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1-Laurin-3-Palmitin as a Novel Matrix of Solid Lipid Particles: Higher Loading Capacity of Thymol and Better Stability of Dispersions Than Those of Glyceryl Monostearate and Glyceryl Tripalmitate

机译:1-Laurin-3-Palmitin作为固体脂质颗粒的新型基质:与单硬脂酸甘油酯和三棕榈酸甘油酯相比百里酚的负载量更高分散稳定性更好

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摘要

To develop solid lipid nanoparticles (SLNs) with a new lipid matrix for delivery of hydrophobic bioactive molecules, high purity 1-laurin-3-palmitin (1,3-LP) was synthesized and the prepared 1,3-LP SLNs were compared with those of two common SLN matrices in glyceryl monostearate (GMS) and glyceryl tripalmitate (PPP). Conditions of preparing SLNs were first optimized by evaluating the particle size, polydispersity index (PDI), zeta-potential, and stability. Thereafter, the performance of SLN loading of a model compound in thymol was studied. The loading capacity of thymol in 1,3-LP SLNs was 16% of lipids and higher than 4% and 12% for GMS- and PPP-SLNs, respectively. The 1,3-LP SLNs also had the best efficiency to entrapment thymol during the prolonged storage. X-ray diffraction (XRD) analyses confirmed the excellent crystalline stability of 1,3-LP leading to the stable entrapment efficiency and better stability of thymol-loaded SLNs. Conversely, the polymorphic transformation of GMS and PPP resulted in the declined entrapment efficiency of thymol in the corresponding SLNs. This work indicated the 1,3-diacylglycerol (DAG) SLNs could be used as a promising delivery system for the encapsulation of hydrophobic bioactive molecules with high loading capacity and stability.
机译:为了开发具有新型脂质基质的固体脂质纳米颗粒(SLN),该脂质基质可用于输送疏水性生物活性分子,合成了高纯度的1-laurin-3-palmitin(1,3-LP),并与制备的1,3-LP SLN进行了比较。单硬脂酸甘油酯(GMS)和三棕榈酸甘油酯(PPP)中两种常见SLN矩阵的特征。首先通过评估粒径,多分散指数(PDI),ζ电位和稳定性来优化制备SLN的条件。此后,研究了百里香酚对模型化合物的SLN加载性能。百里香酚在1,3-LP SLNs中的负载能力为脂质的16%,而对于GMS-和PPP-SLNs则分别高于4%和12%。 1,3-LP SLNs在长时间储存​​期间也具有最佳的捕获百里酚的效率。 X射线衍射(XRD)分析证实1,3-LP具有出色的结晶稳定性,从而导致稳定的包封效率和负载百里香酚的SLN具有更好的稳定性。相反,GMS和PPP的多态性转化导致百里香酚在相应SLNs中的包封效率下降。这项工作表明1,3-二酰基甘油(DAG)SLN可用作具有高负载能力和稳定性的疏水性生物活性分子封装的有前途的传递系统。

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