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目的:探讨纳米载体(PBCA-NP)联合光敏剂(HMME)应用于家兔腹腔淋巴结组织的淋巴靶向性研究。方法:制备血卟啉单甲醚-聚氰基丙烯酸正丁酯纳米载体(HMME-PBCA-NP)并检测纳米粒的理化性质和体外释放情况;将家兔随机分为两组,分别给予腹腔注射相同剂量HMME-DMSO和HMME-PBCA-NP溶液,检测血浆中HMME含量得到血卟啉单甲醚的药物代谢动力学参数,于不同时间点处死家兔,检测不同组织中的HMME含量,得到血卟啉单甲醚的组织药物分布。结果:成功制备出HMME-PBCA-NP纳米胶束,粒径为160nm左右,包封率为87.9%,载药量为13.4%;与单纯血卟啉单甲醚溶液组相比,纳米组家兔血清及组织到达药物峰浓度时间均向后推迟(6h vs 3h);腹腔注射不同剂型药物6h后,药物浓度在家兔肠系膜淋巴组织中的差值达到最大[(1.2884±0.04695)μg/ml vs(0.0438±0.00558)μg/ml],肉眼观察,纳米载体组家兔肠系膜淋巴结明显肿大。结论:纳米粒经过腹腔注射具有缓释作用;载药纳米载体经过腹腔注射途径具有淋巴靶向性作用。
OBJECTIVE: To investigate the lymphatic targeting study of the application of nanocarrier (PBCA-NP) and photosensitizer (HMME) in the abdominal lymph node of rabbits. Methods: Hematoporphyrin monomethyl ether-polybutylcyanoacrylate (HMME-PBCA-NP) was prepared and its physical and chemical properties and in vitro release were tested. The rabbits were randomly divided into two groups, The same dose of HMME-DMSO and HMME-PBCA-NP solution was injected to test the HMME content in plasma to get the pharmacokinetic parameters of hematoporphyrin monomethyl ether. The rabbits were sacrificed at different time points to detect HMME content in different tissues to obtain Hematoporphyrin monomethyl ether tissue drug distribution. Results: The HMME-PBCA-NP nanomicelles were successfully prepared. The particle size was about 160 nm, the entrapment efficiency was 87.9% and the drug loading was 13.4%. Compared with the pure hematoporphyrin monomethyl ether solution group, Rabbit serum and tissue reached the peak drug concentration postponed late (6h vs 3h); intraperitoneal injection of different formulations of drug 6h, the concentration of drug in rabbit mesentery lymphoid tissue to achieve the maximum difference [(1.2884 ± 0.04695) μg / ml vs (0.0438 ± 0.00558) μg / ml]. The macroscopic observation showed that the mesenteric lymph nodes in the nanocarrier group were significantly enlarged. CONCLUSION: The nanoparticles have a sustained-release effect after intraperitoneal injection. The drug-loaded nanocarriers have lymphatic targeting effect via intraperitoneal injection.