Andalib Sare, Varshosaz Jaleh, Hassanzadeh Farshid, Sadeghi Hojjat
Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, India.
Adv Biomed Res. 2012;1:45. doi: 10.4103/2277-9175.100147. Epub 2012 Aug 28.
Nanostructured lipid carriers (NLC) are a mixture of solid and liquid lipids or oils as colloidal carrier systems that lead to an imperfect matrix structure with high ability for loading water soluble drugs. The aim of this study was to find the best proportion of liquid and solid lipids of different types for optimization of the production of LDL targeted NLCs used in carrying 5-Fu by the emulsification-solvent evaporation method.
The influence of the lipid type, cholesterol or cholesteryl stearate for targeting LDL receptors, oil type (oleic acid or octanol), lipid and oil% on particle size, surface charge, drug loading efficiency, and drug released percent from the NLCs were studied by a full factorial design.
The NLCs prepared by 54.5% cholesterol and 25% of oleic acid, showed optimum results with particle size of 105.8 nm, relatively high zeta potential of -25 mV, drug loading efficiency of 38% and release efficiency of about 40%. Scanning electron microscopy of nanoparticles confirmed the results of dynamic light scattering method used in measuring the particle size of NLCs.
The optimization method by a full factorial statistical design is a useful optimization method for production of nanostructured lipid carriers.
纳米结构脂质载体（NLC）是固体和液体脂质或油的混合物，作为胶体载体系统，可形成具有高水溶性药物负载能力的不完美基质结构。本研究的目的是通过乳化 - 溶剂蒸发法，找出不同类型的液体和固体脂质的最佳比例，以优化用于运载5-氟尿嘧啶的低密度脂蛋白靶向NLC的生产。
通过全因子设计研究脂质类型（胆固醇或硬脂酸胆固醇酯用于靶向低密度脂蛋白受体）、油类型（油酸或辛醇）、脂质和油的百分比对粒径、表面电荷、药物负载效率以及NLC中药物释放百分比的影响。
由54.5%胆固醇和25%油酸制备的NLC显示出最佳结果，粒径为105.8 nm，相对较高的ζ电位为 -25 mV，药物负载效率为38%，释放效率约为40%。纳米颗粒的扫描电子显微镜证实了用于测量NLC粒径的动态光散射法的结果。
全因子统计设计的优化方法是生产纳米结构脂质载体的一种有用的优化方法。
