Role of zein incorporation on hydrophobic drug-loading capacity and colloidal stability of phospholipid nanoparticles
Role of zein incorporation on hydrophobic drug-loading capacity and colloidal stability of phospholipid nanoparticles
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DOI：
10.1016/j.colsurfb.2018.07.068
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发表时间：
2018-11-01
影响因子：
5.8
通讯作者：
Lim, Soo-Jeong
中科院分区：
文献类型：
--
作者：
Hong, Soon-Seok;Thapa, Raj Kumar;Lim, Soo-Jeong
脂质体--磷脂酰胆碱纳米粒（PC-NP）是一种很有吸引力的疏水性药物胶体载体，但其载药量低、物理不稳定性限制了其临床应用。玉米醇溶蛋白是从玉米中获得的不溶于水的两亲性蛋白质。我们在此研究了开发玉米醇溶蛋白-磷脂酰胆碱混合纳米颗粒（Z/PC-NP）作为先进的疏水药物载体的可能性。采用传统的脂质体制备方法，加入树脂，制备Z/PC-NP。玉米醇溶蛋白掺入PC-NP的程度受PC组成的影响。DSC表明玉米醇溶蛋白降低了PC的相变温度，FTIR显示玉米醇溶蛋白的酰胺键减弱但清晰，与PC NP相比，Z/PC NP的异质氢键水平增加。LS、TEM和cryo-TEM研究表明Z/PC-NP是由玉米醇溶蛋白核和玉米醇溶蛋白-PC混合壳组成的球形纳米粒，Z/PC-NP对疏水模型药物（紫杉醇、多西他赛、塞来昔布和姜黄素）的载药量高于玉米醇溶蛋白纳米粒和PC-NP，但药物释放速率居中。Z/PC-NP的血清稳定性和贮存稳定性均高于PC-NP，玉米醇溶蛋白在冻干过程中起到保护作用。Z/PC-NP有望成为一种新型的疏水性药物纳米载体。
Liposome, phosphatidylcholine nanoparticle (PC-NP), is an attractive colloidal carrier of hydrophobic drugs but its clinical development is often limited by low drug-loading capacity and the physical instability. Zein is a water-insoluble amphiphilic protein obtained from the corn. We herein investigated a possibility to develop zein-phosphatidylcholine hybrid nanoparticle (Z/PC-NP) as an advanced hydrophobic drug carrier. By employing the conventional liposome preparation method with the addition of rein, Z/PC-NP were produced. The extent of zein incorporation in PC-NP was affected by PC composition. DSC demonstrated the lowered phase transition temperature of PC by zein and FTIR showed the appearance of weakened but clear amide bonds of zein as well as increased levels of heterogeneous hydrogen bonding of Z/PC-NP compared to PC-NP. LS, TEM and cryo-TEM studies suggested Z/PC-NP to be spherical nanoparticles composed of a zein core and a zein-PC hybrid shell, Z/PC-NP exhibited a higher loading capacity for hydrophobic model drugs (paclitaxel, docetaxel, celecoxib and curcumin), than did the zein nanoparticle and PC-NP, while exhibiting an intermediate drug release rate. The serum stability and the storage stability of Z/PC-NP were greater than those of PC-NP, Zein functioned as a cryoprotectant of PC-NP during freeze-drying. Z/PC-NP may provide a promising nanoparticle carrier of hydrophobic drugs.