Evaluation of antitumor effects of vitamin K2 (menaquinone-7) nanoemulsions modified with sialic acid-cholesterol conjugate (Shi et al.)

Numerous studies have recently shown that vitamin K has antitumor effects in a variety of tumor cells, but there are few reports demonstrating antitumor effects of vitamin K2 in vivo, and the antitumor effects of vitamin K2 in nanoemulsions are currently not known. Therefore, researchers sought to characterize the antitumor potential of vitamin K2 nanoemulsions in S180 tumor cells in a study recently published in Drug Delivery Translation Research.

A ligand conjugate sialic acid cholesterol, with enhanced affinity towards the membrane receptors overexpressed in tumors, was anchored on the surface of the nanoemulsions to increase vitamin K2 as menaquinone-7 (MK-7) distribution to the tumor tissue. Vitamin K2 was encapsulated in oilinwater nanoemulsions, and the physical and chemical stability of the nanoemulsions were characterized during storage at 25 °C. At 25 °C, all nanoemulsions remained physically and chemically stable with little change in particle size.

An in-vivo study using syngeneic mice with subcutaneously established S180 tumors demonstrated that intravenous or intragastric administration of vitamin K2 nanoemulsions significantly suppressed the tumor growth. The vitamin K2 nanoemulsions modified with sialic acid cholesterol conjugate showed higher tumor growth suppression than the vitamin K2 nanoemulsions, while neither of them exhibited signs of drug toxicity.

At 25 °C, all nanoemulsions remained physically and chemically stable with little change in particle size. An in-vivo study using syngeneic mice with subcutaneously established S180 tumors demonstrated that intravenous or intragastric administration of vitamin K2 nanoemulsions significantly suppressed the tumor growth. The vitamin K2 nanoemulsions modified with sialic acid–cholesterol conjugate showed higher tumor growth suppression than the vitamin K2 nanoemulsions, while neither of them exhibited signs of drug toxicity.

In summary, vitamin K2 as MK-7 exerted effective antitumor effects in vivo, and vitamin K2 nanoemulsions modified with sialic acid–cholesterol conjugate enhanced the antitumor activity, suggesting that vitamin K2 may be promising agents for the prevention or treatment of tumor in patients.

 

Reference:

Shi J et al. Evaluation of the antitumor effects of vitamin K2 (menaquinone-7) nanoemulsions modified with aialic acid-cholesterol conjugate. Drug Deliv Tranl Res. 2017 Aug 28. Doi: 10.1007/s13346-017-0424-1.

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