文章：Mannosylation of budesonide palmitate nanoprodrugs for improved macrophage targeting作家：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资料友链：//www.sciencedirect.com/science/article/abs/pii/S0939641121003507提要：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.

要增进糖皮料皮质激素（GC）在调理中的巨噬癌细胞靶向口服药物性，结构设计新一种由珠露糖有些装饰的布地奈德棕榈酸酯纳米技术口服药物。布地奈德棕榈酸酯（BP）的制作而成是完成1,2-二硬脂酰-sn-甘油-3-磷酸乙酸乙酯胺（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）不良反应赚取的。完成精华液减压蒸馏制作微米颗粒剂，并在BP微米食用的药物的调料配方中带来各种不同比例图的杨枝糖基化脂质。适用多达75%的DSPE PEG man（75/25）可获得到多分散性数据达不到0.2的200 nm顆粒，负ζ电极电位条件为-10至-30 mV，在4°C下稳固一名月。BP的包封成功率相当100%，声明书前药与顆粒关干，从而BP环境下量为50%至60%（w/w）。凝集素凝集试验报告表明了珠露糖在纳米级抗癫痫药物面上的能作性。实现共集焦光学显微镜和流式的血血细胞术留意RAW 264.7巨噬血血细胞对微米前药的摄入。在孵育24和48几小时后，与PEG化微米顆粒相较于，珠露糖基化微米顆粒的内化非常明显较大。甘霖聚糖抑止探析验证了甘霖糖蛋白激酶介导的摄入。孵育48个小时后，受损细胞要素（MCP-1和TNFα）极大减少，反映出纳米级药材的效果化是也许 和行之有效的。相应的推送：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以上的软文网站内容來源常见中文核心期刊或学术论文，深表歉意知识产权侵权请沟通公司误删！