Artemisinin is highly soluble in polyethylene Glycol 4000 and such solution has multiple biological effects.

Artemisinin has a significant role in treatment of malaria, as well as effective anti-inflammatory and anti-cancer activities. However, such problems as poor water solubility and easy recrystallization limit its application. In this study, polyethylene glycol, a solvent which is widely used in pharmaceutics, was introduced to prepare an artemisinin dissolution. Under the action of hydrogen bonding in 12% polyethylene glycol 4000 solvent, the maximum solubility of artemisinin could reach up to 1 mg/mL. Meanwhile, biological functions of such artemisinin solution were evaluated. The obtained artemisinin solution had a significant inhibitory effect on Gram-positive bacteria, Gram-negative bacteria and fungi. As for the anti-inflammatory property, 0.031 mg/mL artemisinin solution had an obvious inhibitory effect on nitric oxide release in inflammatory cells, and the survival rate of cells was greater than 50%. Low concentration of the obtained artemisinin solution (0.031 mg/mL) had no significant cytotoxicity, while it displayed selective inhibition in cancer cells. IC50 for human hepatoma cells BEL-7404, SMMC7721 and Hep G2 is 0.0016 mg/mL, 0.0084 mg/mL and 0.0541 mg/mL, respectively. In conclusion, the 12% PEG4000-assisted artemisinin solution has a good biological effect and it can be further applied in pharmaceutics, biomaterials and medicine.

[1]  H. Danafar,et al.  Preparation and in vivo evaluation of anti-plasmodial properties of artemisinin-loaded PCL–PEG–PCL nanoparticles , 2018, Pharmaceutical development and technology.

[2]  H. Allgayer,et al.  Prevention of carcinogenesis and metastasis by Artemisinin-type drugs. , 2018, Cancer letters.

[3]  Haiying Cui,et al.  Antibacterial mechanism of artemisinin / beta-cyclodextrins against methicillin-resistant Staphylococcus aureus (MRSA). , 2018, Microbial pathogenesis.

[4]  Yuxin Liu,et al.  Artemisinin-Loaded Mesoporous Nanoplatform for pH-Responsive Radical Generation Synergistic Tumor Theranostics. , 2018, ACS applied materials & interfaces.

[5]  Hongyu Chen,et al.  The selectivity of artemisinin-based drugs on human lung normal and cancer cells. , 2018, Environmental toxicology and pharmacology.

[6]  I. Noda,et al.  Investigation on the relationship between solubility of artemisinin and polyvinylpyrroli done addition by using DAOSD approach. , 2017, Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy.

[7]  D. Hur,et al.  The Effects of Artemisinin on the Cytolytic Activity of Natural Killer (NK) Cells , 2017, International journal of molecular sciences.

[8]  D. Ashour,et al.  Implication of artemisinin nematocidal activity on experimental trichinellosis: In vitro and in vivo studies. , 2017, Parasitology international.

[9]  Xu Zhang,et al.  Preclinical Efficacy and Safety Assessment of Artemisinin-Chemotherapeutic Agent Conjugates for Ovarian Cancer , 2016, EBioMedicine.

[10]  Feng Wang,et al.  Immunomodulation of artemisinin and its derivatives , 2016 .

[11]  J. Qian,et al.  Artemisinin inhibits gallbladder cancer cell lines through triggering cell cycle arrest and apoptosis. , 2016, Molecular medicine reports.

[12]  A. Shelat,et al.  Evaluation of artemisinins for the treatment of acute myeloid leukemia , 2016, Cancer Chemotherapy and Pharmacology.

[13]  Wang Xiuzhen,et al.  [STUDIES ON THE CONSTITUENTS OF ARTEMISIA ANNUA L]. , 2015, Yao xue xue bao = Acta pharmaceutica Sinica.

[14]  Gopal Chakrabarti,et al.  Inhibition of autophagy by chloroquine potentiates synergistically anti-cancer property of artemisinin by promoting ROS dependent apoptosis. , 2014, Biochimie.

[15]  M. Ansari,et al.  Water soluble binary and ternary complexes of diosmin with β-cyclodextrin: Spectroscopic characterization, release studies and anti-oxidant activity , 2014 .

[16]  A. Yan,et al.  Bacterial multidrug efflux pumps: mechanisms, physiology and pharmacological exploitations. , 2014, Biochemical and biophysical research communications.

[17]  A. S. Othman,et al.  Antimicrobial Activity of Artemisinin and Precursor Derived from In Vitro Plantlets of Artemisia annua L. , 2014, BioMed research international.

[18]  R. Clark,et al.  Dihydroartemisinin (DHA) treatment causes an arrest of cell division and apoptosis in rat embryonic erythroblasts in whole embryo culture. , 2013, Birth defects research. Part B, Developmental and reproductive toxicology.

[19]  Xichun Pan,et al.  Design, Synthesis and Evaluation of the Antibacterial Enhancement Activities of Amino Dihydroartemisinin Derivatives , 2013, Molecules.

[20]  Zhang Shu-qiu.  Determination of equilibrium solubility and apparent octanol/water partition coefficient of artemisinin in different solvents , 2013 .

[21]  A. Sekmen,et al.  Effect of Coronatine on Antioxidant Enzyme Response of Chickpea Roots to Combination of PEG-Induced Osmotic Stress and Heat Stress , 2013, Journal of Plant Growth Regulation.

[22]  S. Oh,et al.  Artemisinin inhibits lipopolysaccharide-induced interferon-β production in RAW 264.7 cells: implications on signal transducer and activator of transcription-1 signaling and nitric oxide production. , 2012, International immunopharmacology.

[23]  S. Nekhai,et al.  Iron Metabolism in Cancer and Infection , 2012 .

[24]  Hong Chen,et al.  Anti-inflammatory and immunomodulatory mechanisms of artemisinin on contact hypersensitivity. , 2012, International immunopharmacology.

[25]  M. Nilsson,et al.  Novel artemisinin and curcumin micellar formulations: drug solubility studies by NMR spectroscopy. , 2009, Journal of pharmaceutical sciences.

[26]  S. Doublier,et al.  Artemisinin induces doxorubicin resistance in human colon cancer cells via calcium‐dependent activation of HIF‐1α and P‐glycoprotein overexpression , 2009, British journal of pharmacology.

[27]  Huisheng Lü,et al.  Solubility of Artemisinin in Seven Different Pure Solvents from (283.15 to 323.15) K , 2009 .

[28]  Jing Yi,et al.  Cancer cell killing via ROS: To increase or decrease, that is the question , 2008, Cancer biology & therapy.

[29]  L. Xiaotian.  Studies on the Constituents of Artemisia annua , 2007 .

[30]  E. De Clercq,et al.  Hemin potentiates the anti-hepatitis C virus activity of the antimalarial drug artemisinin. , 2006, Biochemical and biophysical research communications.

[31]  Leah E. Mechanic,et al.  Nitric Oxide, a Mediator of Inflammation, Suppresses Tumorigenesis , 2004, Cancer Research.

[32]  K. Yuen,et al.  Improved oral bioavailability of artemisinin through inclusion complexation with β- and γ-cyclodextrins , 2001 .

[33]  Y. Tu,et al.  The development of new antimalarial drugs: qinghaosu and dihydro-qinghaosu. , 1999, Chinese medical journal.

[34]  T. Eggelte,et al.  Artemisinin drugs in the treatment of malaria: from medicinal herb to registered medication. , 1999, Trends in pharmacological sciences.

[35]  H. Lennernäs,et al.  High in situ rat intestinal permeability of artemisinin unaffected by multiple dosing and with no evidence of P-glycoprotein involvement. , 1999, Drug metabolism and disposition: the biological fate of chemicals.

[36]  B. Lentz,et al.  Poly(ethylene glycol) (PEG)-mediated fusion between pure lipid bilayers: a mechanism in common with viral fusion and secretory vesicle release? , 1999, Molecular membrane biology.

[37]  A. Fitton,et al.  Artesunate. A review of its pharmacology and therapeutic efficacy in the treatment of malaria. , 1995, Drugs.

[38]  A. Kedar,et al.  Neuroblastomas contain iron‐rich ferritin , 1988, Cancer.