結果證實，不同性質的親脂性溶劑及複合溶劑配方能成功地與油體鈣蛋白及磷脂質形成油水型人造油體。而由篦麻油與複合溶劑配方形成的油水型人造油體來攜帶雌激素，均有明顯提高雌激素的生體可用率。顯示人造油體有保護雌激素在磷脂質及油體鈣蛋白內，免於酵素的破壞作用。其中複合溶劑配方形成的人造油體具有最佳的生體可用率，這可能因其形成較小粒徑的液滴，可經由腸道培氏斑的吸收，除了減少腸道酵素的破壞外，也可避免肝臟的首渡代謝。 The bioavailability of a poorly water-soluble drug in a crystalline solid dosage form is usually poor. The lipid formulation is one of the common methods used to increase the bioavailability and the artificial oil body can be a new lipid formulation. The artificial oil body, an artificial lipoprotein, is composed with triglyceride, cleocin and phospholipid.
The full advantages of the artificial oil body to carry a poorly water-soluble drug and increase its bioavailability remain to be explored, for example, its ability to form the artificial oil body with various oils or lipid formulations and protect the drug from enzyme degradation. Therefore, estradiol, a poorly water-soluble drug with extensive enzyme degradation and first pass effect, was chosen as a model drug to be encapsulated into the artificial oil body to increase the bioavailability.
Mineral oil, diglyceride, various triglycerides, or lipid formulations containing a surfactant, cosurfactant or solubilizer were used to prepare artificial oil bodies and their stability was observed.
Male Sprague-Dawley rats were gavaged by various artificial oil bodies with estradiol, and the level of serum estradiol was determined by EIA to investigate the potential of the artificial oil body as a drug delivery system.
The results show that cleocin and phospholipid have the ability to form the artificial oil body with every kind of oil and lipid formulations. The artificial oil body can protect the estradiol from degradation and increase the bioavailability. The artificial oil body containing the specific lipid formulation has the best bioavailability, indicating it might be absorbed through the peyer’s patches because of its smaller size and avoid the hepatic first-pass metabolism.