Varan Gamze, Varan Cem, Erdoğar Nazlı, Hıncal A Atilla, Bilensoy Erem
Department of Nanotechnology and Nanomedicine, Instıtute of Graduate Studies in Science, Hacettepe University, 06800 Beytepe-Ankara, Turkey.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, 06100 Sıhhiye-Ankara, Turkey.
Int J Pharm. 2017 Oct 15;531(2):457-469. doi: 10.1016/j.ijpharm.2017.06.010. Epub 2017 Jun 6.
Cyclodextrins are cyclic oligosaccharides obtained by enzymatic digestion of starch. The α-, β- and γ- cyclodextrins contain respectively 6, 7 and 8 glucopyranose units, with primary and secondary hydroxyl groups located on the narrow and wider rims of a truncated cone shape structure. Such structure is that of a hydrophobic inner cavity with a hydrophilic outer surface allowing to interact with a wide range of molecules like ions, protein and oligonucleotides to form inclusion complexes. Many cyclodextrin applications in the pharmaceutical area have been widely described in the literature due to their low toxicity and low immunogenicity. The most important is to increase the solubility of hydrophobic drugs in water. Chemically modified cyclodextrin derivatives have been synthesized to enhance their properties and more specifically their pharmacological activity. Among these, amphiphilic derivatives were designed to build organized molecular structures, through selfassembling systems or by incorporation in lipid membranes, expected to improve the vectorization in the organism of the drug-containing cyclodextrin cavities. These derivatives can form a variety of supramolecular structures such as micelles, vesicles and nanoparticles. The purpose of this review is to summarize applications of amphiphilic cyclodextrins in different areas of drug delivery, particularly in protein and peptide drug delivery and gene delivery. The article highlights important amphiphilic cyclodextrin applications in the design of novel delivery systems like nanoparticles.
环糊精是通过淀粉的酶促消化获得的环状寡糖。α-、β-和γ-环糊精分别含有6、7和8个吡喃葡萄糖单元，其一级和二级羟基位于截顶圆锥形状结构的窄边和宽边。这种结构是一个疏水内腔和亲水外表面，允许与离子、蛋白质和寡核苷酸等多种分子相互作用形成包合物。由于环糊精的低毒性和低免疫原性，其在制药领域的许多应用已在文献中得到广泛描述。最重要的是提高疏水药物在水中的溶解度。已经合成了化学修饰的环糊精衍生物以增强其性质，更具体地说是增强其药理活性。其中，两亲性衍生物被设计用于通过自组装系统或通过掺入脂质膜来构建有组织的分子结构，预期可改善含药物环糊精腔在生物体内的载体化。这些衍生物可以形成多种超分子结构，如胶束、囊泡和纳米颗粒。本综述的目的是总结两亲性环糊精在药物递送的不同领域中的应用，特别是在蛋白质和肽药物递送以及基因递送方面。本文重点介绍了两亲性环糊精在纳米颗粒等新型递送系统设计中的重要应用。
