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Yuandong Ma Yi Zheng Kexin Liu Ge Tian Yan Tian Lei Xu Fei Yan Laiqiang Huang Lin Mei 《Nanoscale research letters》2010,5(7):1161-1169
Cancer is the leading cause of death worldwide. Nanomaterials and nanotechnologies could provide potential solutions. In this
research, a novel biodegradable poly(lactide-co-glycolide)-d-a-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) random
copolymer was synthesized from lactide, glycolide and d-a-tocopheryl polyethylene glycol 1000 succinate (TPGS) by ring-opening
polymerization using stannous octoate as catalyst. The obtained random copolymers were characterized by 1H NMR, FTIR, GPC and TGA. The docetaxel-loaded nanoparticles made of PLGA-TPGS copolymer were prepared by a modified solvent
extraction/evaporation method. The nanoparticles were then characterized by various state-of-the-art techniques. The results
revealed that the size of PLGA-TPGS nanoparticles was around 250 nm. The docetaxel-loaded PLGA-TPGS nanoparticles could achieve
much faster drug release in comparison with PLGA nanoparticles. In vitro cellular uptakes of such nanoparticles were investigated
by CLSM, demonstrating the fluorescence PLGA-TPGS nanoparticles could be internalized by human cervix carcinoma cells (HeLa).
The results also indicated that PLGA-TPGS-based nanoparticles were biocompatible, and the docetaxel-loaded PLGA-TPGS nanoparticles
had significant cytotoxicity against Hela cells. The cytotoxicity against HeLa cells for PLGA-TPGS nanoparticles was in time-
and concentration-dependent manner. In conclusion, PLGA-TPGS random copolymer could be acted as a novel and promising biocompatible
polymeric matrix material applicable to nanoparticle-based drug delivery system for cancer chemotherapy. 相似文献
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蜜胺甲醛树脂-钯催化剂的制备及其催化氢解氯代苯基中间体合成多西紫杉醇及其异构体侧链的研究 总被引:1,自引:1,他引:0
制备和表征了蜜胺甲醛树脂钯催化剂,通过光电子能谱、顺磁共振谱和X-射线衍射等测试证明新催化剂与Pd^2 络合,起催化作用的是Pd^0,研究发现催化剂的N/Pd原子在25.6-12.8具有较好的催化效果,而催化氢化温度则在35-40℃之间进行更好。蜜胺甲醛树脂的聚合度越高对钯的附载能力越强,催化剂的催化效果超好。该催化剂在常压和室温条件下将氯代苯基化合物催化氢化为苯基化合物,并有很高的催化活性,通过该方法以较高收率制备了多西紫杉醇和异构体侧链。得到了新化合物均经过^1HNMR、^13CNMR、IR、旋光度和元素分析等给予确证,(3S,4R)-3-羟基-N-[(S)-(1-苯基)乙基]-4-(2′-氯苯基)-2-氮杂环丁酮通过X-单晶衍射确定四元环构型为3S,4R型,并进一步确定了其它化合物的结构。 相似文献
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Li-Li Shi Jia Lu Yue Cao Jiang-Yan Liu Xiao-Xue Zhang Hongjian Zhang 《Drug development and industrial pharmacy》2017,43(5):839-846
AbstractObjective: The purpose of this study was to prepare the positively charged chitosan (CS)- or hydroxypropyl trimethyl ammonium chloride chitosan (HACC)-modified solid lipid nanoparticles (SLNs) loading docetaxel (DTX), and to evaluate their properties in vitro and in vivo.Methods: The DTX-loaded SLNs (DTX-SLNs) were prepared through an emulsion solvent evaporation method and further modified with CS or HACC (CS-DTX-SLNs or HACC-DTX-SLNs) via noncovalent interactions. The gastrointestinal (GI) stability, dissolution rate, physicochemical properties and cytotoxicities of SLNs were investigated. In addition, the GI mucosa irritation and oral bioavailability of SLNs were also evaluated in rats.Results: The HACC-DTX-SLNs were highly stable in simulated gastric and intestinal fluids (SGF and SIF). By contrast, the CS-DTX-SLNs were less stable in SIF than in SGF. The drug dissolution remarkably increased when DTX was incorporated into the SLNs, which may be attributed to the change in the crystallinity of DTX and some molecular interactions that occurred between DTX and the carriers. The SLNs showed low toxicity in Caco-2 cells and no GI mucosa irritations were observed in rats. A 2.45-fold increase in the area under the curve of DTX was found in the HACC-DTX-SLN group compared with the DTX group after the modified SLNs were orally administered to rats. However, the oral absorption of DTX-SLN or CS-DTX-SLN group showed no significant difference compared with that of DTX group.Conclusions: The positively charged HACC-DTX-SLNs with a stable particle size could provide the enhanced oral bioavailability of DTX in rats. 相似文献
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《Drug development and industrial pharmacy》2013,39(7):1010-1019
The aim of this research is to develop novel chitosan nanoparticles including cyclodextrins complexes for docetaxel (DTX), evaluate the performance of nanoparticles which could enhance the oral permeability and bioavailability of DTX in vitro and in vivo. DTX/sulfobutylether-β-cyclodextrin inclusion complexes were made and it was the main ingredient to prepare the DTX/sulfobutylether-β-cyclodextrin/chitosan nanoparticles due to their promising physicochemical properties. DTX/sulfobutylether-β-cyclodextrin/chitosan nanoparticles were prepared by the ionic gelation of chitosan with tripolyphosphate in the presence of cyclodextrins. Results indicated that DTX/sulfobutylether-β-cyclodextrin inclusion complexes and docetaxel/sulfobutylether-β-cyclodextrin/chitosan nanoparticles both had good performances in the studies of release and the rat small intestinal absorption in vitro. DTX/sulfobutylether-β-cyclodextrin/chitosan nanoparticles showed preferable capability in improving the small intestinal absorption and inhibiting the efflux of DTX. In pharmacokinetics study, the DTX/sulfobutylether-β-cyclodextrin/chitosan nanoparticles increased the AUC0→t and decreased the clearance significantly, and the oral relative bioavailability of the DTX/sulfobutylether-β-cyclodextrin/chitosan nanoparticles was as high as 1447.53% compared to the pure DTX formulation. The DTX/sulfobutylether-β-cyclodextrin/chitosan nanoparticles prepared in this study have a good prospect for oral administration as an alternative of current DTX formulations. 相似文献
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泰索帝对Lewis肺癌放疗增敏作用的实验研究 总被引:13,自引:0,他引:13
研究了泰索帝(docetaxel)对荷Lewis肺癌C57BL小鼠的放疗增敏作用。给荷Lewis肺癌C57BL小鼠腹腔注射不同剂量的泰索帝12h或48h后进行10Gy局部照射,结果表明,经过泰索帝放疗增敏治疗后肿瘤生长相对速率明显减慢,4个放疗增敏组q值在1.21-1.38之间。研究还显示泰索帝的放疗增敏作用机制是通过将大量增殖期细胞阻滞的G2和M期以及诱导细胞凋亡。本实验提示秦索帝作为放疗增敏剂应用于肺癌的治疗,既发挥了化疗作用,又具有放疗增敏作用,是很有开发潜力的抗肿瘤药物。 相似文献
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Hongbo Chen Yi Zheng Ge Tian Yan Tian Xiaowei Zeng Gan Liu Kexin Liu Lei Li Zhen Li Lin Mei Laiqiang Huang 《Nanoscale research letters》2011,6(1):4
Three types of nanoparticle formulation from biodegradable PLGA-TPGS random copolymer were developed in this research for oral administration of anticancer drugs, which include DMAB-modified PLGA nanoparticles, unmodified PLGA-TPGS nanoparticles and DMAB-modified PLGA-TPGS nanoparticles. Firstly, the PLGA-TPGS random copolymer was synthesized and characterized. DMAB was used to increase retention time at the cell surface, thus increasing the chances of particle uptake and improving oral drug bioavailability. Nanoparticles were found to be of spherical shape with an average particle diameter of around 250 nm. The surface charge of PLGA-TPGS nanoparticles was changed to positive after DMAB modification. The results also showed that the DMAB-modified PLGA-TPGS nanoparticles have significantly higher level of the cellular uptake than that of DMAB-modified PLGA nanoparticles and unmodified PLGA-TPGS nanoparticles. In vitro, cytotoxicity experiment showed advantages of the DMAB-modified PLGA-TPGS nanoparticle formulation over commercial Taxotere® in terms of cytotoxicity against MCF-7 cells. In conclusion, oral chemotherapy by DMAB-modified PLGA-TPGS nanoparticle formulation is an attractive and promising treatment option for patients. 相似文献
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经不对称氨羟基化反应合成多西紫杉醇及其衍生物的新方法研究 总被引:5,自引:0,他引:5
首次用取代肉桂酸酯和叔丁氧基碳酰胺为原料,经改进的Sharphless不对称氨羟基化反应一步得到了多西紫杉醇及其衍生物的侧链,并最终得到了多西紫杉醇和新型抗癌化合物3,4-亚甲二氧基取代多西紫杉醇,该方法是目前合成多西紫杉醇及其衍生物的最简化和较高收率的路线。研究发现Sharphless不对称氨羟基化反应中手性配体、催化剂的用量和比例对原料的转化率、产物的产率等都有影响,当催化剂K2OsO2(OH)4、手性配体(DHQ)2PHAL的摩尔分数分别为原料的4%和5%时更倾向于生成多西紫杉醇衍生物侧链。所有新化合物及其结构均经过^1HNMR、^13CNMR、IR、MS、旋光度和元素分析等给予确证。3,4-OCH2O取代多西紫杉醇的初步药理活性显示具有较好的抗癌活性。 相似文献