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酸响应性核交联纳米胶束用于肝癌细胞的靶向药物递送和磁共振成像。

Acid-triggered core cross-linked nanomicelles for targeted drug delivery and magnetic resonance imaging in liver cancer cells.

机构信息

Radiology Department, The Sun Yat-Sen Memorial Hospital, Sun Yat-Sen University, Guangzhou, People's Republic of China.

出版信息

Int J Nanomedicine. 2013;8:3019-31. doi: 10.2147/IJN.S45767. Epub 2013 Aug 12.

DOI:10.2147/IJN.S45767
PMID:23976852
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3746790/
Abstract

PURPOSE

To research the acid-triggered core cross-linked folate-poly(ethylene glycol)-b-poly[N-(N',N'-diisopropylaminoethyl) glutamine] (folated-PEG-P[GA-DIP]) amphiphilic block copolymer for targeted drug delivery and magnetic resonance imaging (MRI) in liver cancer cells.

METHODS

As an appropriate receptor of protons, the N,N-diisopropyl tertiary amine group (DIP) was chosen to conjugate with the side carboxyl groups of poly(ethylene glycol)-b-poly (L-glutamic acid) to obtain PEG-P(GA-DIP) amphiphilic block copolymers. By ultrasonic emulsification, PEG-P(GA-DIP) could be self-assembled to form nanosized micelles loading doxorubicin (DOX) and superparamagnetic iron oxide nanoparticles (SPIONs) in aqueous solution. When PEG-P(GA-DIP) nanomicelles were combined with folic acid, the targeted effect of folated-PEG-P(GA-DIP) nanomicelles was evident in the fluorescence and MRI results.

RESULTS

To further increase the loading efficiency and the cell-uptake of encapsulated drugs (DOX and SPIONs), DIP (pKa≈6.3) groups were linked with ~50% of the side carboxyl groups of poly(L-glutamic acid) (PGA), to generate the core cross-linking under neutral or weakly acidic conditions. Under the acidic condition (eg, endosome/lysosome), the carboxyl groups were neutralized to facilitate disassembly of the P(GA-DIP) blocks' cross-linking, for duly accelerating the encapsulated drug release. Combined with the tumor-targeting effect of folic acid, specific drug delivery to the liver cancer cells and MRI diagnosis of these cells were greatly enhanced.

CONCLUSION

Acid-triggered and folate-decorated nanomicelles encapsulating SPIONs and DOX, facilitate the targeted MRI diagnosis and therapeutic effects in tumors.

摘要

目的

研究酸触发的核心交联叶酸-聚乙二醇-b-聚[N-(N'，N'-二异丙基氨基乙基)谷氨酸]（叶酸-PEG-P[GA-DIP]）两亲嵌段共聚物在肝癌细胞中的靶向药物递送和磁共振成像（MRI）中的应用。

方法

选择 N，N-二异丙基叔胺基（DIP）作为适当的质子受体，与聚乙二醇-b-聚（L-谷氨酸）的侧羧基缀合，得到 PEG-P（GA-DIP）两亲嵌段共聚物。通过超声乳化，PEG-P（GA-DIP）可以自组装形成纳米尺寸的胶束，在水溶液中装载阿霉素（DOX）和超顺磁性氧化铁纳米颗粒（SPIONs）。当 PEG-P（GA-DIP）纳米胶束与叶酸结合时，叶酸-PEG-P（GA-DIP）纳米胶束的靶向效果在荧光和 MRI 结果中表现明显。

结果

为了进一步提高包封药物（DOX 和 SPIONs）的载药效率和细胞摄取，将 DIP（pKa≈6.3）基团与聚 L-谷氨酸（PGA）的约 50%侧羧基连接，在中性或弱酸性条件下生成核心交联。在酸性条件下（例如内体/溶酶体），羧基被中和，有利于 P（GA-DIP）嵌段的交联解组装，从而适当加速包封药物的释放。结合叶酸的肿瘤靶向作用，极大地增强了对肝癌细胞的特异性药物递送和这些细胞的 MRI 诊断。

结论

酸触发和叶酸修饰的纳米胶束包封 SPIONs 和 DOX，有利于肿瘤的靶向 MRI 诊断和治疗效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/bfeef6386d44/ijn-8-3019Fig13.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/8cbac3ae2531/ijn-8-3019Fig1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/342831a7e63c/ijn-8-3019Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/848c0c78bc25/ijn-8-3019Fig8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/09e824fd22d2/ijn-8-3019Fig9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/219c9302af48/ijn-8-3019Fig10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/5fec9a83d3c4/ijn-8-3019Fig11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/bb975a237072/ijn-8-3019Fig12.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/bfeef6386d44/ijn-8-3019Fig13.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/8cbac3ae2531/ijn-8-3019Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/fec08d7659fe/ijn-8-3019Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/203078a64ff8/ijn-8-3019Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/d0022bb1a7aa/ijn-8-3019Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/efa8b6183307/ijn-8-3019Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/d8eb19c1d3f1/ijn-8-3019Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/342831a7e63c/ijn-8-3019Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/848c0c78bc25/ijn-8-3019Fig8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/09e824fd22d2/ijn-8-3019Fig9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/219c9302af48/ijn-8-3019Fig10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/5fec9a83d3c4/ijn-8-3019Fig11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/bb975a237072/ijn-8-3019Fig12.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d9b/3746790/bfeef6386d44/ijn-8-3019Fig13.jpg

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