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采用高真空法载顺铂微孔磷酸钙的结晶:特性分析与释放研究。

Crystallization of carboplatin-loaded onto microporous calcium phosphate using high-vacuum method: Characterization and release study.

机构信息

Department of Mechanical Engineering, College of Technological Science, Santa Catarina State University, Joinville, Santa Catarina, Brazil.

出版信息

PLoS One. 2020 Dec 8;15(12):e0242565. doi: 10.1371/journal.pone.0242565. eCollection 2020.

Abstract

Drug delivery systems are a new approach to increase therapeutic efficacy and to reduce the side effects of traditional treatments. Calcium phosphates (CaPs) have been studied as drug delivery systems, especially in bone diseases. However, each system has some particularities that depend on the physical and chemical characteristics of the biomaterials and drug interaction. In this work, granulated CaPs were used as a matrix for loading the anticancer drug carboplatin using the high-vacuum method. Five compositions were applied: hydroxyapatite (HA), β-tricalcium phosphate (β-TCP), biphasic HAp 60%/β-TCP 40% (BCP), β-TCP/MgO nanocomposite, and β-TCP/SiO2 nanocomposite. Carboplatin drug in 50, 60, and 70 mg/g was precipitated on the surface of CaPs. Morphological, chemical and surface modifications in the carboplatin-CaPs were investigated by scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS), backscattered electron microscopy (BSE), X-ray diffraction (XRD), X-ray fluorescence spectroscopy (XRF), Fourier transform infrared (FT-IR), and Raman spectroscopy. The characterization of the CaP-carboplatin biomaterials showed heterogeneous crystalline precipitation of the drug, and no morphological modifications of the CaPs biomaterials. The in vitro release profile of carboplatin from CaPs was evaluated by the ultraviolet-visible (UV-Vis) method. The curves showed a burst release of upon 60% of carboplatin loaded followed by a slow-release of the drug for the time of the study. The results were typical of a low-interaction system and physisorption mechanism. The high-vacuum method permitted to load the high amount of carboplatin drug on the surface of the biomaterials despite the low interaction between carboplatin and CaPs.

摘要

药物传递系统是一种提高治疗效果和降低传统治疗副作用的新方法。钙磷酸盐 (CaPs) 已被研究作为药物传递系统,特别是在骨疾病中。然而,每个系统都有一些特殊之处,这取决于生物材料的物理和化学特性以及药物相互作用。在这项工作中,使用粒状 CaPs 作为基质,通过高真空法加载抗癌药物卡铂。应用了五种组合物:羟基磷灰石 (HA)、β-磷酸三钙 (β-TCP)、双相 HAp60%/β-TCP40%(BCP)、β-TCP/MgO 纳米复合材料和β-TCP/SiO2 纳米复合材料。将 50、60 和 70mg/g 的卡铂药物沉淀在 CaPs 的表面上。通过扫描电子显微镜 (SEM)、能量色散光谱 (EDS)、背散射电子显微镜 (BSE)、X 射线衍射 (XRD)、X 射线荧光光谱 (XRF)、傅里叶变换红外 (FT-IR) 和拉曼光谱研究了 CaPs 表面的形态、化学和表面修饰。CaP-卡铂生物材料的特性研究表明,药物呈异质结晶沉淀,而 CaP 生物材料的形态没有变化。通过紫外-可见 (UV-Vis) 法评估了 CaPs 中卡铂的体外释放曲线。结果表明,负载的卡铂中有 60%的药物呈现出突释,随后在研究时间内药物缓慢释放。结果表明,这是一种低相互作用体系和物理吸附机制。尽管卡铂与 CaPs 之间的相互作用较低,但高真空法允许在生物材料表面负载大量的卡铂药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fb4/7723252/875f4907c2ec/pone.0242565.g001.jpg

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