Geniposide/Baicalin Cardiovascular Function And Applied To The Stent Coatings

Restenosis is an ongoing problem after the implantation of vascular stents and requires secondary intervention to the patient. Drug eluting stents (DES) are developed to reduce these problems. They are optimized with smooth surface finishing and a controlled release kinetic of the bioactive substance. But most important is the selection of a drug, which selectively inhibits the proliferation of smooth muscle cells but does not affect the proliferation of endothelial cells but rather promotes it, and additionally, it also should have anticoagulant properties.Traditional Chinese medicine typically deals with bioactive components, which influence multiple targets in the human body, which presents a complex network of interactions. This treatment approach therefore is promising to fulfill the multiple requirements of a vascular stent. The present study therefore evaluates several traditional Chinese medicine components for their effect on blood coagulation, blood cells including endothelial progenitor cells and blood vessel cells. (1) Gardenosides especially geniposide from Gardenia jasminoides Ellis extracts and (2) baicalin from Scutellaria baicalensis and geniposide/baicalin. Further, (3) formulations of a geniposide-loaded PLGA film and baicalin containing phospholipid vesicles are evaluated.The main conclusions were as following:(1) Geniposide decreases whole blood viscosity and suppresses ADP induced platelet aggregation in vitro. In cell culture it inhibits the release of the vasoconstrictive endothelin and raises the content of prostaglandin. In animal models the thrombus weight of arterio-venous thrombi is decreased, and it inhibits FeCl3 induced thrombosis a rat carotid artery model. (2) While both geniposide and baicalin have stimulating effect on endothelial cell function and suppressive effect on smooth muscle cell proliferation, the combined application in thin films has clearly enhanced effects. (3) PLGA as drug carrier at a ratio LA:GA=60:40 forms smooth coatings with favorable degradation properties for drug eluting stents. Drug loadings is 10%, gardenoside and baicalin phospholipid complex phosphatide compound ratio of 1:2 drug-coated drugs within one month of the cumulative release amount to 90%, with endothelial cells, inhibits the hyperplasia of smooth muscle cells, at the same time can reduce the number of platelets and significantly prolong thrombin time (TT) and plasma part activated clotting time (APTT) live enzymes, drug coating can be used as a drug-eluting stent.