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从海枣属植物种子中提取的大孔天然胶囊及其在口服药物递送中的应用。

Macroporous natural capsules extracted from Phoenix dactylifera L. spore and their application in oral drugs delivery.

作者信息

Alshehri Saad M, Al-Lohedan Hamad A, Al-Farraj Eida, Alhokbany Norah, Chaudhary Anis Ahmad, Ahamad Tansir

机构信息

Department of Chemistry, College of Science, King Saud University, Riyadh 11451, Saudi Arabia.

Department of Chemistry, College of Science, King Saud University, Riyadh 11451, Saudi Arabia; Surfactant Research Chair, Department of Chemistry, King Saud University, P.O. Box-2455, Riyadh 11451, Saudi Arabia.

出版信息

Int J Pharm. 2016 May 17;504(1-2):39-47. doi: 10.1016/j.ijpharm.2016.02.049. Epub 2016 Mar 2.

Abstract

Macroporous natural sporopollenin exine capsules (SEC) were extracted from date palm (Phoenix dactylifera L.) and coated by natural polymer composite (carboxymethyl cellulose with epichlorohydrin). The polymer coated exine capsules (PCEC) were used in in-vitro investigations for controlled delivery of paracetamol. SEC, PCEC, and drugs loaded capsules (PCEC-PAR) were characterized by scanning electron microscope (SEM), surface area (BET), Fourier-transform infrared (FT-IR), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA). The length of SEC was found to be 20-20.5 μm, and the pore sized was 50-135 nm, as measured using SEM. The studies revealed that maximum loading of the drug was at pH 6.0 (97.2%, with 50 mg mL(-1)). The results indicate that by increasing the pH from 1.4 to 7.4, the cumulative release rates of paracetamol in physiological buffer solution (PBS) is more than two times as in simulated gastric fluid (SGF). In addition, the in-vitro toxicity of PCEC against Caco-2 cells was tested by the 3-[4,5-dimethylthiazole-2-yl]-2,5 diphenyltetrazolium bromide (MTT) assay, and the results revealed that PCEC are biocompatible materials. The overall results encourage further studies on the clinical use of PCEC as drug carriers.

摘要

从椰枣(Phoenix dactylifera L.)中提取了大孔天然孢粉素外壁胶囊(SEC),并用天然聚合物复合材料(羧甲基纤维素与环氧氯丙烷)进行包衣。聚合物包衣的外壁胶囊(PCEC)用于对乙酰氨基酚的体外控释研究。通过扫描电子显微镜(SEM)、比表面积(BET)、傅里叶变换红外光谱(FT-IR)、X射线衍射(XRD)、差示扫描量热法(DSC)和热重分析(TGA)对SEC、PCEC和载药胶囊(PCEC-PAR)进行了表征。使用SEM测量发现SEC的长度为20 - 20.5μm,孔径为50 - 135nm。研究表明,药物的最大载量是在pH 6.0时(97.2%,50mg mL(-1))。结果表明,将pH从1.4提高到7.4时,对乙酰氨基酚在生理缓冲溶液(PBS)中的累积释放率是在模拟胃液(SGF)中的两倍多。此外,通过3-[4,5-二甲基噻唑-2-基]-2,5-二苯基四氮唑溴盐(MTT)法测试了PCEC对Caco-2细胞的体外毒性,结果表明PCEC是生物相容性材料。总体结果鼓励进一步研究PCEC作为药物载体的临床应用。

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