Characterization and Application of Polysaccharide-coated O/W emulsion

我们开发了一种脂质体，其中含有天然存在的多糖，部分被胆固醇取代，以使脂质体具有物理化学稳定性和更强的细胞特异性。此外，我们还报道了用疏水多糖包覆O/ w -卵磷脂乳液的稳定性。在这项工作中，我们采用了一种新的和改进的配方，选择性细胞毒性α -亚麻酸（ALA）。该方法通过在ALA油滴表面包覆含或不含TriC_8的疏水多糖（如降胆固醇普鲁兰，CHP），对O/ w乳液进行胶体稳定，并研究其体内抗肿瘤活性。在三辛烷甘油酯（TriC_8）存在或不存在的情况下，用超声波将CHP和ALA混合制备O/ w乳液。TriC_8的加入大大提高了CHP/ALA乳液的胶体稳定性。腹腔注射CHP/ ala乳状液可有效延长存活时间，尤其是腹腔移植MM46乳腺肿瘤细胞的C3H/He小鼠。静脉注射CHP/ALA/ tric_8乳剂后，C3H/He小鼠皮下移植的同一肿瘤细胞的生长也明显受到抑制，但体重没有下降。通过使用这种胶体稳定的O/ w乳液，可以全身给药一种非常亲脂的液体药物。

We developed a liposome as cated with a naturally occurring polysaccharide which was partly substituted by cholesterol groups in order to make the liposome mrte physicochemically stable and more cell specific. Furthermore, we reported that O/W-lecithin emulsion is stabilized by coating with the hydrophobized polysaccharide. In this work, we employed a new and improved formulation for a very lipofilic and liquid drug, selectively cytotoxic alpha-linolenic acid (ALA). This methodology involves the colloidal stabilization of a O/W-emulsion by coating the surface of oil droplets of ALA with or without TriC_8 with a hydrophobized polysaccharide such as cholesterol-bearing pullulan, CHP and studied its in vivo antitumor activity.The O/W-emulsion was prepared by ultrasonication of a mixture of CHP and ALA in the presence or absence of trioctanoylglyceride (TriC_8). Colloidal stability of the CHP/ALA emulsion was largely improved by adding TriC_8. Intraperitoneal injection of the CHP/ALA-emulsion effectively prolonged the survial, especially, of C3H/He mice which received intraperitoneal transplantation of MM46 mammary tumore cells. The growth of the same tumor cells subcutaneously transplanted in C3H/He mice also was significantly suppressed without any loss of body weight when CHP/ALA/TriC_8-emulsion was intravenously injected. By using such the colloidally stable O/W-emulsion, a systemic administration of a very lipophilic and liquid drug became possible.