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Optimization of the emulsification and solvent displacement method for the preparation of solid lipid nanoparticles.

机译:乳化和溶剂置换法优化固体脂质纳米粒的制备方法。

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OBJECTIVE: The essential aim of this article is to prepare solid lipid nanoparticles (SLNs) by emulsification and solvent displacement method and to determine the best process conditions to obtain submicron particles. METHODS: The emulsification and solvent displacement method is a modification of the well-known emulsification-diffusion method, but without dilution of the system. The extraction of the partially water-miscible solvent from the emulsion globules is carried out under reduced pressure, which causes the diffusion of the solvent toward the external phase, with subsequent lipid aggregation in particles whose size will depend on the process conditions. The critical variables affecting the process, such as stirring rate, the proportion of phases in the emulsion, and the amount of stabilizer and lipid, were evaluated and optimized. RESULTS: By this method, it was possible to obtain a high yield of solids in the dispersion for the lipids evaluated (Compritol((R)) ATO 888, Geleol((R)), Gelucire((R)) 44/14, and stearic acid). SLNs of up to approximately 20 mg/mL were obtained for all lipids evaluated. A marked reduction in size, between 500 and 2500 rpm, was seen, and a transition from micro- to nanometric size was observed. The smaller particle sizes obtained were 113 nm for Compritol((R)) ATO 888, 70 nm for Gelucire((R)) 44/14, 210 nm for Geleol((R)), and 527 nm for stearic acid, using a rotor-stator homogenizer (Ultra-Turrax((R))) at 16,000 rpm. The best phase ratio (organic/aqueous) was 1 : 2. CONCLUSIONS: The process proposed in this study is a new alternative to prepare SLNs with technological potential.
机译:目的:本文的基本目的是通过乳化和溶剂置换法制备固体脂质纳米颗粒(SLNs),并确定获得亚微米颗粒的最佳工艺条件。方法:乳化和溶剂置换法是对众所周知的乳化-扩散法的改进,但不对系统进行稀释。从乳液小球中提取部分与水混溶的溶剂是在减压下进行的,这导致溶剂向外相扩散,随后脂质聚集在颗粒中,其大小将取决于工艺条件。评估和优化了影响该过程的关键变量,例如搅拌速度,乳液中的相比例以及稳定剂和脂质的量。结果:通过该方法,对于所评估的脂质,可以在分散体中获得高产率的固体(Compritol ATO 888,Geleol 44 Gelucire 44/14,和硬脂酸)。对于所有评估的脂质,SLN最高可达约20 mg / mL。观察到尺寸在500至2500 rpm之间显着减小,并且观察到从微米级到纳米级的转变。所获得的较小粒径是ATO 888为Compritol?888的113 nm,Gelucire®44/14的为70 nm,Geleol®的为210 nm,以及硬脂酸为527 nm。转子-定子均质器(Ultra-Turrax(R))的转速为16,000 rpm。最佳相比(有机/水)为1:2。结论:本研究中提出的方法是制备具有技术潜力的SLN的新方法。

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