用于乳腺癌治疗的卡培他滨负载 NLC:制备、表征和体外评估。

Muhammad Hadi Sultan, Yosif Almoshari, Syam Mohan, Mohamed Ahmed Al-Kasim, Hamad S Alyami, Mohammad Azam Ansari, Mohammad Intakhab Alam
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引用次数: 0

摘要

背景:癌症治疗通常需要使用卡培他滨[CAP]等强效抗肿瘤药物,这可能会导致严重的毒性反应。因此需要一种剂型来控制这些毒性,既能有效地将药物输送到靶点,又能在较低剂量下保持疗效。为了实现上述目标,我们制备并评估了含有卡培他滨的 NLC [NANOBIN]。设计并评估了 NANOBIN 的不同配方,分别称为 CaTS、CaT1S、CaT2S、CaTS1 和 CaTS2,以改善药物输送和治疗效果:方法:采用热均质法制备 NANOBIN 制剂。这些制剂的表征基于各种参数,如粒度、多分散指数(PDI)、Zeta 电位(ZP)、透射电子显微镜(TEM)成像和包封效率(EE)。体外评估包括稳定性测试、评估药物释放动力学的释放研究,以及评估这些制剂对人类乳腺癌细胞 MCF-7 的疗效的细胞毒性试验[MTT 试验]:表征结果显示,所有 NANOBIN 制剂的粒径范围为 65 至 193 nm,PDI 值在 0.26 至 0.37 之间,ZP 值在 46.47 至 61.87 mV [-ve] 之间,EE 百分比在 94.121% 至 96.64% 之间。此外,所有 NANOBIN 制剂都显示出 CAP 的持续缓释特性。MTT 试验表明,NANOBINs 的细胞毒性功效明显增强,在 MCF-7 细胞上测试时,其细胞毒性大约是游离 CAP 的 10 倍。这些研究结果表明,NANOBINs 有潜力将 CAP 有效递送至靶点,从而延长药物的可用性,并以较低的剂量提高治疗效果:该研究表明,NANOBINs 能有效地将 CAP 送达靶点,延长药物暴露时间,提高疗效,同时降低所需剂量。有必要开展进一步的研究来验证这些发现,并将 NANOBINs 确立为癌症治疗的首选治疗方案。
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Capecitabine-loaded NLC for Breast Cancer Treatment: Preparation, Characterization, and In vitro Evaluation.

Background: Cancer treatment often involves the use of potent antineoplastic drugs like Capecitabine [CAP], which can lead to serious toxicities. There is a need for dosage forms to manage these toxicities that can deliver the medication effectively to the target site while maintaining therapeutic efficacy at lower doses. To achieve the aforesaid objective, NLC containing capecitabine [NANOBIN] was prepared and evaluated. Different formulations of NANOBIN, denoted as CaTS, CaT1S, CaT2S, CaTS1, and CaTS2, were designed and evaluated to improve drug delivery and therapeutic outcomes.

Methods: The NANOBIN formulations were prepared using the hot homogenization method. The characterization of these formulations was conducted based on various parameters such as particle size, Polydispersity Index [PDI], Zeta Potential [ZP], Transmission Electron Microscopy [TEM] imaging, and Encapsulation Efficiency [EE]. In vitro evaluations included stability testing, release studies to assess drug release kinetics, and a cytotoxicity assay [MTT assay] to evaluate the efficacy of these formulations against human breast cancer cells [MCF-7].

Results: The characterization results revealed that all NANOBIN formulations exhibited particle sizes ranging from 65 to 193 nm, PDI values within the range of 0.26-0.37, ZP values between 46.47 to 61.87 mV [-ve], and high EE percentages ranging from 94.121% to 96.64%. Furthermore, all NANOBIN formulations demonstrated sustained and slow-release profiles of CAP. The MTT assay showed that the NANOBINs exhibited significantly enhanced cytotoxic efficacy, approximately 10 times greater than free CAP when tested on MCF-7 cells. These findings indicate the potential of NANOBINs to deliver CAP effectively to the target site, enabling prolonged drug availability and enhanced therapeutic effects at lower doses.

Conclusion: The study demonstrates that NANOBINs can effectively deliver CAP to target sites, prolonging drug exposure and enhancing therapeutic efficacy while reducing the required dose. Further studies are necessary to validate these findings and establish NANOBINs as a preferred treatment option for cancer therapy.

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