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《Drug development and industrial pharmacy》2013,39(4):557-574
AbstractThe size-dependent disposition of liposomes in rats was studied. Liposomes consisting of phosphatidylcholine, cholesterol, dicetylphospate and alphatocopherol in a molar ratio of 4:4:1:1, containing a trace of [14C]-labeled cholesterol as a marker of the lipid phase, were prepared and sized by extruding through polycarbonate membrane. [3H]-inulin was used as a marker of the aqueous phase. In situ liver perfusion in rats showed that hepatic extraction of liposomes was significant for multilamellar vesicles (MLVs) larger than 0.4 μm (0.40, 0.82 and 1.31 μm) and small unilamellar vesicles (SUV), but negligible for 0.25 μm MLV. Pharmacokinetic analysis after intravenous (i.v.) injection showed that the area under the plasma elimination curve (AUC) was significantly higher, but the volume of distribution (Vd) and the elimination rate constant (ke) were significantly lower for the 0.25 μm than for the 1.31 μm liposomes. Comparing the distribution of 1.36 and 0.25 μm MLVs after i.v. injection, the 1.31 μm MLV showed a significantly higher concentration in liver and spleen, but lower concentration in plasma and kidney, than the 0.26 μm in terms of dose percent. These results suggest that size is one of the important factors affecting the fate of liposmes in vivo. There must be a minimun size for effective uptake of liposomes by the reticuloendothelial system. If below the minimum effective uptake size, the MLV should remain in higher concentration in circulation. 相似文献
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Sumio Chono Yoshihiko Tauchi Kazuhiro Morimoto 《Drug development and industrial pharmacy》2013,39(1):125-135
ABSTRACTIn order to confirm the efficacy of liposomes as a drug carrier for atherosclerotic therapy, the influence of particle size on the distribution of liposomes to atherosclerotic lesions in mice was investigated. In brief, liposomes of three different particle sizes (500, 200, and 70 nm) were prepared, and the uptake of liposomes by the macrophages and foam cells in vitro and the biodistributions of liposomes administered intravenously to atherogenic mice in vivo were examined. The uptake by the macrophages and foam cells increased with the increase in particle size. Although the elimination rate from the blood circulation and the hepatic and splenic distribution increased with the increase in particle size in atherogenic mice, the aortic distribution was independent of the particle size. The aortic distribution of 200 nm liposomes was the highest in comparison with the other sizes. Surprisingly, the aortic distribution of liposomes in vivo did not correspond with the uptake by macrophages and foam cells in vitro. These results suggest that there is an optimal size for the distribution of liposomes to atherosclerotic lesions. 相似文献
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以不饱和聚酯(UPR)为原料,采用悬浮法制备粒径在120~250 μm的UPR微粒.考察了搅拌速度,油水比、分散剂及电解质对聚合物颗粒平均粒径及粒径分布的影响. 相似文献
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This study examined the usefuless of erythrocyte-membrane as a biodegradable carrier for intravenous injection of doxorubicin (DOX). Two different preparations of erythrocyte-membrane were used, erythrocyte-ghosts and erythrocyte-vesicles. Ghosts were prepared from red blood cells by hemolysis and repetitive washing until complete removal of hemoglobin. Erythrocyte-vesicles were prepared by ultrasonication of the ghosts suspension by a sonic dismembrator. The membrane products were then incubated with DOX before the injection. In CD rats, the disposition of DOX solution (DOX in normal saline) and erythrocyte-vesicles-DOX followed a two-compartment open model, whereas the ghosts-DOX exhibited a three-compartment characteristics. The area under the curve of the amount in the heart vs time for ghosts-DOX was approximately the same as for the solution. However, the amount of DOX in the heart after erythrocyte-vesicles-DOX injection was below the sensitivity of the detection. The fraction of DOX excreted unchanged in the urine was 0.54 for ghosts-DOX, 0.22 for DOX solution and 0.06 for erythrocyte-vesicles-DOX. The uptake of the drug by the spleen was increased after the administration of erythrocyte-vesicles-DOX. The observed and the calculated data address the usefulness of these delivery systems for DOX. 相似文献
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《Drug development and industrial pharmacy》2013,39(15):2199-2219
AbstractThis study examined the usefuless of erythrocyte-membrane as a biodegradable carrier for intravenous injection of doxorubicin (DOX). Two different preparations of erythrocyte-membrane were used, erythrocyte-ghosts and erythrocyte-vesicles. Ghosts were prepared from red blood cells by hemolysis and repetitive washing until complete removal of hemoglobin. Erythrocyte-vesicles were prepared by ultrasonication of the ghosts suspension by a sonic dismembrator. The membrane products were then incubated with DOX before the injection. In CD rats, the disposition of DOX solution (DOX in normal saline) and erythrocyte-vesicles-DOX followed a two-compartment open model, whereas the ghosts-DOX exhibited a three-compartment characteristics. The area under the curve of the amount in the heart vs time for ghosts-DOX was approximately the same as for the solution. However, the amount of DOX in the heart after erythrocyte-vesicles-DOX injection was below the sensitivity of the detection. The fraction of DOX excreted unchanged in the urine was 0.54 for ghosts-DOX, 0.22 for DOX solution and 0.06 for erythrocyte-vesicles-DOX. The uptake of the drug by the spleen was increased after the administration of erythrocyte-vesicles-DOX. The observed and the calculated data address the usefulness of these delivery systems for DOX. 相似文献
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制备条件对ZrO_2超细粒子尺寸及分布的影响 总被引:8,自引:0,他引:8
本文采用胶体-超临界流体干燥法制备纳米级ZrO2超细粉料,用透射电镜(TEM)、比表面积(BET)和粒度分析法对颗粒尺寸进行观察和测定,并详细考察了制备条件对产品粒子粒度及其分布的影响 相似文献
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《Drug development and industrial pharmacy》2013,39(6):673-680
ABSTRACTIn this work the effect of the encapsulation of diclofenac sodium within liposomes on the reduction of the myotoxicity after intramuscular administration in rats was studied. Diclofenac sodium was encapsulated in small unilamellar liposomes obtained from phosphatidylcholine, cholesterol, and α-tocopherol (40:10:0.04 mM), and administered by intramuscular injection in the quadriceps femoral muscle of male Wistar rats. After a single dose of 0.2 mg diclofenac formulations the local tissue damage was assessed by plasma creatine kinase (CPK) activity and histological analysis. It was demonstrated that formulations containing free diclofenac produced a higher increase in CPK activity, while those encapsulated in liposomes exhibited CPK activity similar to the control groups. Histopathological analysis of local muscle tissue performed on the third and seventh days following the injection showed intense cellular damage when free drug solution was used, while encapsulation in liposome protected the tissue against the local tissue inflammation. 相似文献
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Liposomes are intensively being developed for biomedical applications including drug and gene delivery. However, targeted liposomal delivery in cancer treatment is a very complicated multistep process. Unfavorable liposome biodistribution upon intravenous administration and membrane destabilization in blood circulation could result in only a very small fraction of cargo reaching the tumors. It would therefore be desirable to develop new quantitative strategies to track liposomal delivery systems to improve the therapeutic index and decrease systemic toxicity. Here, we developed a simple and nonradiative method to quantify the tumor uptake of targeted and nontargeted control liposomes as well as their encapsulated contents simultaneously. Specifically, four different chelated lanthanide metals were encapsulated or surface-conjugated onto tumor-targeted and nontargeted liposomes, respectively. The two liposome formulations were then injected into tumor-bearing mice simultaneously, and their tumor delivery was determined quantitatively via inductively coupled plasma mass spectroscopy (ICPMS), allowing for direct comparisons. Tumor uptake of the liposomes themselves and their encapsulated contents was consistent with targeted and nontargeted liposome formulations that were injected individually. 相似文献
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水泥粒度分布对水泥性能影响的研究进展 总被引:1,自引:0,他引:1
从两个方面总结了水泥粒度分布对水泥性能影响的研究进展,一方面总结了反映水泥颗粒群整体情况的特征参数比表面积S、特征粒径x′和均匀性指数n对水泥性能的影响;另一方面总结了不同粒径区间水泥颗粒的性能。介绍了描述水泥粒度分布的RRB方程和Fuller曲线,综述了理论上粒度分布对水泥性能的影响情况,认为水泥的粒度分布是与其性能有明确定量关系的细度参数,是水泥粉磨细度控制的最终目标。 相似文献
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Ti-Fe nanoparticles with different concentrations were synthesized by gas condensation method.It is found that the size distribution of single phase nanoparticles obeys log normal distribution,and that of multiple phase nanoparticles is quite different. If it is assumed that the size distribution of each phase in multiple phase nanoparticles obeys log normal distribution as that of single phase particles. the calculated distribution curve is agreeable to the empirical curve. The inferences from the hypothesis are also supported by experimental results 相似文献
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P. L. Madan 《Drug development and industrial pharmacy》1976,2(6):495-504
The effect of particle size distribution on the dissolution of salicylic acid in an automated dissolution apparatus has been studied. Tablets were prepared by individually weighing 200 mg of the drug particles having a narrow size distribution, compressing the tablets using a hydraulic press and employing identical compression force for the same time period for each tablet. The results showed that the range values obtained were not significantly different from those obtained when the particle size was not controlled. However, the range values obtained from the dissolution of drug particles recovered from the tablet formulation were found to be similar to the range values obtained from the dissolution of the tablet formulation, indicating that compression during tabletting was responsible for observed differences. 相似文献
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Toshiyuki Kosobe Eiji Moriyama Yoshikazu Tokuoka Norimichi Kawashima 《Drug development and industrial pharmacy》2013,39(7):623-629
5-Aminolevulinic acid (ALA)-containing liposomes having various average diameters and/or positive surface charges were prepared, and their photodynamic therapy (PDT) efficacy for murine thymic lymphoma cells, EL-4 cells, cultivated in vitro was investigated. The PDT efficacy for EL-4 cells and the accumulation of ALA-induced protoporphyrin IX (PpIX) in the cells increased with a decrease in the average diameter of liposomes. In particular, the ALA-containing liposomes smaller than 63.5 nm in diameter promoted the PDT efficacy in comparison with that of ALA alone. We also found no significant changes in PDT efficacy and PpIX accumulation with increasing positive surface charges of liposomes. 相似文献