In vivo studies of octreotide-modified N-octyl-O, N-carboxymethyl chitosan micelles loaded with doxorubicin for tumor-targeted delivery.
In vivo studies of octreotide-modified N-octyl-O, N-carboxymethyl chitosan micelles loaded with doxorubicin for tumor-targeted delivery.
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DOI：
10.1002/jps.23341
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发表时间：
2013
影响因子：
3.8
通讯作者：
Aifeng Zou;Yan Chen;Meirong Huo;Jing Wang;Yong Zhang;Jianping Zhou;Qiang Zhang
中科院分区：
文献类型：
--
作者：
Aifeng Zou;Yan Chen;Meirong Huo;Jing Wang;Yong Zhang;Jianping Zhou;Qiang Zhang
奥曲肽（OCT）最近被发现有一个高的结合亲和力的生长抑素受体表达的肿瘤细胞。本研究以OCT-聚乙二醇-硬脂酸（OCT-Phe-PEG-A）为靶向分子，制备了N-辛基-O，N-羧甲基壳聚糖（OCC）胶束。在体内荧光成像方面，将荧光探针Cy 7成功地负载到具有或不具有OCT修饰的OCC胶束（Cy 7-OCC，Cy 7-OCC-OCT）中，并将它们的物理化学性质与DOX负载胶束（DOX-OCC和DOX-OCC-OCT）进行比较。所有胶束均小于120 nm，具有球形形状和约-30 mV的ζ电位。与OCC胶束相比，在荷MCF-7癌异种移植物的BALB/c裸鼠中观察到增强的肿瘤靶向能力。此外，药效学研究表明，与DOX溶液和DOX-OCC胶束相比，DOX-OCC-OCT呈现出最强的肿瘤生长抑制和最低的全身毒性。结果表明，OCC-OCT胶束有望成为肿瘤靶向治疗的有效载体。
Octreotide (OCT) was recently found to have a high binding affinity for the somatostatin receptor expressed on tumor cells. In this study, OCT-polyethylene glycol-stearic acid (OCT-Phe-PEG-A) was used as a targeting molecule for N-octyl-O, N-carboxymethyl chitosan (OCC) micelles loaded with doxorubicin (DOX). For in vivo fluorescence imaging, the fluorescent probe Cyanine 7 (Cy7) was successfully loaded into OCC micelles with or without OCT modification (Cy7-OCC, Cy7-OCC-OCT), and their physicochemical properties were compared with DOX-loaded micelles (DOX-OCC and DOX-OCC-OCT). All micelles were less than 120 nm with spherical shape and zeta potential of around -30 mV. Enhanced tumor-targeting capacity of OCC-OCT micelles was observed in BALB/c nude mice bearing MCF-7 cancer xenografts as compared with the OCC micelles. Moreover, pharmacodynamic studies demonstrated that DOX-OCC-OCT presented a strongest inhibition of tumor growth and lowest systemic toxicity compared with the DOX solution and DOX-OCC micelles. All the results indicated that OCC-OCT micelles might be a promising tumor-targeting carrier for cancer therapy.