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超声处理定制增强柚皮素纳米颗粒对胰腺癌的细胞毒性:设计、优化和研究。

Sonication tailored enhance cytotoxicity of naringenin nanoparticle in pancreatic cancer: design, optimization, and studies.

机构信息

Faculty of Pharmacy, DIT University, Dehradun, India.

Alwar Pharmacy College Rajasthan University of Health Sciences (RUHS), M.I.A. Alwar-Rajasthan, Alwar, India.

出版信息

Drug Dev Ind Pharm. 2020 Apr;46(4):659-672. doi: 10.1080/03639045.2020.1747485. Epub 2020 Apr 8.

DOI:10.1080/03639045.2020.1747485
PMID:32208984
Abstract

, optimization, characterization, and cytotoxic studies of NAR nanoparticles (NPs) to against pancreatic cancer. The sonication tailored Naringenin (NARG)-loaded poly (lactide-co-glycolic acid) (PLGA) NPs was fabricated for potential cytotoxic effect against pancreatic cancer. NARG NPs were prepared by emulsion-diffusion evaporation technique applying BoxBehnken experimental design based on three-level and three-factors. The effect of independent variables surfactant concentration (), polymer concentration (), and sonication time () were studied on responses particle size (), and drug release % (). NPs characterized for particles size and size distribution, polydispersity index (PDI), zeta potential, transmission electron microscope (TEM), scanning electron microscope (SEM), Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimeter (DSC), and X-ray diffraction (XRD) studies. Further, the studies was fitted to various drug release kinetic model and cytotoxicity evaluated . The nanosized particles were spherical, uniform with an average size of 150.45 ± 12.45 nm, PDI value 0.132 ± 0.026, zeta potential -20.5 ± 2.5 mV, and cumulative percentage release 85.67 ± 6.23%. release of NARG from nanoparticle evaluated initially burst followed by sustained release behavior. The Higuchi was best fitted model to drug release from NARG NPs. The cytotoxicity study of NARG NPs apparently showed higher cytotoxic effect over free NARG ( 0.05). The stability study of optimized formulation revealed no significant physico-chemical changes during 3 months. Thus, NARG-loaded NPs gave ameliorated anticancer effect over plain NARG.

摘要

,优化,表征,并研究 NAR 纳米粒子(NPs)对胰腺癌的细胞毒性。通过超声处理定制了具有潜在细胞毒性的柚皮苷(NARG)负载聚(乳酸-共-乙醇酸)(PLGA) NPs。通过基于三水平和三因素的乳化-扩散蒸发技术制备 NARG NPs。研究了独立变量表面活性剂浓度()、聚合物浓度()和超声时间()对响应粒径()和药物释放%()的影响。 NPs 的特征在于粒径和粒径分布、多分散指数(PDI)、Zeta 电位、透射电子显微镜(TEM)、扫描电子显微镜(SEM)、傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)和 X 射线衍射(XRD)研究。此外,研究拟合了各种药物释放动力学模型并评估了细胞毒性。纳米颗粒为球形,均匀,平均粒径为 150.45±12.45nm,PDI 值为 0.132±0.026,Zeta 电位为-20.5±2.5mV,累积释放百分比为 85.67±6.23%。NARG 从纳米颗粒中的释放表现出初始突释随后是持续释放的行为。Higuchi 是最适合 NARG NPs 药物释放的模型。NARG NPs 的细胞毒性研究明显显示出比游离 NARG 更高的细胞毒性( 0.05)。优化配方的稳定性研究表明,在 3 个月内没有发生显著的物理化学变化。因此,负载 NARG 的 NPs 比普通 NARG 具有更好的抗癌效果。

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