Dehydrocurvularin-loaded mPEG-PLGA nanoparticles for targeted breast cancer drug delivery: preparation, characterization, in vitro, and in vivo evaluation.

IF 4.3 4区 医学 Q1 PHARMACOLOGY & PHARMACY
Journal of Drug Targeting Pub Date : 2024-12-01 Epub Date: 2024-02-01 DOI:10.1080/1061186X.2024.2309566
Xuewei Cui, Zhong He, Jianjia Liang, Mulan Wei, Zhiyong Guo, Yiqing Zhou, Ye Qin, Zhangshuang Deng
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引用次数: 0

Abstract

Dehydrocurvularin (DCV) is a promising lead compound for anti-cancer therapy. Unfortunately, the development of DCV-based drugs has been hampered by its poor solubility and bioavailability. Herein, we prepared a DCV-loaded mPEG-PLGA nanoparticles (DCV-NPs) with improved drug properties and therapeutic efficacy. The spherical and discrete particles of DCV-NPs had a uniform diameter of 101.8 ± 0.45 nm and negative zeta potential of -22.5 ± 1.12 mV (pH = 7.4), and its entrapment efficiency (EE) and drug loading (DL) were ∼53.28 ± 1.12 and 10.23 ± 0.30%, respectively. In vitro the release of DCV-NPs lasted for more than 120 h in a sustained-release pattern, its antiproliferation efficacy towards breast cancer cell lines (MCF-7, MDA-MB-231, and 4T1) was better than that of starting drug DCV, and it could be efficiently and rapidly internalised by breast cancer cells. In vivo DCV-NPs were gradually accumulated in tumour areas of mice and significantly suppressed tumour growth. In summary, loading water-insoluble DCV onto nanoparticles has the potential to be an effective agent for breast cancer therapy with injectable property and tumour targeting capacity.

用于乳腺癌靶向给药的去氢卷曲霉素负载 mPEG-PLGA 纳米粒子:制备、表征、体外和体内评估。
脱氢苦参碱(DCV)是一种很有希望用于抗癌治疗的先导化合物。遗憾的是,由于其溶解性和生物利用度较差,DCV 类药物的开发一直受到阻碍。在此,我们制备了一种负载 DCV 的 mPEG-PLGA 纳米颗粒(DCV-NPs),其药物性质和疗效均有所改善。DCV-NPs为球形离散颗粒,直径为101.8 ± 0.45 nm,负ZETA电位为-22.5 ± 1.12 mV(pH =7.4),其包载效率(EE)和载药量(DL)分别约为53.28 ± 1.12%和10.23 ± 0.30%。体外实验中,DCV-NPs的持续释放时间超过120小时,对乳腺癌细胞株(MCF-7、MDA-MB-231和4T1)的抗增殖效果优于起始药物DCV,并能被乳腺癌细胞高效、快速地内化。在体内,DCV-NPs 在小鼠肿瘤区域逐渐积累,并显著抑制肿瘤生长。总之,将不溶于水的 DCV 添加到纳米颗粒中,具有可注射性和肿瘤靶向能力,有望成为乳腺癌治疗的有效药物。
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来源期刊
CiteScore
9.10
自引率
0.00%
发文量
165
审稿时长
2 months
期刊介绍: Journal of Drug Targeting publishes papers and reviews on all aspects of drug delivery and targeting for molecular and macromolecular drugs including the design and characterization of carrier systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo applications of these drugs. Papers are not restricted to drugs delivered by way of a carrier, but also include studies on molecular and macromolecular drugs that are designed to target specific cellular or extra-cellular molecules. As such the journal publishes results on the activity, delivery and targeting of therapeutic peptides/proteins and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids (e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes), as well as aptamers, mononucleotides and monoclonal antibodies and their conjugates. The diagnostic application of targeting technologies as well as targeted delivery of diagnostic and imaging agents also fall within the scope of the journal. In addition, papers are sought on self-regulating systems, systems responsive to their environment and to external stimuli and those that can produce programmed, pulsed and otherwise complex delivery patterns.
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