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Background: Melanoma is known as the most dangerous form of skin cancer; whereas the malignant choroidal melanoma is an orphan disease known as the most common primary intraocular malignancy in adults. Literature suggests that the consumption of garlic and mistletoe leads to a reduced risk of developing cancer., Objective: The aim of this study was the obtaining and the characterization of polymer structures containing mistletoe or garlic extract., Methods: The structures were obtained in a polyaddition process combined with a spontaneous emulsification; they were characterized by pH, size, Zeta potential and DSC measurements, evaluation of encapsulation efficacy, penetrability through membranes and in vitro cytotoxicity tests., Results: The microstructures present sizes between 1.05 and 2.60 µm and Zeta potentials between -7 and +36 mV. A good encapsulation was observed on different evaluations (88-92%). It was determined that approx. 30% of polymer microstructures containing vegetal extracts pass through an artificial membrane in 4 days. An in vitro cytotoxicity test revealed that these products are safe for administration. The analysis of antitumor efficacy indicates that garlic extracts have important effects after 48 and 72 hours on A375 cells; however, polymer microstructures with herbal extracts did not reveal antiproliferative activities on A375 cells because these polymer structures present a slow degradation., Conclusion: Sterile eye drops solutions based on polymer microstructures containing garlic or mistletoe extracts were obtained; the sample based on garlic extracts may be used in the pharmaceutical field as drug carrier with an antiproliferative effect which occurs after a prolong period., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)

Betulinic acid, a very promising anti-melanoma agent, has very low water solubility that causes low bioavailability. To overcome this inconvenience, a highly water-soluble cyclodextrin was used (octakis-[6-deoxy-6-(2-sulfanyl ethanesulfonic acid)]-γ-cyclodextrin). The complex was physico-chemically analyzed using differential scanning calorimetry (DSC), X-ray and scanning electron microscopy (SEM) methods and then in vitro tested for its antiproliferative activity by the MTT assay and by cell cycle analysis. Finally, the complex was tested in vivo using an animal model of murine melanoma developed in C57BL/6J mice, where it caused a reduction in tumor volume and weight. The study revealed the beneficial influence of betulinic acid inclusion into the cyclodextrin in terms of antiproliferative activity and in vivo tumor development.

Oleanolic and ursolic acids are natural triterpenic compounds with pentacyclic cholesterol-like structures which gives them very low water solubility, a significant disadvantage in terms of bioavailability. We previously reported the synthesis of inclusion complexes between these acids and cyclodextrins, as well as their in vivo evaluation on chemically induced skin cancer experimental models. In this study the synergistic activity of the acid mixture included inside hydroxypropyl-gamma-cyclodextrin (HPGCD) was monitored using in vitro tests and in vivo skin cancer models. The coefficient of drug interaction (CDI) was used to characterize the interactions as synergism, additivity or antagonism. Our results revealed an increased antitumor activity for the mixture of the two triterpenic acids, both single and in complex with cyclodextrin, thus proving their complementary biologic activities.

The isoflavonoid genistein, the aglycone of the heteroside genistin, possesses preventive effect on coronary heart disease and osteoporosis, antioxidant, anthelmintic, antineoplastic and anti-inflammatory properties. Much research has been undertaken regarding the action of genistein on cancer-preventing/treating effects, especially on breast and prostate cancer. The aim of this study was to analyze the effect of this compound in vivo by observing tumor size, metastasis potential and melanization in a mouse model of murine melanoma, employing the B164A5 melanoma cell line and C57BL/6J mice. Genistein decreased the tumor volume and weight by approximately 30%. Non-invasive measurements for both melanin and erythema showed that genistein reduced the quantity of melanin and the degree of erythema in direct proportion to the number of days of treatment. HE analysis diagnosed malignant melanoma in both groups, but no metastasis was recorded in the treated group compared with the liver metastasis in the untreated group after a period of 15 days of experiment at a dose of 15 mg/kg body weight of genistein. Genistein showed beneficial effects regarding tumor size, metastasis potential and melanization in a B16 mouse model of murine melanoma.