【摘 要】
：
Objective: To investigate the effect of phospholipid composition on cellular uptake of lipid-PLGA hybrid nanoparticles.Methods: Coumarin-6 loaded lipid-PLGA hybrid nanoparticles with different phospho
【机 构】
：
Xiangya School of Pharmaceutical Sciences,Central South University, Changsha 410013, Hunan, China;Sc
论文部分内容阅读
Objective: To investigate the effect of phospholipid composition on cellular uptake of lipid-PLGA hybrid nanoparticles.Methods: Coumarin-6 loaded lipid-PLGA hybrid nanoparticles with different phospholipid composition,such as soy posphatidylcholine (SPC),egg posphatidylcholine (EPC),1,2-dipalmitoyl-sn-glycero-phosphatidylcholine (DPPC),and hydrogenated soy posphatidylcholine (HSPC) were prepared by emulsion-solvent evaporation method and characterized.Cellular uptake of formulations above was examined by flow cytometry.Results: The particle size,polydispersity and encapsulation efficiency (EE %) of formulations were characterized to approximately 150-175 nm,below 0.20 and 85 %,respectively (Tab.1).From Fig.1B,compared to SPC-NP,EPC-NP had higher fluorescence intensity (p<0.01).Both DPPC-NP and HSPC-NP showed higher uptake than that of EPC-NP and SPC-NP (p<0.05 for EPC-NP vs DPPC-NP or HSPC-NP;p<0.01 for SPC-NP vs DPPC-NP or HSPC-NP).However,there was no diversity between DPPC-NP and HSPC-NP.Discussion: It showed that lipid composition had little effect on the particle size,polydispersity and EE values.However,lipid composition had effect on the cell uptake.Both SPC and EPC originated naturally had unsaturated hydrocarbon chains.The phase transition temperature (Tm) of EPC was-8 ℃,higher than that of SPC which was-20 ℃.Both DPPC and HSPC have saturated hydrocarbon chains and higher Tin,41 ℃ and 55 ℃,respectively,which decreased the flexibility of the lipid layer,resulting in a more efficient cell uptake.It demonstrated that the saturation and higher Tm of phospholipid might be beneficial to uptake.But the effect of fluidity resulting from chemical properties of phospholipid on cell-particle interaction should be expounded further.It may have important implications for designing drug nanocarriers.
其他文献
以软材质量、颗粒质量、片剂质量等为评价指标,采用单因素法和Box-Behnken设计结合响应面法优化铁皮石斛超微粉泡腾片的处方.所得优化处方为：铁皮石斛超微粉44.5％、无水葡萄糖25％、碳酸氢钠15％和枸橼酸15％,以7％聚乙烯吡咯烷酮(PVP K30)的95％乙醇溶液为黏合剂湿法制粒,干燥至含水量小于3％,最后加硬脂酸镁0.5％混匀后压片.所得泡腾片崩解时间为2.1 min,溶解后pH值为6.
[目的]热敏聚合物即温度敏感聚合物,作为生物医学材料尤其是靶向药物输送系统已经得到广泛关注；为了评价热敏聚合物作为药物载体的安全性和生物相容性,本文重在研究基于水溶性多肽的热敏聚合物(其表现出低临界溶解温度(LCST)或高临界溶解温度(UCST)相的行为类型)对人脐静脉内皮细胞的细胞毒性、氧化损伤和炎症反应。[方法]人脐静脉内皮细胞暴露于100 μg/ml热敏聚合物PPLG-g-OEG2、PPLG
目的 制备灯盏花素聚乙二醇维生素E琥珀酸酯(TPGS)聚合物胶束,并对其体外释放特性和大鼠体内的药动学特征进行研究.方法 采用薄膜溶剂挥发法制备聚合物胶束,考察其形态、粒径、Zeta电位、包封率和载药量；采用动态膜透析法考察胶束的体外释药特性；大鼠静脉给药考察其体内药动学特征.结果 薄膜溶剂挥发法制备的胶束呈球形或类球形,粒径为(20±2.62) nm,Zeta电位0 mV左右,包封率和载药量分别
目的 利用层层自组装(LBL)技术[1],制成一种外层包裹普鲁兰多糖,由聚赖氨酸(PLL)/聚天冬氨酸(PASP)电解质多层膜结构构成的囊状纳米药物载体,搭载二甲双胍,并评价其作为药物载体的特性.方法 以聚赖氨酸作为阳离子、聚天冬氨酸作为阴离子在氨基聚苯乙烯微球表面,通过静电作用进行层层自组装包衣,在包衣的过程中通过电荷的相互作用将带少量正电荷的二甲双胍联合到聚天冬氨酸上使其包载进入纳米囊囊壁,再
目的 优选目安眼用温敏型即型凝胶的基质组成.方法 以相转变温度为考察指标，在单因素试验的基础上，通过星点设计-效应面法筛选目安眼用温敏型即型凝胶处方中泊洛沙姆407、泊洛沙姆188两种基质的配比，采用二项回归分析初步确定基质组成.结果 目安眼用温敏型即型凝胶的最优基质处方为：泊洛沙姆407 19.34％、泊洛沙姆188 1.73％，该基质在25℃下为液体，滴入眼内被泪液稀释后在体温(34℃)下为半
Aim: The main aim of this study is to evaluate the ability of Fluorofenidone to inhibit and induce human cytochrome P450 enzymes in vitro.Methods: The inhibitory effect of AKF-PD on human cytochrome P
目的：作为吡非尼酮的结构类似物,美氟尼酮在临床前研究中显示了良好的抗纤维化活性,具有开发成为新型抗纤维化药物的潜力.本研究主要探讨美氟尼酮在SD大鼠体内的药物动力学特征.方法：单次给药实验,SD大鼠按照31.25、62.5、125、250、500 mg/kg的剂量灌胃给予美氟尼酮生理盐水溶液.重复给药实验,SD大鼠按照62.5mg/kg的剂量每间隔12h灌胃给予美氟尼酮生理盐水溶液,连续给药9次,
目的 应用挤出滚圆法制备盐酸士的宁速释微丸并考察溶出度的影响因素.方法 利用挤出滚圆法制备微丸,设计不同的处方,筛选合适的辅料和粘合剂,使用高效液相色谱仪对制备出的微丸进行测定分析.结果 优化处方是MCC 60 g,蒸馏水96 ml,盐酸士的宁600 mg,乳糖1 g.制备出的微丸具有很好的溶出效果,在30 min时溶出度达到了90％左右,60 min内几乎全部溶出.结论 挤出滚圆法制备的盐酸士的
Objective: Development of chemotherapeutic drugs targeted delivery to tumor cells remains a challenge due to the lower uptake by tumor tissue,and higher exposure of other body compartments to the drug