Nanostructured lipid carriers co-encapsulating Apigenin and Melatonin: An innovative strategy against cancer
Cancer affects 9 million people every year constituting one of the main causes of death. However, current treatments are frequently associated with adverse effects and can exhibit limitations in therapeutic efficacy. Therefore, the combination of the pharmaceutical properties of the natural flavone...
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Elsevier
2025-02-01
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| Series: | Materials & Design |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S0264127524009481 |
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| author | Lorena Bonilla-Vidal Marta Świtalska Marta Espina Joanna Wietrzyk María Luisa García Eliana B Souto Anna Gliszczyńska Elena Sánchez-López |
| author_facet | Lorena Bonilla-Vidal Marta Świtalska Marta Espina Joanna Wietrzyk María Luisa García Eliana B Souto Anna Gliszczyńska Elena Sánchez-López |
| author_sort | Lorena Bonilla-Vidal |
| collection | DOAJ |
| description | Cancer affects 9 million people every year constituting one of the main causes of death. However, current treatments are frequently associated with adverse effects and can exhibit limitations in therapeutic efficacy. Therefore, the combination of the pharmaceutical properties of the natural flavone Apigenin (APG) and the neurohormone Melatonin (MEL), could represent a key finding for tumoral processes. However, both possess low aqueous solubility and photosensitivity. To overcome these limitations, APG and MEL are encapsulated into nanostructured lipid carriers (NLC) based on rosehip oil, to increase their bioavailability and efficacy. Optimization, physicochemical characterization, biopharmaceutical behaviour, and in vitro studies were assessed and compared to individually-loaded NLC. Optimized APG-MEL-NLC owned suitable physicochemical properties with an average size below 200 nm, low polydispersity index, negative charge and high encapsulation efficiency. Biopharmaceutical studies demonstrated that both compounds were released from NLC in a prolonged and sustained manner, following a biphasic behaviour with an initial fast release followed by a slow phase. Cytotoxicity studies showed selective cytotoxicity in tumoral cell lines, especially in the leukaemia cells, where co-encapsulation resulted in an additive pharmacological effect against individually loaded NLC. This novel and natural treatment could open a new therapeutical window in cancer treatment. |
| format | Article |
| id | doaj-art-98fb26e157c6497f87832eed0b733eff |
| institution | Kabale University |
| issn | 0264-1275 |
| language | English |
| publishDate | 2025-02-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Materials & Design |
| spelling | doaj-art-98fb26e157c6497f87832eed0b733eff2025-01-03T04:08:34ZengElsevierMaterials & Design0264-12752025-02-01250113573Nanostructured lipid carriers co-encapsulating Apigenin and Melatonin: An innovative strategy against cancerLorena Bonilla-Vidal0Marta Świtalska1Marta Espina2Joanna Wietrzyk3María Luisa García4Eliana B Souto5Anna Gliszczyńska6Elena Sánchez-López7Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028, Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028 Barcelona, SpainDepartment of Experimental Oncology, Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Weigla 12, 53-114 Wrocław, PolandDepartment of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028, Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028 Barcelona, SpainDepartment of Experimental Oncology, Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Weigla 12, 53-114 Wrocław, PolandDepartment of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028, Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028 Barcelona, SpainUCD School of Chemical and Bioprocess Engineering, University College Dublin, Belfield, Dublin 4, D04 C1P1, IrelandDepartment of Food Chemistry and Biocatalysis, Wrocław University of Environmental and Life Sciences, Norwida 25, 50-375 Wrocław, Poland; Corresponding authors.Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028, Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028 Barcelona, Spain; Corresponding authors.Cancer affects 9 million people every year constituting one of the main causes of death. However, current treatments are frequently associated with adverse effects and can exhibit limitations in therapeutic efficacy. Therefore, the combination of the pharmaceutical properties of the natural flavone Apigenin (APG) and the neurohormone Melatonin (MEL), could represent a key finding for tumoral processes. However, both possess low aqueous solubility and photosensitivity. To overcome these limitations, APG and MEL are encapsulated into nanostructured lipid carriers (NLC) based on rosehip oil, to increase their bioavailability and efficacy. Optimization, physicochemical characterization, biopharmaceutical behaviour, and in vitro studies were assessed and compared to individually-loaded NLC. Optimized APG-MEL-NLC owned suitable physicochemical properties with an average size below 200 nm, low polydispersity index, negative charge and high encapsulation efficiency. Biopharmaceutical studies demonstrated that both compounds were released from NLC in a prolonged and sustained manner, following a biphasic behaviour with an initial fast release followed by a slow phase. Cytotoxicity studies showed selective cytotoxicity in tumoral cell lines, especially in the leukaemia cells, where co-encapsulation resulted in an additive pharmacological effect against individually loaded NLC. This novel and natural treatment could open a new therapeutical window in cancer treatment.http://www.sciencedirect.com/science/article/pii/S0264127524009481Lipid nanoparticlesApigeninMelatonin, cancerNatural compounds, co-encapsulation |
| spellingShingle | Lorena Bonilla-Vidal Marta Świtalska Marta Espina Joanna Wietrzyk María Luisa García Eliana B Souto Anna Gliszczyńska Elena Sánchez-López Nanostructured lipid carriers co-encapsulating Apigenin and Melatonin: An innovative strategy against cancer Materials & Design Lipid nanoparticles Apigenin Melatonin, cancer Natural compounds, co-encapsulation |
| title | Nanostructured lipid carriers co-encapsulating Apigenin and Melatonin: An innovative strategy against cancer |
| title_full | Nanostructured lipid carriers co-encapsulating Apigenin and Melatonin: An innovative strategy against cancer |
| title_fullStr | Nanostructured lipid carriers co-encapsulating Apigenin and Melatonin: An innovative strategy against cancer |
| title_full_unstemmed | Nanostructured lipid carriers co-encapsulating Apigenin and Melatonin: An innovative strategy against cancer |
| title_short | Nanostructured lipid carriers co-encapsulating Apigenin and Melatonin: An innovative strategy against cancer |
| title_sort | nanostructured lipid carriers co encapsulating apigenin and melatonin an innovative strategy against cancer |
| topic | Lipid nanoparticles Apigenin Melatonin, cancer Natural compounds, co-encapsulation |
| url | http://www.sciencedirect.com/science/article/pii/S0264127524009481 |
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