雌二醇聚氰基丙烯酸正丁酯纳米粒肝脏靶向性研究

Study on liver targeting of estradiol polybutylcyanoacrylate nanoparticles

目的观察雌二醇纳米粒(E2-PBCA-NP)在正常肝脏中的靶向性,并比较腹腔给药和静脉给药两种给药途径对E2-PBCA-NP肝脏靶向性的影响。方法采用放射示踪技术,用125-I标记雌二醇,界面聚合法制备125-I-E2-PBCA-NP,经腹腔及静脉给药,分别于注药后15、30min、l、2、4、8、l2、24h处死大鼠,取其血、肺、肝、脾、肾、子宫和卵巢作γ计数,并与普通雌二醇组比较。结果125-I-E2-PBCA-NP和125-I-E2肝摄取分别在注射后15min后最高,与125-I-E2比较125-I-E2-PBCA-NP提高了肝脏、脾脏的放射性强度,降低了子宫及卵巢的放射性强度。腹腔给药及尾静脉给药不影响125-I-E2-PBCA-NP的肝脏靶向性(P>0.05)。结论E2-PB-CA-NP具有明显的肝脏靶向性。

[Objective] To observe the hepatic targeting of estradiol polybutylcyanoacrylate nanoparticles （E2-PBCA-NP） and compare the effect of hepatic tagerting after intraperitoneal（IP） and intravenous（Ⅳ） administration. [Methods] Using radioactive tracer technique, estradiol labelled with ^125-Ⅰ,^125-Ⅰ-E2-PBCA-NP was prepared by inteffacial polymerization and was injected into mice through IP and Ⅳ administration. At 15, 30 min, 1, 2, 4, 8, 12, 24 h after administration, the mice were sacrificed. The blood,lung, liver, spleen, kidney, ovary and womb were analyzed for γ counts and then compared with common estradiol groups. [Results] ^125-Ⅰ-E2-PBCA-NP and ^125-Ⅰ-E2 uptaken by liver reached the peak at 15 min after administration drugs. Compared with ^125-Ⅰ-E2, ^125-Ⅰ-E2-PBCA-NP enhanced the radioactivity of liver and spleen and reduced the radioactivity of ovary and womb. There was no significant difference on liver targeting after IV or IP administration of ^125-Ⅰ-E,-PBCA-NP （P 〉0.05）. [Conclusion] E2- PBCA-NP has remarkable hepatic targeting.