论文部分内容阅读
目的:研究载阿霉素离子交换型微球的制备和体内、外性质。方法:采用反相悬浮聚合法制备聚乙烯醇-丙烯酸(polyvinylalcohol-acrylic acid,PVA-AA)微球,以阿霉素为模型药物,制备载阿霉素的离子交换微球并测定其载药量、包封率。利用光学显微镜、环境扫描电镜、傅里叶转换红外光谱分析仪、物性分析仪分别考察空白及载药微球的形态、结构以及弹性性质,通过T型装置对载阿霉素微球的体外释药性质进行考察。以家兔右颈外动脉为栓塞模型,评价微球在实验动物体内的栓塞效果。结果:通过反相悬浮聚合法制备的PVA-AA微球外观透明、形态圆整;红外光谱证实了PVA和AA的聚合交联;20 min的载药量为(20.56±0.69)g/L,阿霉素包封率达82.22%±2.76%,6 h的载药量为(23.25±0.27)g/L,阿霉素包封率达93.00%±1.06%,载药后的微球呈红色;PVA-AA微球载药前后的杨氏模量分别为(178.30±12.33)kPa和(213.29±15.61)kPa(1 mmHg=0.133 kPa),载药前后均具有良好的抗形变能力,压缩形变至97%时仍未破裂;载阿霉素的微球在去离子水中不释放药物,在磷酸缓冲液中缓慢释放药物,24 h的累积释放量为10.32%±0.47%。0.3 mL空白微球注入家兔颈外动脉后,可成功地实现末端栓塞。结论:载阿霉素离子交换微球有望成为一种新型的经动脉化疗栓塞剂。
Objective: To study the preparation, in vitro and in vivo properties of doxorubicin-containing ion exchange microspheres. Methods: Polyvinylalcohol-acrylic acid (PVA-AA) microspheres were prepared by reversed-phase suspension polymerization. Doxorubicin-loaded ion exchange microspheres were prepared using doxorubicin as a model drug and their drug-loading Volume, encapsulation efficiency. The morphologies, structures and elastic properties of blank and loaded microspheres were investigated by optical microscope, environmental scanning electron microscopy, Fourier transform infrared spectroscopy and physical property analyzer respectively. The in vitro release of doxorubicin-loaded microspheres by T-type device was investigated. Investigate the nature of the drug. The rabbit right external carotid artery was used as an embolization model to evaluate the embolization effect of microspheres in experimental animals. Results: The appearance of PVA-AA microspheres prepared by reversed-phase suspension polymerization was transparent and round in shape. The polymerization and cross-linking of PVA and AA were confirmed by FTIR. The drug loading of 20 min was (20.56 ± 0.69) g / L, The entrapment efficiency of doxorubicin was 82.22% ± 2.76%, the drug loading of 6 h was (23.25 ± 0.27) g / L, the doxorubicin encapsulation efficiency was 93.00% ± 1.06%, and the drug-loaded microspheres were red . The Young’s modulus of PVA-AA microspheres before and after drug loading were (178.30 ± 12.33) kPa and (213.29 ± 15.61) kPa (1 mmHg = 0.133 kPa), respectively. Up to 97%. The doxorubicin-loaded microspheres did not release drug in deionized water and the drug was slowly released in phosphate buffered saline. The 24 h cumulative release was 10.32% ± 0.47%. 0.3 mL blank microspheres injected into the rabbit external carotid artery, the successful implementation of the terminal embolization. Conclusion: Adriamycin-loaded ion exchange microspheres are expected to become a new type of transcatheter arterial chemoembolization.