脂质体的理化特性对其局部给药后的抗再狭窄效果具有决定性作用。
Physicochemical characteristics of liposomes are decisive for their antirestenosis efficacy following local delivery.
机构信息
Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Tehran Heart Center, Tehran University of Medical Sciences, Tehran, Iran.
出版信息
Nanomedicine (Lond). 2017 Jan;12(2):131-145. doi: 10.2217/nnm-2016-0294. Epub 2016 Nov 23.
AIM
To develop an ameliorated sirolimus (SIR) liposome for intramural delivery, the effects of various carrier physicochemical parameters on the antirestenosis efficacy were evaluated.
MATERIALS & METHODS: Different liposomes were prepared, characterized and administered to balloon injured rats (12 animal groups). Their efficacies were investigated using morphometric, immunohistochemical and in vivo computed tomography imaging analyses.
RESULTS
The antirestenosis efficacy of SIR liposomes decreased in the following order: cationic 100 nm vesicles ≥ cationic 60 nm vesicles > neutral 100 nm vesicles ≥ stealth 100 nm vesicles > anionic 100 nm vesicles. The 100 µg SIR loaded in cationic liposomes showed almost no artery stenosis.
CONCLUSION
Appropriate modulation of physicochemical characteristics makes it possible to optimize the liposomes for local delivery.
目的
为了开发一种改良的西罗莫司（SIR）脂质体用于腔内给药，评估了各种载体物理化学参数对抗再狭窄效果的影响。
材料与方法
制备了不同的脂质体，对其进行了表征，并用于球囊损伤大鼠（12 个动物组）。通过形态计量学、免疫组织化学和体内计算机断层扫描成像分析研究了它们的疗效。
结果
SIR 脂质体的抗再狭窄效果按以下顺序降低：阳离子 100nm 囊泡≥阳离子 60nm 囊泡＞中性 100nm 囊泡＞隐形 100nm 囊泡＞阴离子 100nm 囊泡。载有 100µg SIR 的阳离子脂质体几乎没有动脉狭窄。
结论
适当调节物理化学特性使得有可能优化用于局部递送的脂质体。
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