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nanocarriers to Enhance Solubility, Bioavailability, and Efficacy of Artemisinins

World Journal of Traditional Chinese Medicine 2020年第1期6卷 26-38页

作者： Anna Rita Bilia Maria Camilla Bergonzi Joelle CBoulos Thomas Efferth Department of Chemistry University of FlorenceFlorenceItaly Department of Pharmaceutical Biology Institute of Pharmacy and BiochemistryJohannes Gutenberg UniversityMainzGermany

The therapeutic potential of artemisinin (ART) and its derivatives (ARTs) is not limited to malaria but has been recently expanded to other infections with protozoans, trematodes, or viruses as well as to cancer. Due to their limited poor water and oil solubility, rapid degradation by the liver, and short half-life, they have a low bioavailability after oral administration. Consequently, there is a pressing necessity to formulate new ART preparations to raise its bioavailability and efficacy. Nanosized drug delivery systems represent important tools in modern medicine with wide clinical applications, because of their potential modulation of pharmacokinetic and biodistribution. This review focuses on polymer-based systems, lipid-based systems, and inorganic nanoparticles loaded with ARTs. The overall goal of this field of research is to enhance their solubility and stability to improve bioavailability at much lower doses and to increase long-term safety. In addition, the opportunity to reach highly specific site-targeted delivery by these nanocarriers confers a high medicinal value. Remarkably, most of the reported nanoparticulate drug delivery systems are biologically inactive or marginally immunogenic, generating no antigenic or pyrogenic reactions but only partial intrinsic toxicity. As clinical studies in human patients are available so far, there is a pressing need to translate preclinical results on ART-based nanosystems into clinical settings.

关键词： Artemisinin Asteraceae derivatives inorganic nanocarriers lipid nanocarriers nanotechnology polymeric nanocarriers sesquiterpene lactones

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