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Long-circulating and fusogenic liposomes loaded with a glucoevatromonoside derivative induce potent antitumor response.

A new interesting article has been published in Biomed Pharmacother. 2018 Dec;108:1152-1161. doi: 10.1016/j.biopha.2018.09.109. Epub 2018 Oct 1. and titled:

Long-circulating and fusogenic liposomes loaded with a glucoevatromonoside derivative induce potent antitumor response.

Authors of this article are:

Gomes ER, Novais MVM, Silva IT, Barros ALB, Leite EA, Munkert J, Frade ACM, Cassali GD, Braga FC, Pádua RM, Oliveira MC.

A summary of the article is shown below:

Cancer is an important public health problem, being one of the leading causes of death worldwide. Most antineoplastic agents cause severe toxic effects and some types of cancer do not respond or are resistant to the existing pharmacotherapy, necessitating the research and development of new therapeutic strategies. Cardenolides have shown significant antitumor activity due to their ability to inhibit the Na+K+ATPase enzyme, and the expression of this enzyme is increased in tumor cells. Glucoevatromonoside containing peracetylated glucose hydroxyl groups (GEVPG) is a cardenolide derivative that has low solubility in aqueous media, which constitutes a barrier to its potential biological applications. In this context, the use of liposomes represents a promising strategy to deliver GEVPG, thus allowing its intravenous administration. In this study, long-circulating and fusogenic liposomes containing GEVPG (SpHL-GEVPG) were developed, and their chemical and physicochemical properties were evaluated. SpHL-GEVPG presented adequate properties, including a mean diameter of 182.2 ± 2.7 nm, a polydispersity index equal to 0.36 ± 0.03, a zeta potential of -2.37 ± 0.31 mV, and a GEVPG entrapment of 0.38 ± 0.04 mg/mL. Moreover, this formulation showed a good stability after having been stored for 30 days at 4 °C. The cytotoxic studies against breast (MDA-MB-231, MCF-7, and SKBR-3) and lung (A549) cancer cell lines demonstrated that SpHL-GEVPG treatment significantly reduced the cell viability. In addition, the SpHL-GEVPG formulation presented a good selectivity toward these cancer cells. The evaluation of the therapeutic efficacy of the treatment with SpHL-GEVPG showed a potent anticancer effect in an A549 human lung cancer xenograft model. SpHL-GEVPG administered at doses of 1.0 and 2.0 mg/kg (i.v.) induced antitumor effect comparable to paclitaxel given at dose of 10 mg/kg (i.v.) to mice. Therefore, the results of the present work indicate the potential applicability of SpHL-GEVPG as a new anticancer formulation.

Check out the article’s website on Pubmed for more information:

This article is a good source of information and a good way to become familiar with topics such as:

Antitumor efficacy;Breast cancer;Cardenolide;Cytotoxicity;Liposomes;Lung cancer


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