Sonawane Sandeep J, Kalhapure Rahul S, Govender Thirumala
Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa.
Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa..
Eur J Pharm Sci. 2017 Mar 1;99:45-65. doi: 10.1016/j.ejps.2016.12.011. Epub 2016 Dec 12.
Stimuli-responsive polymeric drug delivery systems using various triggers to release the drug at the sites have become a major focus area. Among various stimuli-responsive materials, pH-responsiveness has been studied extensively. The materials used for fabricating pH-responsive drug delivery systems include a specific chemical functionality in their structure that can respond to changes in the pH of the surrounding environment. Various chemical functionalities, for example, acetal, amine, ortho ester, amine and hydrazone, have been used to design materials that are capable of releasing their payload at the acidic pH conditions of the tumor or infection sites. Hydrazone linkages are significant synthons for numerous transformations and have gained importance in pharmaceutical sciences due to their various biological and clinical applications. These linkages have been employed in various drug delivery vehicles, such as linear polymers, star shaped polymers, dendrimers, micelles, liposomes and inorganic nanoparticles, for pH-responsive drug delivery. This review paper focuses on the synthesis and characterization methods of hydrazone bond containing materials and their applications in pH-responsive drug delivery systems. It provides detailed suggestions as guidelines to materials and formulation scientists for designing biocompatible pH-responsive materials with hydrazone linkages and identifying future studies.
利用各种触发因素在特定部位释放药物的刺激响应性聚合物药物递送系统已成为一个主要的研究重点领域。在各种刺激响应性材料中，pH响应性已得到广泛研究。用于制造pH响应性药物递送系统的材料在其结构中具有特定的化学官能团，能够对周围环境pH值的变化做出响应。例如，缩醛、胺、原酸酯、胺和腙等各种化学官能团已被用于设计能够在肿瘤或感染部位的酸性pH条件下释放其负载物的材料。腙键是许多转化反应的重要合成子，由于其各种生物学和临床应用，在药物科学中变得越来越重要。这些键已被应用于各种药物递送载体，如线性聚合物、星形聚合物、树枝状聚合物、胶束、脂质体和无机纳米颗粒，用于pH响应性药物递送。这篇综述文章重点关注含腙键材料的合成和表征方法及其在pH响应性药物递送系统中的应用。它为材料和制剂科学家提供了详细的建议，作为设计具有腙键的生物相容性pH响应性材料和确定未来研究方向的指导方针。
