专著：Mannosylation of budesonide palmitate nanoprodrugs for improved macrophage targeting笔者：Ludmila Pinheiro do Nascimento a, Nicolas Tsapis a, Franceline Reynaud a b, Didier Desmaële a, Laurence Moine a, Juliette Vergnaud a, Sonia Abreu c, Pierre Chaminade c, Elias Fattal期刊论文联接：//www.sciencedirect.com/science/article/abs/pii/S0939641121003507英文论文：In a strategy to improve macrophage targeting of glucocorticoids (GCs) for anti-inflammatory therapy, a so-called nanoprodrug of budesonide palmitate decorated by mannose moieties was designed. The synthesis of budesonide palmitate (BP) was obtained by esterification and mannosylated lipid (DSPE-PEG-Man) by reacting 1,2-Distearoyl-sn-Glycero-3-Phosphoethanolamine (DSPE)-polyethylene glycol-amine and α-D-mannopyranosylphenyl isothiocyanate (MPITC). Nanoparticles were formulated by emulsion-evaporation and different ratios of mannosylated lipid were introduced in the formulation of BP nanoprodrugs. Using up to 75% of DSPE-PEG-man (75/25) led to 200 nm particles with a polydispersity index below 0.2, a negative zeta potential ranging from −10 to −30 mV, and one-month stability at 4 °C. The encapsulation efficiency of BP approached 100% proving that the prodrug was associated with the particles, leading to a final BP loading of 50-to 60% (w/w). The lectin agglutination test confirmed the availability of mannose on the nanoprodrug surface. Nanoprodrug uptake by RAW 264.7 macrophages was observed by confocal microscopy and flow cytometry. After 24 and 48 h of incubation, a significantly greater internalization of mannosylated nanoparticles as compared to PEGylated nanoparticles was achieved. The mannose receptor-mediated uptake was confirmed by a mannan inhibition study. After LPS-induced inflammation, the anti-inflammatory effect of mannosylated nanoparticles was assessed. After 48 h of incubation, cytokines (MCP-1 and TNFα) were reduced demonstrating that the functionalization of nanoprodrugs is possible and efficient.

要想提升 糖皮面抗生素（GC）在进行治疗中的巨噬组织细胞靶向治疗性，制定好几回种由珠露糖组成部分遮盖的布地奈德棕榈酸酯納米类药。布地奈德棕榈酸酯（BP）的合出是确认1,2-二硬脂酰-sn-甘油-3-磷酸工业乙醇胺（DSPE）-聚乙二醇胺和α-D-吡喃杨枝糖基苯基异硫氰酸酯（MPITC）的酯化和杨枝糖基化脂质（DSPE-PEG-Man）发生反应拿到的。确认保湿乳汽化制取奈米粒状，并在BP奈米药剂的成分中导入与众不同占比的杨枝糖基化脂质。便用达75%的DSPE PEG man（75/25）可获得到多不集中指标值超过0.2的200 nm颗料，负ζ电位差条件为-10至-30 mV，在4°C下不稳定性一款 月。BP的包封效应更加接近100%，证件前药与颗料关于，既定BP短路电流量为50%至60%（w/w）。凝集素凝集试验装置声明了珠露糖在nm制剂接触面的能作性。能够 共集聚显微镜观察分析和流式神经元神经元术观察分析RAW 264.7巨噬神经元对納米前药的摄取量。在孵育24和48半小时后，与PEG化納米颗料相信，甘霖糖基化納米颗料的内化很深更好。甘霖聚糖调节论述查证了甘霖糖蛋白激酶介导的摄取量。孵育48时间后，上皮细胞细胞（MCP-1和TNFα）可以减少，表达纳米技术肿瘤药物的功能键化是可能和管用的。关联介绍：AC-PEG-COOHAlKyne-PEG-COOHCOOH-PEG-EPOCOOH-PEG-MACOOH-PEG-N3CHO-PEG-COOHBiotin-PEG-COOHFmoc-NH-PEG-COOHBoc-NH-PEG-COOHMal-PEG-COOHSH-PEG-COOHNH2-PEG-COOH以上的的文章內容来源地特殊刊物或文献综述，烦请侵犯著作权请联系起来.我删出！