ABSTRACT
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.
Subject(s)
Antineoplastic Agents, Phytogenic/administration & dosage , Antineoplastic Agents, Phytogenic/pharmacology , Choroid Neoplasms/drug therapy , Drug Carriers/chemistry , Garlic/chemistry , Melanoma/drug therapy , Mistletoe/chemistry , Polyurethanes/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Cell Line, Tumor , Cell Proliferation/drug effects , Cell Survival/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Mesenchymal Stem Cells/drug effects , Particle Size , Plant Extracts/administration & dosage , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Structure-Activity RelationshipABSTRACT
BACKGROUND: In the last years pectin and other hydrocolloids were tested for improving the color stability and the retention of bioactive compounds in gelled fruit-based products. In line with these concerns, our study has been directed to quantify the changes in antioxidant status and color indices of blackberry jam obtained with different types of pectin (degree of esterification: DE, degree of amidation: DA) and doses in response to processing and storage for 1, 3 and 6 months at 20°C. RESULTS: Blackberry jam was obtained by a traditional procedure used in households or small-scale systems with different commercial pectins (HMP: high-methoxyl pectin, LMP: low-methoxyl pectin and LMAP: low-methoxyl amidated pectin) added to three concentrations (0.3, 0.7 and 1.0%) and investigated in terms of total monomeric anthocyanins (TMA), antioxidant capacity expressed as ferric reducing antioxidant power (FRAP), total phenolics (TP), color density (CD) and percent of polymeric color, PC (%). Thermal processing resulted in significant depreciation of analyzed parameters reported to the corresponding values of fresh fruit as follows: TMA (69-82%), TP (33-55%) and FRAP (18-52%). Biologically active compounds and color were best retained one day post-processing in jams with LMAP followed by samples with LMP and HMP. Storage for 6 months brings along additional dramatic losses reported to the values recorded one day post-processing as follows: TMA (31-56%), TP (29-51%) and FRAP (20-41%). Also, both processing and storage resulted in significant increases in PC (%). The pectin type and dosage are very influential factors for limiting the alterations occurring in response to processing and storage. The best color retention and the highest TMA, TP and FRAP were achieved by LMAP, followed by LMP and HMP. Additionally, a high level of bioactive compounds in jam could be related to a high dose of pectin. LMAP to a level of 1% is the most indicated to provide the highest antioxidant properties in jam. CONCLUSIONS: The retention of bioactive compounds and jam color stability were strongly dependent on the pectin type and dosage. By a proper selection of pectin type and dose could be limited the losses recorded in response to processing and storage.
