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药用和生物医学中的高岭石。

Kaolinite in pharmaceutics and biomedicine.

机构信息

Department of Geology, Faculty of Science, Al Azhar University in Cairo, Nasr City, 11884, Egypt; Instituto Andaluz de Ciencias de la Tierra, CSIC-UGR. Av. de las Palmeras 4, 18100 Armilla, Granada, Spain; Departmento de Farmacia y Tecnología Farmacéutica, Universidad de Granada, 18071, Spain.

Instituto Andaluz de Ciencias de la Tierra, CSIC-UGR. Av. de las Palmeras 4, 18100 Armilla, Granada, Spain.

出版信息

Int J Pharm. 2017 Nov 25;533(1):34-48. doi: 10.1016/j.ijpharm.2017.09.056. Epub 2017 Sep 22.

Abstract

Kaolinite AlSiO(OH) is an abundant and inexpensive geomaterial regarded as one of the most common clay minerals in the earth's crust and the most widespread phase among the other kaolin polymorphs (halloysite, dickite and nacrite). Structurally, it is a hydrous aluminum phyllosilicate member belonging to the dioctahedral 1:1 kaolin mineral group. The particle size of the pseudohexagonal kaolinite platelets is normally <2μm (if compared to a human red blood cell of a typical diameter 6.2-8.2μm or to a virus particle of about 50nm diameter). The kaolinite platelets, either stacked together with a common booklet-like shape in a highly ordered structure (well crystallized) or disordered structure (poorly crystallized), consist of layers considered as a strong dipole of hydrophobic siloxane surface dominated by negative charges, and the other hydrophilic aluminol surface carries positive charges. Kaolinite has been used in many pharmaceutical applications as excipient or active ingredient, because it exhibits excellent physical, chemical and surface physicochemical properties. In addition to their classical pharmaceutical uses, kaolinite and its derivatives have been recently considered as a promising material in many biomedical innovation areas such as drug, protein and gene delivery based on the high interaction capacities with organic and biochemical molecules, bioadhesion and cellular uptake. Pharmaceutical kaolin grades are considerably demanded for usage as excipient in formulations of solid and semi-solid dosage forms. The most important functionalities of kaolin used as excipient are reported as diluent, binder, disintegrant, pelletizing and granulating, amorphizing, particle film coating, emulsifying and suspending agent. Because of its uninjured bioactivity, kaolinite has been also used as active agent for treatment of some common diseases. It can be topically administered as hemostatic agent, dermatological protector, anti-inflammatory agent and in pelotherapy, or orally as gastrointestinal protector, and antibacterial, antiviral, detoxification or antidiarrheal agent. With these premises, the future of kaolinite in health-care uses is strongly interesting, especially in the development of pharmaceutical and cosmetic industries. In biomedicinal investigations, it can be considered as a promising natural geomaterial for designing new derivatives that can contribute in the trials of discovering new therapeutic systems and treatment pathways of global challenge diseases such as cancer, viruses, antibiotic resistant bacteria, alzheimer, chronic skeletomuscular and geriatric diseases.

摘要

高岭石 AlSiO(OH) 是一种丰富且廉价的地质材料,被认为是地壳中最常见的粘土矿物之一,也是其他高岭石多晶型物(埃洛石、地开石和珍珠陶土)中分布最广的相。在结构上,它是一种含水的铝层状硅酸盐,属于二八面体 1:1 高岭石矿物族。准六边形高岭石薄片的粒径通常小于 2μm(与典型直径为 6.2-8.2μm 的人类红细胞或直径约 50nm 的病毒颗粒相比)。高岭石薄片要么以共同的书本状堆叠在一起,形成高度有序的结构(结晶良好),要么形成无序结构(结晶不良),由被认为是强疏水性硅氧烷表面的层组成,该表面主要带负电荷,而另一个亲水的水铝醇表面带正电荷。高岭石因其具有优异的物理、化学和表面物理化学性能,已被广泛应用于许多药物制剂中,作为赋形剂或活性成分。除了其在药物制剂中的传统用途外,高岭石及其衍生物最近还被认为是许多生物医学创新领域的一种很有前途的材料,例如基于与有机和生化分子的高相互作用能力的药物、蛋白质和基因递送、生物黏附性和细胞摄取。医药级高岭土在固体制剂和半固体制剂的配方中作为赋形剂的需求量很大。作为赋形剂使用的高岭石最重要的功能包括稀释剂、粘合剂、崩解剂、制粒和造粒、无定形化、颗粒薄膜包衣、乳化和悬浮剂。由于其无损的生物活性,高岭石也被用作治疗某些常见疾病的活性成分。它可以局部用作止血剂、皮肤病保护剂、抗炎剂和 Pelotherapy,或口服作为胃肠道保护剂、抗菌、抗病毒、解毒或止泻剂。基于这些前提,高岭石在保健用途方面的未来非常有前景,尤其是在制药和化妆品行业的发展方面。在生物医学研究中,它可以被视为一种很有前途的天然地质材料,用于设计新的衍生物,这些衍生物可以为癌症、病毒、抗生素耐药菌、阿尔茨海默病、慢性骨骼肌肉和老年疾病等全球性挑战疾病的新治疗系统和治疗途径的发现试验做出贡献。

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