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活性炭作为无定形药物递送的载体:药物特性和载体润湿性的影响。

Activated carbon as a carrier for amorphous drug delivery: Effect of drug characteristics and carrier wettability.

作者信息

Miriyala Nikhila, Ouyang Defang, Perrie Yvonne, Lowry Deborah, Kirby Daniel J

机构信息

Aston Pharmacy School, School of Life and Health Sciences, Aston University, Birmingham B4 7ET, United Kingdom.

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences (ICMS), University of Macau, Macau, China.

出版信息

Eur J Pharm Biopharm. 2017 Jun;115:197-205. doi: 10.1016/j.ejpb.2017.03.002. Epub 2017 Mar 8.

Abstract

Recent research on porous silica materials as drug carriers for amorphous and controlled drug delivery has shown promising results. However, due to contradictory literature reports on toxicity and high costs of production, it is important to explore alternative safe and inexpensive porous carriers. In this study, the potential of activated carbon (AC) as an amorphous drug carrier was investigated using paracetamol (PA) and ibuprofen (IBU) as model drugs. The solution impregnation method was used for drug loading, with loading efficiency determined by UV spectroscopy and drug release kinetics studied using USP II dissolution apparatus. The physical state of the drug in the complex was characterised using differential scanning calorimetry and X-ray diffractions techniques, whilst sites of drug adsorption were studied using Fourier transform infrared spectroscopy and N adsorption techniques. In addition, the cytotoxicity of AC on human colon carcinoma (Caco-2) cells was assessed using the MTT assay. Results presented here reveal that, for PA/AC and IBU/AC complexes, the saturation solubility of the drug in the loading solvent appears to have an effect on the drug loading efficiency and the physical state of the drug loaded, whilst drug release kinetics were affected by the wettability of the activated carbon particles. Furthermore, activated carbon microparticles exhibited very low cytotoxicity on Caco-2 cells at the concentrations tested (10-800μg/mL). This study, therefore, supports the potential of activated carbon as a carrier for amorphous drug delivery.

摘要

最近关于多孔二氧化硅材料作为无定形药物载体用于药物控释的研究已显示出有前景的结果。然而,由于关于毒性和高生产成本的文献报道相互矛盾,探索替代的安全且廉价的多孔载体很重要。在本研究中,以对乙酰氨基酚(PA)和布洛芬(IBU)作为模型药物,研究了活性炭(AC)作为无定形药物载体的潜力。采用溶液浸渍法进行药物负载,通过紫外光谱法测定负载效率,并使用美国药典II溶出装置研究药物释放动力学。使用差示扫描量热法和X射线衍射技术对复合物中药物的物理状态进行表征,同时使用傅里叶变换红外光谱法和N吸附技术研究药物吸附位点。此外,使用MTT法评估AC对人结肠癌细胞(Caco-2)的细胞毒性。此处给出的结果表明,对于PA/AC和IBU/AC复合物,药物在负载溶剂中的饱和溶解度似乎对药物负载效率和负载药物的物理状态有影响,而药物释放动力学受活性炭颗粒润湿性的影响。此外,在测试浓度(10 - 800μg/mL)下,活性炭微粒对Caco-2细胞表现出非常低的细胞毒性。因此,本研究支持了活性炭作为无定形药物递送载体的潜力。

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