维生素 K1 传递用固体脂质纳米粒的特性描述和制剂优化。

Characterization and formulation optimization of solid lipid nanoparticles in vitamin K1 delivery.

机构信息

Graduate Institute of Biochemical and Biomedical Engineering, Chang Gung University, Taoyuan, Taiwan, ROC.

出版信息

Drug Dev Ind Pharm. 2010 Jul;36(7):751-61. doi: 10.3109/03639040903460453.

Abstract

BACKGROUND

Solid lipid nanoparticle (SLN) systems have been applied to various drugs and delivery routes. Vitamin K1 is an important cofactor for maintaining hemostasis and preventing hemorrhage.

METHOD

Vitamin K1-loaded SLNs are systematically being developed by optimizing triglycerides and lipophilic and hydrophilic surfactants based on the size and stability of the resulting SLNs. Concentrations of the surfactants, Myverol and Pluronic, were optimized by a central composite design and response surface methodology. Vitamin K1 (phylloquinone) was used as a lipophilic drug in the SLN system to evaluate the potential for oral delivery.

RESULTS

Vitamin K1-loaded SLNs had a mean size of 125 nm and a zeta potential of -23 mV as measured by photon correlation spectroscopy. The prepared SLNs were examined by differential scanning calorimetry and transmission electron microscopy and found to have an imperfect crystalline lattice and a spherical morphology. Effects of ultrasonication duration and drug load on the particle size and entrapment efficiency of the SLNs were also evaluated.

CONCLUSION

More than 85% of the vitamin K1 was entrapped in SLNs when the payload was <5%. The vitamin K1 in SLNs was stable for a 54-h duration in simulated gastric and intestinal fluids. The particle size and vitamin K1 entrapped in the SLN were stable after 4 months of storage at 25 degrees C. The results demonstrated that SLNs prepared herein can potentially be exploited as carriers for the oral delivery of vitamin K1.

摘要

背景

固体脂质纳米粒(SLN)系统已应用于各种药物和给药途径。维生素 K1 是维持止血和预防出血的重要辅助因子。

方法

基于所得 SLN 的粒径和稳定性,通过优化甘油三酯和亲脂性和亲水性表面活性剂,系统地开发了载有维生素 K1 的 SLN。通过中心复合设计和响应面法优化了表面活性剂 Myverol 和 Pluronic 的浓度。将维生素 K1(叶绿醌)用作 SLN 系统中的亲脂性药物,以评估口服递送的潜力。

结果

通过光子相关光谱法测量,载有维生素 K1 的 SLN 的平均粒径为 125nm,Zeta 电位为-23mV。通过差示扫描量热法和透射电子显微镜检查了所制备的 SLN,并发现其具有不完美的结晶晶格和球形形态。还评估了超声处理时间和药物载量对 SLN 的粒径和包封效率的影响。

结论

当载药量<5%时,超过 85%的维生素 K1 被包封在 SLN 中。在模拟胃液和肠液中,SLN 中的维生素 K1 在 54 小时内稳定。在 25°C 下储存 4 个月后,SLN 的粒径和包封的维生素 K1 稳定。结果表明,本文制备的 SLN 可作为维生素 K1 口服递送的载体。

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