Improved anticancer efficacy of artemisinin and its derivatives through nanodelivery

Aim and Background: Cancer is a life-challenging disease across the world which its mortality rate is still increasing. Beside surgery, current approaches that have been employed for cancer treatment include chemotherapy, hormonal therapy, immunotherapy and radiotherapy. Nevertheless, clinical outcome of chemotherapy is unsatisfactory, due to high side effects and drug resistance. Artemisinin (C15H22O5) is a sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, with a unique peroxide bridge which plays an important role in its active biological mode of action. Methods: A systematic search was performed in databases Science Direct, PubMed and Google Scholar, using keywords, natural sesquiterpene, artemisinin, nanodelivery and anticancer effects. Results and discussion: Derivatives of artemisinin include artesunate, artemether and dihydroartemisinin that are recommended for cancer studies. These agents act through induction of apoptosis, suppression of cell proliferation, inhibition of cell invasion and metastasis, disruption of cancer signaling pathway, hindering angiogenesis and regulating the tumor microenvironment. Pharmacological properties of artemisinin and its derivatives could be improved by incorporating them into nanocarriers such as nanoparticles, nanocapsules, nanomicelles and nanoliposomes. This incorporation provides advantages in the field of oncology such as reduced/non-drug toxicity, improved aqueous solubility, specific-site drug delivery and drug cellular internalization, the overcoming of drug resistance, enhanced bioavailability and pharmacokinetics. Conclusion: As proved by recent reports, artemisinin and its derivatives have useful effects against cancer cells, especially when incorporated with nanocarriers. Hence, use of nanoparticles loaded with artemisinin and its derivatives is recommended as potential anticancer therapeutics.