Stebbins Nicholas D, Ouimet Michelle A, Uhrich Kathryn E
Department of Chemistry and Chemical Biology, Rutgers University, 610 Taylor Road Piscataway, NJ 08854, USA.
Department of Chemistry and Chemical Biology, Rutgers University, 610 Taylor Road Piscataway, NJ 08854, USA.
Adv Drug Deliv Rev. 2014 Nov 30;78:77-87. doi: 10.1016/j.addr.2014.04.006. Epub 2014 Apr 18.
Many currently used antibiotics suffer from issues such as systemic toxicity, short half-life, and increased susceptibility to bacterial resistance. Although most antibiotic classes are administered systemically through oral or intravenous routes, a more efficient delivery system is needed. This review discusses the chemical conjugation of antibiotics to polymers, achieved by forming covalent bonds between antibiotics and a pre-existing polymer or by developing novel antibiotic-containing polymers. Through conjugating antibiotics to polymers, unique polymer properties can be taken advantage of. These polymeric antibiotics display controlled, sustained drug release and vary in antibiotic class type, synthetic method, polymer composition, bond lability, and antibacterial activity. The polymer synthesis, characterization, drug release, and antibacterial activities, if applicable, will be presented to offer a detailed overview of each system.
许多目前使用的抗生素存在诸如全身毒性、半衰期短以及细菌耐药性增加等问题。尽管大多数抗生素类别是通过口服或静脉途径进行全身给药,但仍需要一种更有效的给药系统。本综述讨论了抗生素与聚合物的化学偶联,这是通过在抗生素与预先存在的聚合物之间形成共价键或通过开发新型含抗生素聚合物来实现的。通过将抗生素与聚合物偶联,可以利用聚合物的独特性质。这些聚合物抗生素表现出可控的、持续的药物释放,并且在抗生素类别类型、合成方法、聚合物组成、键的稳定性和抗菌活性方面各不相同。将介绍聚合物的合成、表征、药物释放以及抗菌活性(如适用),以详细概述每个系统。