目的:以伊文思蓝为被包封物制备聚乳酸(LA)-羟基乙酸(GA)-聚乙二醇(PEG)嵌段共聚物(PLGA-PEG,PLGE)多孔载药微球,并研究超声波对药物体外释放的影响。方法:以LA-GA-PEG(63.00∶27.50∶9.50,m/m/m)为原料制备PLGE;以二氯甲烷为有机相,采...目的:以伊文思蓝为被包封物制备聚乳酸(LA)-羟基乙酸(GA)-聚乙二醇(PEG)嵌段共聚物(PLGA-PEG,PLGE)多孔载药微球,并研究超声波对药物体外释放的影响。方法:以LA-GA-PEG(63.00∶27.50∶9.50,m/m/m)为原料制备PLGE;以二氯甲烷为有机相,采用复乳法制备PLGE包封的伊文思蓝多孔载药微球。采用扫描电子显微镜对载药微球的形态进行观察;采用紫外分光光度法测定伊文思蓝的载药量和包封率;考察低频率(20 k Hz,40 W)超声波对其药物累积释放度的影响。结果:所制备的多孔载药微球成球规整,彼此不粘连,表面孔隙均匀,载药量为0.38%,包封率为89.92%;15 min时的累积释放度在超声和未超声条件下分别为2.76、0.91μg/mg。结论:PLGE可用作微球药物的载体,低频率超声波可促进微球内药物的释放。展开更多
A novel vehicle for the delivery of aspirin (ASA) was prepared from porous nano-hydroxyapafite/poly(styrene-divinylbenzene) [nano-HAP/P(St-DVB)] composite microspheres by grafting nano-HAP [Ca10(PO4)6(OH)2] ...A novel vehicle for the delivery of aspirin (ASA) was prepared from porous nano-hydroxyapafite/poly(styrene-divinylbenzene) [nano-HAP/P(St-DVB)] composite microspheres by grafting nano-HAP [Ca10(PO4)6(OH)2] onto porous P(St-DVB) micro- spheres. Four types of porous composite microspheres were prepared, each with different nano-HAP contents. The ASA-loaded composite microspheres prepared with 10% and 15% nano-HAP (mass ratio) exhibited excellent buoyancy with relatively short instantaneous floating time (within l0 min) and a long sustained floating time (12 h) in simulated gastric juice. They also offered good sustained release of ASA (up to 8 h). Furthermore, these composite microspheres displayed good buff- ering capacity that prevented the buildup of acidity caused by hydrolysis of ASA, keeping the pH of gastric juice within the normal range (pH 0.9 to 1.5). The results showed that porous nano-HAP/P(St-DVB) composite microspheres prepared with 10% and 15% nano-HAP could be used as a novel drug carrier for ASA, providing a sustained release dose without leading to stomach irritation, a side effect that is often associated with ASA medication.展开更多
文摘目的:以伊文思蓝为被包封物制备聚乳酸(LA)-羟基乙酸(GA)-聚乙二醇(PEG)嵌段共聚物(PLGA-PEG,PLGE)多孔载药微球,并研究超声波对药物体外释放的影响。方法:以LA-GA-PEG(63.00∶27.50∶9.50,m/m/m)为原料制备PLGE;以二氯甲烷为有机相,采用复乳法制备PLGE包封的伊文思蓝多孔载药微球。采用扫描电子显微镜对载药微球的形态进行观察;采用紫外分光光度法测定伊文思蓝的载药量和包封率;考察低频率(20 k Hz,40 W)超声波对其药物累积释放度的影响。结果:所制备的多孔载药微球成球规整,彼此不粘连,表面孔隙均匀,载药量为0.38%,包封率为89.92%;15 min时的累积释放度在超声和未超声条件下分别为2.76、0.91μg/mg。结论:PLGE可用作微球药物的载体,低频率超声波可促进微球内药物的释放。
基金financially supported by the Young Scientists Fund of the Natural Science Foundation of Heilongjiang Province (QC2011C099)Scientific Fund of Heilongjiang Province Department of Health (2009-259)+3 种基金Grant from Educational Office of Heilongjiang Province (11551178 and1154HZ11)Fund of Daqing GaoXin Qu (DQGX09YF016)the National Natural Science Foundation of China (30871007)the Natural Science Foundation of Heilongjiang Province (ZD2008-08 and LC2009C12)
文摘A novel vehicle for the delivery of aspirin (ASA) was prepared from porous nano-hydroxyapafite/poly(styrene-divinylbenzene) [nano-HAP/P(St-DVB)] composite microspheres by grafting nano-HAP [Ca10(PO4)6(OH)2] onto porous P(St-DVB) micro- spheres. Four types of porous composite microspheres were prepared, each with different nano-HAP contents. The ASA-loaded composite microspheres prepared with 10% and 15% nano-HAP (mass ratio) exhibited excellent buoyancy with relatively short instantaneous floating time (within l0 min) and a long sustained floating time (12 h) in simulated gastric juice. They also offered good sustained release of ASA (up to 8 h). Furthermore, these composite microspheres displayed good buff- ering capacity that prevented the buildup of acidity caused by hydrolysis of ASA, keeping the pH of gastric juice within the normal range (pH 0.9 to 1.5). The results showed that porous nano-HAP/P(St-DVB) composite microspheres prepared with 10% and 15% nano-HAP could be used as a novel drug carrier for ASA, providing a sustained release dose without leading to stomach irritation, a side effect that is often associated with ASA medication.