Oil components modulate physical characteristics and function of the natural oil emulsions as drug or gene delivery system
Oil components modulate physical characteristics and function of the natural oil emulsions as drug or gene delivery system
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DOI：
10.1016/s0168-3659(00)00363-1
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发表时间：
2001-04-28
影响因子：
10.8
通讯作者：
Jeong, SY
中科院分区：
文献类型：
--
作者：
Chung, H;Kim, TW;Jeong, SY
用18种不同的天然油脂与鸡蛋磷脂酰胆碱(鸡蛋PC)配制水包油型(O/W)型脂肪乳剂，考察不同油脂对乳状液粒径和稳定性的影响。棉籽油、亚麻籽油和月见草油形成的乳状液具有非常大且不稳定的颗粒。角鲨烯、轻质矿物油和霍霍巴豆油形成了颗粒较小的稳定乳状液。剩下的天然油形成了相当稳定的乳状液。初始粒子尺寸较小的乳液比粒子较大的乳液更稳定。研究了不同油品所制得的乳化液尺寸与油品两种物理性质的相关性。乳液的O/W界面张力与粒子大小成反比。粘度的影响不那么明显。为了研究乳剂中的油脂成分对亲脂性药物体外释放特性的调节作用，制备了3种不同载药量的乳剂。角鲨烯、大豆油和亚麻油乳状液分别代表最稳定、中等和最不稳定的体系。对于亲脂性药物，必须稳定的角鲨烯乳剂释放最慢，其次是大豆油，然后是亚麻籽油乳剂。以上述三种不同的油脂作为基因载体，制备了阳离子乳液。最稳定的角鲨烯乳状液的体外转染率最高，豆油次之，亚麻籽油乳状液次之。尽管在无血清条件下乳剂的体外转染率低于脂质体，但在血清浓度为80%(v/v)的条件下，角鲨烯乳剂的体外转染率约为脂质体的30倍。综上所述，O/W乳剂中油组分的选择对于配制乳剂药物或基因递送系统非常重要。(C)2001 Elsevier Science B.V.保留所有权利。
Oil-in-water (o/w) type lipid emulsions were formulated by using 18 different natural oils and egg phosphatidylcholine (egg PC) to investigate how emulsion particle size and stability change with different oils. Cottonseed, linseed and evening primrose oils formed emulsions with very large and unstable particles. Squalene, light mineral oil and jojoba bean oil formed stable emulsions with small particles. The remaining natural oils formed moderately stable emulsions. Emulsions with smaller initial particle size were mon stable than those with larger particles. The correlation between emulsion size made with different oils and two physical properties of the oils was also investigated. The o/w interfacial tension and particle size of the emulsion were inversely proportional. The effect of viscosity was less pronounced. To study how the oil component in the emulsion modulates the in vitro release characteristics of lipophilic drugs, three different emulsions loaded with two different drugs were prepared. Squalene, soybean oil and linseed oil emulsions represented the most, medium and the least stable systems, respectively. For the lipophilic drugs, release was the slowest from the must stable squalene emulsion, followed by soybean oil and then by linseed oil emulsions. Cationic emulsions were also prepared with the above three different oils as gene carriers. In vitro transfection activity was the highest for the most stable squalene emulsion followed by soybean oil and then by linseed oil emulsions. Even though the in vitro transfection activity of emulsions were lower than the liposome in the absence of serum, the activity of squalene emulsion, for instance, was ca. 30 times higher than that of liposome in the presence of 80% (v/v) serum. In conclusion, the choice of oil component in o/w emulsion is important in formulating emulsion-based drug or gene delivery systems. (C) 2001 Elsevier Science B.V. All rights reserved.