专著：A folate receptor-targeted liposomal formulation for paclitaxel著者：Jun Wu, Qing Liu, Robert J. Lee专著环节： 绪论：A novel liposomal formulation of paclitaxel targeting the folate receptor (FR) was synthesized and characterized. This formulation was designed to overcome vehicle toxicity associated with the traditional Cremophor EL-based formulation and to provide the added advantages of prolonged systemic circulation time and selective targeting of the FR, which is frequently overexpressed on epithelial cancer cells. The formulation had the composition of dipalmitoyl phosphatidylcholine/dimyristoyl phosphatidylglycerol/monomethoxy-polyethylene glycol (PEG)2000-distearoyl phosphatidylethanolamine/folate-PEG3350-distearoyl phosphatidylethanolamine (DPPC/DMPG/mPEG-DSPE/folate-PEG-DSPE) at molar ratios of (85.5:9.5:4.5:0.5) and a drug-to-lipid molar ratio of 1:33. The liposomes were prepared by polycarbonate membrane extrusion. The mean particle size of the liposomes was 97.1 nm and remained stable for at least 72 h at 4 °C. FR-targeted liposomes of the same lipid composition entrapping calcein were shown to be efficiently taken up by KB oral carcinoma cells, which are highly FR+. FR-targeted liposomes containing paclitaxel showed 3.8-fold greater cytotoxicity compared to non-targeted control liposomes in KB cells. Plasma clearance profiles of paclitaxel in the liposomal formulations were then compared to paclitaxel in Cremophor EL formulation. The liposomal formulations showed much longer terminal half-lives (12.33 and 14.23 h for FR-targeted and non-targeted liposomes, respectively) than paclitaxel in Cremophor EL (1.78 h). In conclusion, the paclitaxel formulation described in this study has substantial stability and favorable pharmacokinetic properties. The FR-targeted paclitaxel formulation is potentially useful for treatment of FR+ tumors and warrants further investigation.

合出并研究方法了了种靶点叶酸片感觉（FR）的紫杉醇脂质体系剂。该药品旨在通过刻服与中国传统的针对Cremophor EL的药品一些的承载毒素，并能提供延伸整体循环往复时候和挑选性靶点FR的30%优越，FR在皮组织上隔三差五过描述。该剂型的组合为二棕榈酰磷脂酰胆碱/二肉肉豆蔻酰磷脂酰甘油/单甲氧基聚乙二醇（PEG）2000二硬脂酰磷脂酰乙酸乙酯胺/孕妇DHA-PEG3350-二硬脂酰膦酰乙酸乙酯胺（DPPC/DMPG/mPEG-DSPE/孕妇DHA-PEG-DSPE），摩尔之比（85.5:9.5:4.5:0.5），药物治疗与脂质摩尔之比1:33。脂质体经过pc聚碳酸酯膜熔融挤出光催化原理。脂质体的分別比表面积为97.1 nm，在4°C下做到稳定性不低于72h。包埋钙黄绿素的相同之处脂质组建的FR靶点脂质体被极度FR+的KB细胞膜合理有效汲取。在KB体生殖细胞中，具有紫杉醇的FR靶点脂质体的体生殖细胞致毒在靶点相较相对脂质体的3.8倍。其次将脂质体系剂中紫杉醇的血浆解决率与Cremophor EL注射剂中的紫杉醇实行相对。脂质管理体溶液剂的终末半衰期（FR靶点治疗和非靶点治疗脂质体分辨为12.33和14.231天）比Cremophor EL中的紫杉醇（1.781天）长得多。尽管，本研究分析中分析的紫杉醇溶液剂具备着一定的稳固性和良好的的药代能源学特质。相应选择：Cy5-PEG-DPPECy7-DOPECy7-DPPECy7-DSPECy7-PEG-DOPECy7-PEG-DPPEDSPE-PEG-Cy7DSPE-PEG-cRGDDPPE-PEG-cRGDDMPE-PEG-cRGDDOPE-PEG-cRGD综上所述句子介绍源常见刊物或论文，深表歉意侵权案请联络我们大家清空！