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Summary: Arsenic trioxide albumin microspheres (As2O3-BSA-NS) were prepared by using methods of chemical cross-linking. The desirability function (DF), calculated according to the size (<1 μm) distribution, drug loading and drug trapping efficiency, was introduced as a total index for the microspheres formulation. Four factors, inculding W/O ratio, decentralization speed, BSA concentration and stirring stabilization time, were selected and arranged in an orthogonal experimental table. The release characteristic was studied by the drug release experiment in vitro. The four factors affected DF differently. Decentralization speed behaved as the maximum (P<0.01), followed by BSA concentration (P<0.05) and the W/O ratio dose (P<0.05). Stirring stabilization time did not influence DF (P>0.05). The release experiment in vitro showed that As2O3 in As2O3-BSA-NS was released more slower than pure As2O3. It was concluded that regular As2O3-BSA-NS may be prepared by the methods of chemical cross-linking, which was optimized by orthogonal experimental analysis of different factors, and the microspheres can release As2O3 slowly.
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OBJECTIVE:To investigate the biological property of doxorubicin albumin microspheres(DR-HAS-MS) and its tissue distribution in the rats.METHODS:Pancreatin degradation method was applied to determine the biodegradation property of DR-HAS-MS as well as the correlation between the cross linking agent concentration and the degradation time and between the setting time and the degradation time.The dialysis method was applied to study the in vitro drug dissolution/ release characteristics of DR-HAS-MS vs.DR solution.DR concentrations in different tissue of rats at different time following intravenous DR HAS-MS vs.DR solution(at a dose of 2.5 mg?kg~(-1))were determined.RESULTS:The degra dation time increased with the increase of cross linking agent concentration and cross - link time.The optimal setting time was 90 min.Within 6 hours the dissolution ratio of DR from DR solution was 100%,while the releasing ratio of DR from DRHAS -MS suspension was only 80%within 168 hours;DR concentrations in the liver and the spleen in the DR HAS-MS group were significantly higher than in DR solution group(P
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Objective: To evaluate the distribution and degradatio n of albumin microspheres (AMS) with average diameter of 56.3 ?m injected into jugular external artery.Methods: 125 I labeled AMS we re injected into rabbit's jugular external artery. The radioactive amount of loc al tissue and internal organs was measured. 760 ml/L urografin angiography was e mployed to observe the re opening of embolized vessels after AMS infusion of e xternal jugular artery in 5 dogs. Results: The AMS was mai nly concentrated in the target area (92.23%) after injection. The micro artery was obviously embolized by AMS and re opened in 7～9 days. Conclusio n : The AMS can be used as the drug bearer with delayed releasing eff ection.
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0.05), except PYM-AMS of 1.130 mg/ml and PYM of 300 ?g/ml at 24 h.In the same group and at the same exposure time,higher dose of the corresponding agents showed higher growth inhibition ratio(P0.05).At the same doses 48 h exposure of PYM-AMS or PYM gave higher apoptosis rate than 24 h exposure(P
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Objective: To evaluate the effect of pingyangmycin-albumin microspheres (PYM-AMS) on the modality of endothelial cells. Methods:In the in vitro study blood vessle endothelial cells of ECV 304 cell line were exposed to PYM-AMS(containing PYM at 150 ?g/ml),AMS and PYM(150 ?g/ml) for 24,48,72 and 96 h respectively. In the in vivo study,24 Japanese white rabbits were divided into 4 groups using randomized block design. PYM+9 g/L NaCl,PYM+soyabean oil, PYM-AMS+soyabean oil(PYM at 5 mg/ml) were injected into the central auricular arteries of the animals(0.26 ml/per ear), then these vessels were examined histologically 2, 7, 14, 21 days after injection respectively. The mophorlogy of the cells was observed by light microscope and electron microscope.Results:In vitro, a great part of cells were swollen and cell number decreased in PYM and PYM-AMS group. But there was no change in AMS group.In vivo, the endothelial cells had no significant changes in PYM+9 g/L NaCl group.In PYM+soyabean oil group, at the 2nd day, the endothelial cells were a little bit swollen. At the 7th day, some endothelial cells were dropped off. At the 21st day, a few of endothelial cells were proliferative. In PYM-AMS group, at the 2nd day, the endothelial cells were a little bit swollen and small vessels were embolized by PYM-AMS. At the 7th day, the endothelial cells were swollen. At the 14th day, the endothelial cells were proliferative and the wall of the central auricular artery had more layers. The lumen of the central artery became smaller, while the surface of PYM-AMS was absorbed. At the 21st day, the wall of the central auricular artery was proliferative and the artery became sclerostenosed. The PYM-AMS was obviously absorbed, while the wall of small vein was proliferative, too. Conclusion:PYM-AMS and PYM may injure blood vessel endothelial cells, the effect of PYM-AMS is more obvious than pingyangmycin.