Preparation In Vivo And In Vitro Assessment Of The Flavonoids Liposome From Leaves Of Acanthopanax Senticosus Harms

Acanthopanax is traditional Chinese medicine, which was first recorded in the"Shen Nong Ben Cao Jing" and its active ingredient is flavonoids. However, the poorwater solubility as well as low polar seriously influence the in vivo absorption ofacanthopanax flavonoids, which limit its clinical application．In order to increase theabsorption of the acanthopanax flavonoids, the acanthopanax leaf flavonoids liposomewas prepared.Liposomes can be used for a variety of drug carrier. In this study, the filmdispersion method was used to prepare the acanthopanax leaf flavonoids liposome andthe single factor study was adopted to investigate the preparation process. The factorsof the ratio of phospholipid and cholesterol, the ratio of drug and phospholipids, thewater and medium Ph were choosing to optimize the composition of liposomes. Theoptimization results were as follows: the ratio of phospholipid and cholesterl was10to1, the ratio of drug and phospholipids was1to5, the water and medium Ph was6.0.UV-Vis was used to determine the content of flavonoids in the flavonoidsliposome from Acanthopanax with choosing hyperoside as the reference.The detectivewavelength was510nm. The standard curve of hyperoside was that:Y=16.450X-0.0118（R2=0.9999）,the linear range was from0.01mg/mL to0.07mg/mL．The average recovery was98.32%and RSD was1.28%. The content offlavonoids in the flavonoids liposome from Acanthopanax was8.5%.HPLC was used to determine the content of hyperoside in the flavonoidsliposome from Acanthopanax senticosus. The mobile phase was acetonitrile and0.5%acetic acid aqueous solution,the detective wavelength was360nm, and the columntemperature was28℃. The standard curve of hyperoside was that:Y=3.0×106X-74874(R2=0.9995), the linear range was from0.0984μg to0.5904μg. Theaverage recovery was99.18and RSD was1.07. The content of hyperoside in theflavonoids liposome fromAcanthopanax senticosus was0.891%.Compared with the acanthopanax leaf flavonoids, the oil/water partition coefficient of the flavonoids liposome from acanthopanax senticosus was increased，the increment reached1.51in water,1.67in hydrochloric acid(Ph=1.2),1.37inPBS(Ph=7.4),1.4in PBS(Ph=7.8),1.42in PBS(Ph=8.0).The Wista rats were injuected acanthopanax leaf flavonoids(dosage is200mg/kg),and the pharmacokinetic parameters was calculated by PKSolver. The experimentalresults show that liposomes rats’ AUC and Cmaxwas increased compared withdripping pills rats, and Tmaxwas pushed back.Experimental results showed that thebioavailability of acanthopanax leaf flavonoid liposomes was greater thanacanthopanax leaf flavonoids and acanthopanax leaf drop pills.Pharmacodynamic studies showed that acanthopanax leaf flavonoid liposomescan reduce the water content and brain index of cerebral ischemia rats, which has nosignificant difference with positive drug Buchang Naoxintong Jiaonang. Theacanthopanax leaf flavonoid liposomes can significantly reduce SOD enzyme activityand the levels of NOS and MDA in serum and brain tissue of rats. The experimentalresults showed that the acanthopanax leaf flavonoid liposomes have a protective effecton ischemic brain injury in rats.