Preparation Of Breviscapine Phytosomes And Study Of Their Pharmacological Activities

Phytosome is a new drug delivery system in recent years. Many natural drugs, especially some types of flavonoids, may exhibit a marked affinity for phospholipids. The drug-phospholipid complexes, so called phytosomes, may show some superior chemico-physical properties and enhance the absorption of the drugs. In this paper, Breviscapine phytosomes were prepared, their pharmacological activities in vivo and in vitro were investigated. The full work includes the following contents:Breviscapine phytosomes were prepared and the prescription composition was screened out by orthogonal design. The complexes were characterized by infrared spectrum and differential scanning calorimetry. Particle size analyzing and morphologic observing showed that the complexes were about 830 nm spherical vesicle when dispersed in water. Combining Breviscapine phytosomes with solid dispersion technology, we prepared the Breviscapine phytosomes solid disperse system for better administration. The uptake and wall intestinal permeability of Breviscapine and Breviscapine phytosomes were tested with the use of intestine perfusion technique and everted gut sac method. The result indicated that Breviscapine phytosomes may enhance their absorption by increasing the wall permeability and are mainly absorpted by passive mechanism.Two models were applied to study the pharmacodynamics properties of Breviscapine phytosomes. In the anti-hypoxia tests, we found Breviscapine phytosomes prolonged the mice survival time more effective than that of Breviscapin powder. In the acute hepatic injury induced by CCl4, we found Breviscapine phytosomes may eliminate the edema of liver, enhance the anti-oxidative activity in serum, and protect the configuration and function of hepatocytes. The effection is more obvious than that of Breviscapin powder.