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载双氢青蒿素纳米粒的制备及其体内抗弓形虫作用研究。

Comparative studies of salinomycin-loaded nanoparticles prepared by nanoprecipitation and single emulsion method.

机构信息

Nanjing Drum Tower Hospital, Clinical College of Nanjing Medical University, 321 Zhongshan Road, Nanjing 210008, China.

The Comprehensive Cancer Center of Drum Tower Hospital, Medical School of Nanjing University and Clinical Cancer Institute of Nanjing University, Zhongshan Road 321, Nanjing 210008, People's Republic of China.

出版信息

Nanoscale Res Lett. 2014 Jul 15;9(1):351. doi: 10.1186/1556-276X-9-351. eCollection 2014.

DOI:10.1186/1556-276X-9-351
PMID:25147486
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4134115/
Abstract

To establish a satisfactory delivery system for the delivery of salinomycin (Sal), a novel, selective cancer stem cell inhibitor with prominent toxicity, gelatinase-responsive core-shell nanoparticles (NPs), were prepared by nanoprecipitation method (NR-NPs) and single emulsion method (SE-NPs). The gelatinase-responsive copolymer was prepared by carboxylation and double amination method. We studied the stability of NPs prepared by nanoprecipitation method with different proportions of F68 in aqueous phase to determine the best proportion used in our study. Then, the NPs were prepared by nanoprecipitation method with the best proportion of F68 and single emulsion method, and their physiochemical traits including morphology, particle size, zeta potential, drug loading content, stability, and in vitro release profiles were studied. The SE-NPs showed significant differences in particle size, drug loading content, stability, and in vitro release profiles compared to NR-NPs. The SE-NPs presented higher drug entrapment efficiency and superior stability than the NR-NPs. The drug release rate of SE-NPs was more sustainable than that of the NR-NPs, and in vivo experiment indicated that NPs could prominently reduce the toxicity of Sal. Our study demonstrates that the SE-NPs could be a satisfactory method for the preparation of gelatinase-responsive NPs for intelligent delivery of Sal.

摘要

为了建立一个令人满意的 delivery 系统，以输送新型、选择性的癌症干细胞抑制剂——黏菌素（Sal），我们制备了明胶酶响应性核壳纳米粒子（NPs），包括纳米沉淀法（NR-NPs）和单乳液法（SE-NPs）。通过羧基化和双胺化方法制备了明胶酶响应性共聚物。我们研究了不同比例 F68 在水相中的纳米沉淀法制备的 NPs 的稳定性，以确定我们研究中使用的最佳比例。然后，我们使用最佳比例的 F68 通过纳米沉淀法和单乳液法制备了 NPs，并研究了它们的物理化学特性，包括形态、粒径、zeta 电位、载药量、稳定性和体外释放曲线。与 NR-NPs 相比，SE-NPs 在粒径、载药量、稳定性和体外释放曲线方面存在显著差异。SE-NPs 比 NR-NPs 具有更高的药物包封效率和更好的稳定性。SE-NPs 的药物释放速率比 NR-NPs 更可持续，体内实验表明 NPs 可以显著降低 Sal 的毒性。我们的研究表明，SE-NPs 可以成为制备明胶酶响应性 NPs 的一种令人满意的方法，用于 Sal 的智能输送。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/6b1288a6e60e/1556-276X-9-351-5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/706c74c28df8/1556-276X-9-351-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/8e92db679939/1556-276X-9-351-2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/16192f8c4467/1556-276X-9-351-3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/7b6c0150bb12/1556-276X-9-351-4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/6b1288a6e60e/1556-276X-9-351-5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/706c74c28df8/1556-276X-9-351-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/8e92db679939/1556-276X-9-351-2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/16192f8c4467/1556-276X-9-351-3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/7b6c0150bb12/1556-276X-9-351-4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16bb/4134115/6b1288a6e60e/1556-276X-9-351-5.jpg

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