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纳米结构脂质载体作为药物递送系统的表征与稳定性

Characterization and stability of nanostructured lipid carriers as drug delivery system.

作者信息

Abbasalipourkabir R, Salehzadeh A, Abdullah R

机构信息

Faculty of Medicine, Hamadan University of Medical Science, Hamadan, Iran.

出版信息

Pak J Biol Sci. 2012 Feb 1;15(3):141-6. doi: 10.3923/pjbs.2012.141.146.

DOI:10.3923/pjbs.2012.141.146
PMID:22866544
Abstract

Recently more focus has been put to the development of innovative drug-delivery systems that includes polymer nanoparticles, emulsions and liposomes and solid lipid nanoparticles (SLNs). The SLNs have been proposed to be an alternative colloidal drug delivery system. The aim of this study was preparation and characterization of solid lipid nanoparticle (SLN) using varieties of emulsifier for encapsulation of the drug with poor water solubility. In these study four types of solid lipid nanoparticles were prepared based on different compositions of palm oil (S154) and lecithin (Lipoid 100) using the high pressure homogenization method. The SLN formulation had the following (palm oil+lecithin) compositions: SLN-01 (90 + 10%, respectively), SLN-02 (80 + 20%, respectively), SLN-03 (70 + 30%, respectively) and SLN-04 (60 + 40%, respectively). The SLNs were characterized and the optimum stability factors for one year storage determined. The parameters used to characterize the SLNs were particle size and polydispersity index (particle sizer), zeta potential (zetasizer), crystallinity (differential scanning calorimetry and wide angle X-ray diffraction), ultrastructure (transmission electron microscopy). Varying the palm oil and lecithin compositions resulted in SLNs of variable sizes and zeta potentials. The particle sizes of SLN-01, SLN-02, SLN-03 and SLN-04 were 298.40 +/- 11.80, 255.40 +/- 3.20, 145.00 +/- 3.39 and 273.00 +/- 86.50 nm, respectively, while the zeta potentials were -19.44 +/- 60.00, -19.50 +/- 1.80, -17.83 +/- 10.00 and -13.33 +/- 2.30 mV, respectively. Thermoanalysis and X-ray diffraction analysis showed that the SLNs had lower crystallinity than bulk lipid. The SLNs were generally round and uniform in shape under transmission electron microscopy. The SLN dimensional data suggested they had high quality physicochemical characteristics, which are conducive for the loading of poor water solubility drugs.

摘要

最近,更多的注意力被放在了创新药物递送系统的开发上,这些系统包括聚合物纳米颗粒、乳剂、脂质体和固体脂质纳米粒(SLNs)。固体脂质纳米粒已被提议作为一种替代的胶体药物递送系统。本研究的目的是使用多种乳化剂制备和表征用于包封水溶性差的药物的固体脂质纳米粒(SLN)。在这些研究中,采用高压均质法,基于棕榈油(S154)和卵磷脂(Lipoid 100)的不同组成制备了四种类型的固体脂质纳米粒。SLN制剂具有以下(棕榈油+卵磷脂)组成:SLN-01(分别为90 + 10%)、SLN-02(分别为80 + 20%)、SLN-03(分别为70 + 30%)和SLN-04(分别为60 + 40%)。对SLNs进行了表征,并确定了一年储存期的最佳稳定性因素。用于表征SLNs的参数有粒径和多分散指数(粒度分析仪)、zeta电位(zeta电位仪)、结晶度(差示扫描量热法和广角X射线衍射)、超微结构(透射电子显微镜)。改变棕榈油和卵磷脂的组成导致了不同尺寸和zeta电位的SLNs。SLN-01、SLN-02、SLN-03和SLN-04的粒径分别为298.40±11.80、255.40±3.20、145.00±3.39和273.00±86.50 nm,而zeta电位分别为-19.44±60.00、-19.50±1.80、-17.83±10.00和-13.33±2.30 mV。热分析和X射线衍射分析表明,SLNs的结晶度低于块状脂质。在透射电子显微镜下,SLNs的形状通常为圆形且均匀。SLN的尺寸数据表明它们具有高质量的物理化学特性,这有利于负载水溶性差的药物。

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