Nanomedicine: Nanotechnology, Biology and Medicine
Original ArticleIn vitro anti-cancer effects of artemisone nano-vesicular formulations on melanoma cells
Graphical Abstract
Artemisone, a new artemisinin derivative, was encapsulated in nano-vesicular niosome and solid lipid nanoparticles with the aim of enhancing its efficacy against melanoma cells. The formulated artemisone displayed highly selective and significant cytotoxicity when compared to free artemisone. The toxicity of these formulations was also evaluated on human keratinocytes; no significant effects were observed, thus indicating a substantial safety profile. Importantly, these formulations also ameliorated the effects of artemisone on human keratinocytes when compared to free artemisone. The results overall suggest a potent therapeutic strategy that needs to be evaluated for the treatment of melanoma and other cancers.
Section snippets
Methods
Full details of materials and methods appear in the supplementary material.
Particle size and zeta potential of niosomes and SLNs
Since adequate characterisation of these nano-vesicles is crucial for ensuring reproducibility of the results, particle size, zeta potential, structure morphology, encapsulation efficiency of the niosomes and SLNs were carefully evaluated. The size ranges (nm), zeta potentials (mV) and encapsulation efficiencies (EE%) obtained are listed in Table 1. For preparation of the niosomes, the effect of the sorbitan monostearate:cholesterol ratio on the stability and size of the niosomes was evaluated.
Discussion
This study was aimed at evaluating the anticancer effects of artemisone and its nano-vesicular formulation on human melanoma cells with normal human keratinocytes being used as a control. Artemisone was entrapped into two different types of nano-vesicles – niosomes and SLNs. It was anticipated that due to their nanoscale structure, these carriers would efficiently penetrate the cells and enhance drug efficacy according to literature precedent involving other drugs.19, 20, 21, 22 One previous
Acknowledgements
We would like to thank Laura Guembe (Servicio de Morfología, Centro para la Investigación Médica Aplicada, CIMA), Ainhoa Urbiola and Cristina Ederra (Unidad de Imagen, CIMA) for their excellent technical support with imaging techniques.
References (38)
- et al.
Artemisinins: their growing importance in medicine
Trends Pharmacol Sci
(2008) - et al.
Etoposide loaded solid lipid nanoparticles for curtailing B16F10 melanoma colonization in lung
Biomed Pharmacother
(2014) - et al.
Pharmacokinetics study of arteether loaded solid lipid nanoparticles: an improved oral bioavailability in rats
Int J Pharm
(2014) - et al.
Curcuminoids-loaded liposomes in combination with arteether protects against Plasmodium berghei infection in mice
Exp Parasitol J
(2012) - et al.
Absorption of the novel artemisinin derivatives artemisone and artemiside: potential application of Pheroid™ technology
Int J Pharm
(2011) - et al.
Emodin loaded solid lipid nanoparticles: preparation, characterization and antitumor activity studies
Int J Pharm
(2012) - et al.
Apoptosis and beyond: cytometry in studies of programmed cell death
Methods Cell Biol
(2011) - et al.
Elevated copper and oxidative stress in cancer cells as a target for cancer treatment
Cancer Treat Rev
(2009) - et al.
Prognostic factors in metastatic melanoma: a pooled analysis of Eastern Cooperative Oncology Group trials
J Clin Oncol
(2000) - et al.
Caspase independent induction of apoptosis in human melanoma cells by the proapoptotic Bcl-2-related protein Nbk/Bik
Oncogene
(2005)
Surgery for distant melanoma metastasis
Cancer J
Antimalaria studies on qinghaosu
Chin Med J
Qinghaosu (artemisinin): an antimalarial drug from China
Science
Cytotoxicity of artemisinin-related endoperoxides to Ehrlich ascites tumor cells
J Nat Prod
Modulation of multidrug resistance by artemisinin, artesunate and dihydroartemisinin in K562/adr and GLC4/adr resistant cell lines
Biol Pharm Bull
Molecular modes of action of artesunate in tumour cell lines
Mol Pharmacol
Antitumor activity of artemisinin and its derivatives: from a well-known antimalarial agent to a potential anticancer drug
J Biomed Biotechnol
Development of artemisinin compounds for cancer treatment
Investig New Drugs
Considerations on the mechanism of action of artemisinin antimalarials: part 1—the 'carbon radical' and 'heme' hypotheses
Infect Disord Drug Targets
Cited by (0)
Source of funding: This work was carried out with the financial support of the National Research Foundation of South Africa (NRF) (grants no. IFRR81178 and CPRR13091742482), the MAL-TB REDOX MRC Flagship Project and the Centre of Excellence for Pharmaceutical Sciences (Pharmacen) of the North-West University, Potchefstroom Campus, South Africa.
Disclaimer: Any opinions, findings and conclusions, or recommendations expressed in this material are those of the authors and therefore the NRF does not accept any liability in regard thereto.
Conflict of Interest: None of the authors have any conflict of interest to declare.