Aderibigbe Blessing Atim
Department of Chemistry, University of Fort Hare, Alice Campus, Eastern Cape 5700, South Africa.
Molecules. 2017 Feb 20;22(2):323. doi: 10.3390/molecules22020323.
Artemisinin and its derivatives have been reported to be experimentally effective for the treatment of highly aggressive cancers without developing drug resistance, they are useful for the treatment of malaria, other protozoal infections and they exhibit antiviral activity. However, they are limited pharmacologically by their poor bioavailability, short half-life in vivo, poor water solubility and long term usage results in toxicity. They are also expensive for the treatment of malaria when compared to other antimalarials. In order to enhance their therapeutic efficacy, they are incorporated onto different drug delivery systems, thus yielding improved biological outcomes. This review article is focused on the currently synthesized derivatives of artemisinin and different delivery systems used for the incorporation of artemisinin and its derivatives.
据报道,青蒿素及其衍生物在实验中对治疗侵袭性很强的癌症有效且不会产生耐药性,它们可用于治疗疟疾、其他原生动物感染,还具有抗病毒活性。然而,它们在药理学上存在局限性,生物利用度差、体内半衰期短、水溶性差,长期使用会产生毒性。与其他抗疟药相比,它们用于治疗疟疾的成本也很高。为了提高其治疗效果,它们被载入不同的药物递送系统,从而产生了更好的生物学效果。这篇综述文章聚焦于目前合成的青蒿素衍生物以及用于载入青蒿素及其衍生物的不同递送系统。