Jenning V, Mäder K, Gohla S H
Department of Pharmaceutics, Biopharmaceutics and Biotechnology, Free University of Berlin, Kelchstr. 31, D-12169 Berlin, Germany.
Int J Pharm. 2000 Sep 15;205(1-2):15-21. doi: 10.1016/s0378-5173(00)00462-2.
SLN with improved payloads and enhanced storage stability were investigated. Based on the experiences with solid lipid nanoparticles, a new type of solid lipid nanoparticle has been developed by incorporating triglyceride containing oils in the solid shell of the particle. The structure and mixing behaviour of these particles was characterised by DSC and (1)H-NMR. DSC yields information on the melting and crystallisation behaviour of the solid and liquid constituents of the particles. NMR is especially suited for the characterisation of the liquid oil domains inside the SLN. In this study a medium chain triglyceride oil was successfully incorporated in a matrix of a solid long chain glyceride (glyceryl behenate). The resulting particles were solid but the oil inside the particle remained in a liquid state. The relation between oil supplementation and melting point depression of glyceryl behenate proved to be linear. Mobility of the oil molecules inside the particles was considerably reduced compared to the emulsified oil. Moreover, two different chemical shifts for each of the lipid signals were observed indicating two different chemical environments. The experimental data is in line with a model describing uniform distribution of the oil molecules in the glyceryl behenate for low oil loads. However, at higher oil loads our data indicate the formation of oil clusters within the solid nanoparticle.
对具有改进的载药量和增强的储存稳定性的固体脂质纳米粒(SLN)进行了研究。基于固体脂质纳米粒的经验,通过在颗粒的固体壳中掺入含甘油三酯的油,开发了一种新型的固体脂质纳米粒。这些颗粒的结构和混合行为通过差示扫描量热法(DSC)和氢核磁共振(¹H-NMR)进行了表征。DSC可提供有关颗粒中固体和液体成分的熔化和结晶行为的信息。核磁共振特别适合于表征固体脂质纳米粒内部的液态油域。在本研究中,一种中链甘油三酯油成功地掺入了固体长链甘油酯(山嵛酸甘油酯)的基质中。所得颗粒是固体,但颗粒内部的油保持液态。山嵛酸甘油酯的油添加量与熔点降低之间的关系被证明是线性的。与乳化油相比,颗粒内部油分子的流动性大大降低。此外,每个脂质信号观察到两个不同的化学位移,表明存在两种不同的化学环境。实验数据与描述低油负载下山嵛酸甘油酯中油分子均匀分布的模型一致。然而,在较高油负载下,我们的数据表明在固体纳米颗粒内形成了油簇。
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