Toxicology Department, University of Medicine and Pharmacy Victor Babes Timisoara, Eftimie Murgu Square, No. 2, Timisoara, 300041, Romania.
J Biomed Nanotechnol. 2011 Apr;7(2):317-24. doi: 10.1166/jbn.2011.1297.
Betulinic acid (3beta, hydroxy-lup-20(29)-en-28-oic acid, BA), a pentacyclic triterpenoid, is derived from a widely distributed natural anticancer compound betulin. It has selective anticancer activity against several tumor cells, and recently it was shown that it also possess anti-angiogenic effects. The objective of this study was to formulate betulinic acid, a poorly aqueous-soluble compound, in flax-seed oil containing nanoemulsion formulation for enhanced delivery efficiency and to effectively inhibit the tumor angiogenic process. The nanoemulsion was prepared using high pressure homogenization method with a Microfludizer processor. The betulinic acid nanoemulsion was studied for the effect on the angiogenic process by performing the in vivo chick embryo chorioallantoic membrane (CAM) assay. The sample volume of 1 microl and 5 microl of the blank and BA nanoemulsions were applied directly on the CAM. The preliminary results from macroscopic, morphological and immunohistochemical evaluations have shown that morphological change was produced in the CAM mesenchyme with a negative impact on the normal growth of the capillaries. Betulinic acid does possess anti-angiogenic activity in a dose dependent manner, and the nanoemulsion formulation maintained this effect.
白桦脂酸（3β，羟基-羊毛甾-20（29）-烯-28-酸，BA）是一种五环三萜，来源于广泛分布的天然抗癌化合物白桦脂醇。它对几种肿瘤细胞具有选择性抗癌活性，最近表明它还具有抗血管生成作用。本研究的目的是将白桦脂酸（一种水溶性差的化合物）制成亚麻籽油中的纳米乳剂配方，以提高递送效率，并有效抑制肿瘤血管生成过程。纳米乳剂采用高压均质法，使用 Microfludizer 处理器制备。通过进行体内鸡胚绒毛尿囊膜（CAM）试验，研究了白桦脂酸纳米乳剂对血管生成过程的影响。将 1 微升和 5 微升的空白和 BA 纳米乳剂样品直接应用于 CAM。宏观、形态学和免疫组织化学评价的初步结果表明，CAM 间质发生了形态变化，对毛细血管的正常生长产生了负面影响。白桦脂酸具有剂量依赖性的抗血管生成活性，纳米乳剂配方保持了这种作用。
