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阿霉素载脂肽酰乙醇胺偶联纳米脂质体的体外特性及其在大鼠肝、肾和肺中的蓄积。

Doxorubicin-loaded phosphatidylethanolamine-conjugated nanoliposomes: in vitro characterization and their accumulation in liver, kidneys, and lungs in rats.

机构信息

Department of Pharmaceutical Technology, Jadavpur University, Kolkata (Calcutta), India.

出版信息

Int J Nanomedicine. 2010 Oct 21;5:811-23. doi: 10.2147/IJN.S13031.

DOI:10.2147/IJN.S13031
PMID:21042545
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2963929/
Abstract

INTRODUCTION

Phosphatidylethanolamine (PE)-conjugated nanoliposomes were developed, characterized, and investigated for their accumulation in liver, kidneys, and lungs in rats.

METHODS

Drug-excipient interaction was studied using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), surface morphology by field emission scanning electron microscopy, elemental analysis by energy dispersive X-ray (EDX) analysis, zeta potential and size distribution using a Zetasizer and particle size analyzer, and in vitro drug release by dialysis membrane. In vivo accumulation of liposomes in tissues was also studied.

RESULTS

No chemical reaction was observed between drug and excipients. EDX study confirmed PE-conjugation in liposomes. Doxorubicin-loaded liposomes (DOX-L) and PE-conjugated doxorubicin-loaded liposomes (DOX-PEL) were of smooth surface and homogenously distributed in nanosize range (32-37 nm) with a negative surface charge. Loading efficiencies were 49.25% ± 1.05% and 52.98% ± 3.22% respectively, for DOX-L and DOX-PEL. In vitro drug release study showed 69.91% ± 1.05% and 77.07% ± 1.02% doxorubicin released, from DOX-L and DOX-PEL, respectively, in nine hours. Fluorescence microscopic study showed that liposomes were well distributed in liver, lungs, and kidneys.

CONCLUSION

Data suggests that PE-conjugated nanoliposomes released the drug in a sustained manner and were capable of distributing them in various organs. This may be used for cell/ tissue targeting, attaching specific antibodies to PE.

摘要

简介

研制了磷脂酰乙醇胺（PE）缀合的纳米脂质体，并对其在大鼠肝脏、肾脏和肺部的积累进行了特征描述和研究。

方法

使用傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）、场发射扫描电子显微镜的表面形态、能量色散 X 射线（EDX）分析的元素分析、Zetasizer 和粒度分析仪的动电位和粒径分布以及体外药物释放研究了药物-赋形剂相互作用。还研究了脂质体在体内组织中的积累。

结果

药物和赋形剂之间未观察到化学反应。EDX 研究证实了脂质体中的 PE 缀合。多柔比星负载脂质体（DOX-L）和 PE 缀合的多柔比星负载脂质体（DOX-PEL）具有光滑的表面，均匀分布在纳米范围内（32-37nm），带负电荷。DOX-L 和 DOX-PEL 的载药量分别为 49.25%±1.05%和 52.98%±3.22%。体外药物释放研究表明，DOX-L 和 DOX-PEL 分别在 9 小时内释放了 69.91%±1.05%和 77.07%±1.02%的多柔比星。荧光显微镜研究表明，脂质体在肝脏、肺和肾脏中分布良好。

结论

数据表明，PE 缀合的纳米脂质体以持续的方式释放药物，并能够将其分布在各种器官中。这可用于细胞/组织靶向，将特定抗体附着到 PE 上。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1286/2963929/c42cf981de2e/ijn-5-811f9.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1286/2963929/cbc2b81aed85/ijn-5-811f1a.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1286/2963929/c42cf981de2e/ijn-5-811f9.jpg

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