阴阳离子聚氨酯/羟基磷灰石复合微球的制备及其自组装

分别以2,2-双羟基丙酸(DMPA)和N-甲基二乙醇胺(MDEA)作扩链剂,采用自乳化法成功制备出带有正、负电荷的阳、阴离子聚氨酯/羟基磷灰石(PU/HA)微球,并考察HA的复合比例对微球形貌、理化性能的影响。在此基础上,通过微球间的静电作用力,将制备出的阴、阳离子复合微球自组装形成凝胶体系,并对其力学性能进行探究。SEM、ζ电位和激光粒度结果显示成功制备出具有一定形貌的带电微球,其中当扩链剂含量为15%(n/n)、HA含量为10%(w/w)时,微球形貌较佳且粒度分布均匀;X射线衍射、热分析结果表明,微球确为一定比例的HA与PU复合产物;自组装体系的流变学测试结果表明,微球组装后的产物呈类凝胶状态,具有较高的弹性模量,并有一定的可注射性。同时,骨髓间充质干细胞(BMSCs)可在组装材料表面粘附、铺展,生长良好。     

Enhanced Antioxidant and Anti-Inflammatory Effects of Self-Nano and Microemulsifying Drug Delivery Systems Containing Curcumin

Turmeric has been used for decades for its antioxidant and anti-inflammatory effect, which is due to an active ingredient isolated from the plant, called curcumin. However, the extremely poor water-solubility of curcumin often limits the bioavailability of the drug. The aim of our experimental work was to improve the solubility and thus bioavailability of curcumin by developing self-nano/microemulsifying drug delivery systems (SN/MEDDS). Labrasol and Cremophor RH 40 as nonionic surfactants, Transcutol P as co-surfactant and isopropyl myristate as the oily phase were used during the formulation. The average droplet size of SN/MEDDS containing curcumin was between 32 and 405 nm. It was found that the higher oil content resulted in larger particle size. The drug loading efficiency was between 93.11% and 99.12% and all formulations were thermodynamically stable. The curcumin release was studied at pH 6.8, and the release efficiency ranged between 57.3% and 80.9% after 180 min. The results of the MTT cytotoxicity assay on human keratinocyte cells (HaCaT) and colorectal adenocarcinoma cells (Caco-2) showed that the curcumin-containing preparations were non-cytotoxic at 5 w/v%. According to the results of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide dismutase (SOD) assays, SNEDDS showed significantly higher antioxidant activity. The anti-inflammatory effect of the SN/MEDDS was screened by enzyme-linked immunosorbent assay (ELISA). SNEDDS formulated with Labrasol as surfactant, reduced tumor necrosis factor-alpha (TNF-α) and interleukin-1 beta (IL-1β) levels below 60% at a concentration of 10 w/w%. Our results verified the promising use of SN/MEDDS for the delivery of curcumin. This study demonstrates that the SN/MEDDS could be promising alternatives for the formulation of poorly soluble lipophilic compounds with low bioavailability.     

阴阳离子聚氨酯/羟基磷灰石复合微球的制备及其自组装

分别以2,2-双羟基丙酸(DMPA)和N-甲基二乙醇胺(MDEA)作扩链剂,采用自乳化法成功制备出带有正、负电荷的阳、阴离子聚氨酯/羟基磷灰石(PU/HA)微球,并考察HA的复合比例对微球形貌、理化性能的影响。在此基础上,通过微球间的静电作用力,将制备出的阴、阳离子复合微球自组装形成凝胶体系,并对其力学性能进行探究。SEM、ζ电位和激光粒度结果显示成功制备出具有一定形貌的带电微球,其中当扩链剂含量为15%(n/n)、HA含量为10%(w/w)时,微球形貌较佳且粒度分布均匀;X射线衍射、热分析结果表明,微球确为一定比例的HA与PU复合产物;自组装体系的流变学测试结果表明,微球组装后的产物呈类凝胶状态,具有较高的弹性模量,并有一定的可注射性。同时,骨髓间充质干细胞(BMSCs)可在组装材料表面粘附、铺展,生长良好。     

水溶性AM-St两亲嵌段共聚物的自乳化微乳液法合成

水溶性AM-St两亲嵌段共聚物的自乳化微乳液法合成;丙烯酰胺;苯乙烯;疏水缔合共聚物