Design and in vitro characterization of ivermectin nanocrystals liquid formulation based on a top-down approach

被引:10
|
作者
Javier Starkloff, Walter [1 ,2 ]
Bucala, Veronica [2 ]
Daniel Palma, Santiago [3 ]
Gonzalez Vidal, Noelia L. [1 ,4 ]
机构
[1] UNS, Dept Biol Bioquim & Farm, San Juan 670, RA-8000 Bahia Blanca, Buenos Aires, Argentina
[2] UNS, Planta Piloto Ingn Quim PLAPIQUI, CONICET, Bahia Blanca, Buenos Aires, Argentina
[3] Univ Nacl Cordoba, Fac Ciencias Quim, Dept Farm, Unidad Invest & Desarrollo Tecnol Farmaceut UNITE, Cordoba, Argentina
[4] Consejo Nacl Invest Cient & Tecn, Bahia Blanca, Buenos Aires, Argentina
关键词
Antihelmintics; dissolution rate; high pressure homogenization; nanosuspensions; solubility; stability; POORLY SOLUBLE DRUGS; DISSOLUTION RATE; NANOSUSPENSIONS; STABILIZATION; PERMEABILITY; SURFACTANTS; INHIBITION; STABILITY; EFFLUX;
D O I
10.1080/10837450.2016.1200078
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of this study was to develop ivermectin (IVM) nanosuspensions (NSs) to improve the dissolution rate of this poorly water-soluble drug. Different NSs combining different stabilizers, i.e. poloxamer 188 (P188), polysorbate 80 (T80), polyvinylpyrrolidone (PVP), and sodium lauryl sulfate (SLS), were prepared by high-pressure homogenization. The stabilizers were selected based on the saturation solubility and IVM stability within 72h. The screening of formulations was performed by considering the drug content within the nanosize range. The best formulation (IVM:T80:PVP 1:0.5:0.5wt%) was characterized in terms of the particle size distribution, morphology, crystallinity, drug content, and in vitro dissolution profile. This NS was also evaluated from a stability point of view, by conditioning samples at a constant temperature and relative humidity for six months. The fresh and conditioned best NSs Z-sizes were 174.6 and 215.7nm, respectively; while both NSs showed low polydispersity indexes. The faster dissolution rate for the IVM NS was attributed to the presence of nanoparticles and changes to the crystal structure (i.e. amorphization) that further improved solubility. The best NS had a 4-fold faster initial dissolution rate than raw IVM, and is thus a promising formulation for the treatment of human and animal parasitic diseases.
引用
收藏
页码:809 / 817
页数:9
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