In vitro anti-cancer effects of artemisone nano-vesicular formulations on melanoma cells

Dwivedi, Anupma; Mazumder, Anisha; Plessis, Lissinda H. Du; Preez, Jan L. du; Haynes, Richard K.; Plessis, Jeanetta du

doi:10.1016/j.nano.2015.07.010

Cited by 92 publications

(55 citation statements)

References 35 publications

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“…Overall, in conjunction with evolvingt he synthetic routes described here to generate more soluble artemisinin-cholesterol conjugates, resort will also be made to generating lipophilic formulations of the currentc ompounds in order to facilitatea dministration. [43] The antimycobacterial activity of the compounds against Mtb H37Rvw as assessed by treatingc ultures with 10 and 80 mm of the drug dissolved in DMSO followed by incubation for 24 h. Colony-forming unit (CFU) enumeration for 12-15 days was carried out following plating of the cultures on agar. Cholesterol, the artemisinin artemether 3 (Figure 1), the DHApiperazine derivative 10 (Scheme1), and the known TB drug isoniazid were used as comparator compounds.…”

Section: Biological Activitiesmentioning

confidence: 99%

Preliminary Evaluation of Artemisinin–Cholesterol Conjugates as Potential Drugs for the Treatment of Intractable Forms of Malaria and Tuberculosis

et al. 2017

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To evaluate the feasibility of developing drugs that may be active against both malaria and tuberculosis (TB) by using in part putative cholesterol transporters in the causative pathogens and through enhancement of passive diffusion in granulomatous TB, artemisinin–cholesterol conjugates were synthesized by connecting the component molecules through various linkers. The compounds were screened in vitro against Plasmodium falciparum (Pf) and Mycobacterium tuberculosis (Mtb). Antimalarial activities (IC50) against Pf drug‐sensitive NF54, and drug‐resistant K1 and W2 strains ranged from 0.03–2.6, 0.03–1.9, and 0.02–1.7 μm. Although the compounds are less active than the precursor artemisinin derivatives, the cholesterol moiety renders the compounds relatively insoluble in the culture medium, and variation in solubilities among the different compounds may reflect in the range of efficacies observed. Activities against Mtb H37Rv were assessed using a standardized colony‐forming unit (CFU) assay after 24 h pretreatment of cultures with each of the compounds. Percentage inhibition ranged from 3–38 % and 18–52 % at 10 and 80 μm, respectively. Thus, in contrast to the comparator drug artemether, the conjugates display enhanced activities. The immediate aims include the preparation of conjugates with enhanced aqueous solubilities, assays against malaria and TB in vivo, and for TB, assays using an infected macrophage model and assessment of granuloma influx.

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Section: Biological Activitiesmentioning

confidence: 99%

Preliminary Evaluation of Artemisinin–Cholesterol Conjugates as Potential Drugs for the Treatment of Intractable Forms of Malaria and Tuberculosis

et al. 2017

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“…SLNs and SLNs-based systems to deliver cytotoxic drugs have been used, and doxorubicin loaded SLNs for improving the efficacy of MDR cancer chemotherapy [2] is one of the glaring examples. The artemisone loaded SLNs have been used for efficient targeting of melanoma cells in treating skin cancer [3]. A number of strategies have been devised to meet major challenges in the anti-cancer drug delivery using SLNs including; i) encapsulation of water-soluble anti-cancer compounds, ii) control of rate and extent of drug release, and iii)…”

Section: Introductionmentioning

confidence: 99%

Fucose decorated solid-lipid nanocarriers mediate efficient delivery of methotrexate in breast cancer therapeutics

Garg

Singh

Jain

et al. 2016

Colloids and Surfaces B: Biointerfaces

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“…To improve the efficacy of artemisinin, Dwivedi et al encapsulated the compound in nanovesicular niosomes. Results show that the encapsulated artemisinin was cytotoxic toward melanoma cells with negligible toxicity toward normal skin cells, suggesting its potential as a useful therapeutic strategy for the treatment of melanoma [68].…”

Section: Neoplasiamentioning

confidence: 99%

Niosomes: a review of their structure, properties, methods of preparation, and medical applications

et al. 2017

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Target-specific drug-delivery systems for the administration of pharmaceutical compounds enable the localization of drugs to diseased sites. Various types of drug-delivery systems utilize carriers, such as immunoglobulins, serum proteins, synthetic polymers, liposomes, and microspheres. The vesicular system of niosomes, with their bilayer structure assembled by nonionic surfactants, is able to enhance the bioavailability of a drug to a predetermined area for a period. The amphiphilic nature of niosomes promotes their efficiency in encapsulating lipophilic or hydrophilic drugs. Other additives, such as cholesterol, can be used to maintain the rigidity of the niosomes' structure. This narrative review describes fundamental aspects of niosomes, including their structural components, methods of preparation, limitations, and current applications to various diseases.

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In vitro anti-cancer effects of artemisone nano-vesicular formulations on melanoma cells

Cited by 92 publications

References 35 publications

Preliminary Evaluation of Artemisinin–Cholesterol Conjugates as Potential Drugs for the Treatment of Intractable Forms of Malaria and Tuberculosis

Preliminary Evaluation of Artemisinin–Cholesterol Conjugates as Potential Drugs for the Treatment of Intractable Forms of Malaria and Tuberculosis

Fucose decorated solid-lipid nanocarriers mediate efficient delivery of methotrexate in breast cancer therapeutics

Niosomes: a review of their structure, properties, methods of preparation, and medical applications

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