Breviscapine Liposome For Lung Targeting Pharmaceutical Research

Aiming at the rapid lung infection resulted from different factors, we have made researches on breviscapine, an effective traditional Chinese medicine for SARS. separating from Dengzhanxixin (Herb Erigerontis). With modern preparation technology, breviscapine liposome is ready for use, which will release only on target lungs. Therefore, a more effective lung-targeting drug with fewer side effects is expected to be produced.Safe and innoxious SPC for injection as the carrier, breviscapine liposome is prepared by means of thin film evaporation and probe ultrasonic technique, then of lyophilization. Its lung targeting characteristics are proved to be true in the research on its preparing process, quality evaluation, pharmacokinetics and its targeting effects.In the research on preparation techniques, we took particle size, morphology, polydispersity (PDI), encapsulation efficiency as parameters, the factors influencing the preparation of breviscapine liposome were studied separately. Then orthogonal design was adopted to acquire the optimal technological conditions under the evaluation direction of encapsulation efficiencies. With morphology, color and redispersion as index, we have made out freeze-dried breviscapine liposome.The. result of cryprotector-screening assay suggested that 10% sucrose should be appropriate. The experiment of stability indicated that the shelf-life of breviscapine liposome can be improved to three months after lyophilization.In the research on quality evaluation, we established an overall quality standard of breviscapine liposome. The liposome had a fine-looking appearance, narrow size distribution under the transmission electron microscope (TEM). Its mean diameter is 379.4nm on average measured by Zetamaster, and its average drug load and encapsulation efficiency are 23.6% ± 1.53% and 87.5%+ 1.2%.The experimenting result of its pharmacokinetics and targeting effects showed :hat breviscapine liposome are selectively concentrated in lungs. As a result, it can increase its concentration in lungs and decrease in other organs, thus its toxicity is reduced, but the effect is enhanced.