
authors: W
authors: W
authors: Weyenberg
authors: S
authors: S
authors: Apers
authors: A
authors: A
authors: Ludwig
mesh_terms: D004655:Emulsions; D004928:Escin / Q000008:administration & dosage / Q000737:chemistry*; D019344:Lactic Acid / Q000008:administration & dosage / Q000737:chemistry*; D007891:Leishmania / Q000187:drug effects*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000008:administration & dosage / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D014783:Viscosity
chemical_list: D004655:Emulsions; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D004928:Escin