title: Crystalline drug aconitine-loaded poly(d,l-lactide-coglycolide) nanoparticles: preparation and in vitro release.
abstract: This paper reports both the optimization of aconitine entrapment and its release from biodegradable poly(d,l-lactide-coglycolide) (PLGA) nanoparticles prepared using the O/W single-emulsion/solvent-evaporation technique. The influence of several parameters, such as the initial aconitine mass, aqueous-phase pH, volume ratio of aqueous/organic phase (W/O), PLGA concentration in the organic phase, etc., on aconitine encapsulation were investigated. The optimized nanoparticles had an entrapment efficiency of 88.40+/-3.02% with drug loading capacity of 9.42+/-2.93%. Crystallization growth, which played a crucial role in hindering the incorporation of aconitine into the polymer carrier, was proposed. Differential scanning calorimetry and X-ray powder diffraction demonstrated that aconitine existed in an amorphous state or as a solid solution in the polymeric matrix. The in vitro release profiles exhibited a sustained release of aconitine from nanoparticles and a pH-dependent character in phosphate-buffered saline with different pH values. Moreover, aconitine-loaded PLGA nanoparticles could lead to improvement in the stability of aconitine. This work demonstrated the feasibility of encapsulating aconitine into PLGA nanoparticles using the O/W single-emulsion/solvent-evaporation technique.
authors.affiliation: Key Laboratory of Drug Targeting of the Ministry of Education, West China School of Pharmacy, Sichuan University, China.
authors.forename: Xuefan
authors.initials: X
authors.lastname: Xu
authors.forename: Qingyu
authors.initials: Q
authors.lastname: Xiang
authors.forename: Zhiyao
authors.initials: Z
authors.lastname: He
authors.forename: Yuehua
authors.initials: Y
authors.lastname: Liu
authors.forename: Dan
authors.initials: D
authors.lastname: Zhou
authors.forename: Xuan
authors.initials: X
authors.lastname: Qin
authors.forename: Tingting
authors.initials: T
authors.lastname: Fan
authors.forename: Zhirong
authors.initials: Z
authors.lastname: Zhang
authors.forename: Yuan
authors.initials: Y
authors.lastname: Huang
mesh_terms: D000157:Aconitine / Q000008:administration & dosage / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D019344:Lactic Acid; D053769:Nanocapsules; D053758:Nanoparticles; D036103:Nanotechnology / Q000379:methods; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D003692:Delayed-Action Preparations; D053769:Nanocapsules; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000157:Aconitine