Preparation of technetium labeled docetaxel liposome and its distribution in rabbits

刘宇; 邱峰; 吕志祥; 兰作平; 张梨; 王杰; 余瑜

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Preparation of technetium labeled docetaxel liposome and its distribution in rabbits

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- Preparation of technetium labeled docetaxel liposome and its distribution in rabbits
- Journal of Army Medical University Vol. 38, Issue 21, Pages: 2303-2308(2016)
- 作者机构：
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  CLC： R817.9;R944.9;R969.1
- Published：2016
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刘宇,邱峰,吕志祥,兰作平,张梨,王杰,余瑜.99m锝标记多西他赛脂质体的制备及其在兔体内的组织分布研究[J].陆军军医大学学报(原第三军医大学学报),2016,38(21):2303-2308.

　Liu Yu,Qiu Feng,Lyu Zhixiang,Lan Zuoping,Zhang Li,Wang Jie,Yu Yu.Preparation of technetium labeled docetaxel liposome and its distribution in rabbits[J].J Amry Med Univ (J Third Mil Med Univ),2016,38(21):2303-2308.
刘宇,邱峰,吕志祥,兰作平,张梨,王杰,余瑜.99m锝标记多西他赛脂质体的制备及其在兔体内的组织分布研究[J].陆军军医大学学报(原第三军医大学学报),2016,38(21):2303-2308. DOI：

　Liu Yu,Qiu Feng,Lyu Zhixiang,Lan Zuoping,Zhang Li,Wang Jie,Yu Yu.Preparation of technetium labeled docetaxel liposome and its distribution in rabbits[J].J Amry Med Univ (J Third Mil Med Univ),2016,38(21):2303-2308. DOI：

摘要

目的考察多西他赛脂质体（DTX-LP）在兔体内的生物分布及其在各主要脏器的靶向参数。方法通过固体分散与泡腾组合技术，使用放射性同位素锝（

99m

TC）对DTX-LP进行标记（DTX-LP-

99m

TC）。考察DTX-LP-

99m

TC的外观、粒径、Zeta电荷、包封率、载药量以及放射化学纯度及稳定性。将DTX-LP-

99m

TC或游离锝（

99m

TC-Free）经耳缘静脉注射入兔体内，经SPECT/CT静态采集数据及计算机融合显像获得DTX-LP-

99m

TC及

99m

TC-Free在兔体内的放射性影像。另将注射DTX-LP-

99m

TC或

99m

TC-Free的兔分别于给药后1、2、4、8、12 h处死，使用甲状腺功能测定仪采集兔各离体器官的放射性计数，并计算各脏器的相对摄取率（Re）和靶向效率（Te）。结果 DTX-LP-

99m

TC平均粒径为726 nm，Zeta电荷为-35.6 mV，包封率及载药量分别为（90.27±1.15）%和（1.30±0.20）%。在室温放置或兔血清中37 ℃温育1、4、12 h后，DTX-LP-

99m

TC的放射化学纯度分别为98.45%、96.32%、94.28%及96.78%、93.45%、91.56%。放射性影像显示DTX-LP-

99m

TC在兔肺浓聚；每克兔组织的放射性计数由高到低排列，在DTX-LP-99mTC组为肺、脾、肝、肾、心、脑，在

99m

TC-Free组为肝、脾、肾、心、肺、脑，同一时间点相同脏器的放射性计数在两组之间差异有统计学意义（P0.01）。Re值表明，DTX-LP

99m

TC组在肺、脾和脑的放射性计数分别是

99m

TC-Free组的64.41、1.62倍和1.57倍，而心、肝、肾的放射性计数较

99m

TC-Free组明显减少。Te值表明，DTX-LP-

99m

TC在兔肺的放射性计数是脑的64.01倍，心的40.73倍，肾的14.01倍，肝的3.22倍。结论 DTX-LP主要浓集在兔肺，具有高度的肺靶向性。

Abstract

Objective To investigate the ti

ssue distribution of docetaxel liposome (DTX-LP) in rabbits. Methods DTX-LP was labeled with 99mTC (DTX-LP-

99m

TC) by solid dispersion and effervescent techniques. The appearance

particle size

Zeta potential

encapsulation efficiency

drug loading rate and radiochemical purity of DTX-LP-

99m

TC were investigated. DTX-LP-

99m

TC or

99m

TC-Free was injected to rabbits through ear vein

respectively. Then the rabbits were scanned with SPECT/CT to obtain the three-dimensional radioactive images. The rabbits were sacrificed at 1

8 and 12 h after injection

and the heart

liver

spleen

lungs

kidneys and brain were harvested. The radioactive counts (RC) of these organs were detected using thyroid function tester. According to RC

the average relative uptake rate (Re) and average targeting efficiency (Te) of each organ were calculated. ResultsDTX-LP-

99m

TC was in spherical shape

at a particle size of 726 nm and with a Zeta potential of -35.6 mV. Its encapsulation efficiency and drug loading rate were (90.27±1.15)% and (1.30±0.20)%

respectively. After placing at room temperature for 1

4 and 12 h

the radiochemical purity of DTX-LP-

99m

TC was 98.45%

96.32% and 94.28%

respectively

while it was 96.78%

93.45% and 91.56% separately after being incubated at 37 ℃ in rabbit serum. The radioactive enriched image of lung was observed in the rabbits injected with DTX-LP-

99m

TC. RC of per gram tissue in the DTX-LP-

99m

TC group was reduced in the lungs

spleen

liver

kidneys

heart and brain in order. In contrast

it was in the liver

spleen

kidneys

heart

lungs and brain in the

99m

TC-Free group. At the same time

RC of the same organ were significant different between DTX-LP-

99m

TC group and 99mTC-free group (P0.01). Re showed that the RC of the lungs

spleen and brain were by 64.41

1.62 and 1.57 times higher in the DTX-LP-

99m

TC group than the

99m

TC-Free group

respectively. But the RC of

the heart

liver and kidneys in DTX-LP-

99m

TC group were significantly lower than that of

99m

TC-Free group. In the DTX-LP-

99m

TC group

the RC of lung was 64.01 times higher than that of the brain

40.73 times higher than that of the heart

14.01 times than that of the kidneys and 3.22 times than that of the liver

respectively. Conclusion DTX-LP is accumulated in the rabbit’s lungs

showing excellent lung-targeting effect.

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