Islam Mohammad Ariful, Park Tae-Eun, Reesor Emma, Cherukula Kondareddy, Hasan Anwarul, Firdous Jannatul, Singh Bijay, Kang Sang-Kee, Choi Yun-Jaie, Park In-Kyu, Cho Chong-Su
Department of Agricultural Biotechnology and Research Institute for Agriculture and Life Sciences, Seoul National University, Seoul 151-921, Korea.
Curr Pharm Des. 2015;21(29):4285-309. doi: 10.2174/1381612821666150901103819.
Chitosan on its own is a well-established natural polymer and is widely regarded as a biodegradable, biocompatible and nontoxic material for drug delivery applications. Although unmodified chitosan has some mucoadhesive properties on its own, its bioavailability is limited due to its short retention time in the body. Moreover, the high solubility of chitosan at acidic pH levels limits its use for mucosal drug delivery (especially through the oral route). Chemically-modified mucoadhesive chitosan, especially thiolated chitosan, has arisen as an alternative to create novel mucosal drug delivery systems. The mucoadhesive properties that are conferred to the thiolated chitosan certainly set this novel class of second or third-generation thiomers apart. To understand the significance of mucoadhesive chitosan, we first present the mechanism of mucoadhesion and provide comprehensive coverage of description of a variety of chemical modifications to prepare mucoadhesive thiolated chitosan derivatives. We then present the plethora of applications of these modified chitosan variants in a wide range of drug delivery fields, including the delivery of antigens, proteins and genes through a variety of routes, including oral, nasal, pulmonary, vaginal and others. By presenting the range of applications for mucoadhesive chitosan drug carriers we herein demonstrate that chemically-modified thiolated chitosan is a versatile and effective material for a new class of drug delivery vehicles.
壳聚糖本身是一种成熟的天然聚合物，被广泛认为是一种可生物降解、生物相容且无毒的药物递送材料。尽管未改性的壳聚糖本身具有一定的粘膜粘附特性，但其在体内的滞留时间较短，导致其生物利用度有限。此外，壳聚糖在酸性pH值下的高溶解性限制了其在粘膜药物递送中的应用（尤其是通过口服途径）。化学改性的粘膜粘附性壳聚糖，特别是硫醇化壳聚糖，已成为创建新型粘膜药物递送系统的替代方案。赋予硫醇化壳聚糖的粘膜粘附特性无疑使这类新型的第二代或第三代硫醇聚合物与众不同。为了理解粘膜粘附性壳聚糖的重要性，我们首先介绍粘膜粘附的机制，并全面描述制备粘膜粘附性硫醇化壳聚糖衍生物的各种化学修饰。然后，我们展示这些改性壳聚糖变体在广泛的药物递送领域中的大量应用，包括通过口服、鼻腔、肺部、阴道等多种途径递送抗原、蛋白质和基因。通过展示粘膜粘附性壳聚糖药物载体的应用范围，我们在此证明化学改性的硫醇化壳聚糖是一类新型药物递送载体的通用且有效的材料。
