Encapsulation and Enhanced Release of Resveratrol from Mesoporous Silica Nanoparticles for Melanoma Therapy

abstract

Chemotherapy has limited success in the treatment of malignant melanoma due to fast development of drug resistance and the low bioavailability of chemotherapeutic drugs. Resveratrol (RES) is a natural polyphenol with recognized preventive and therapeutic anti-cancer properties. However, poor RES solubility hampers its bioactivity, thus creating a demand for suitable drug delivery systems to improve it. This work aimed to assess the potential of RES-loaded mesoporous silica nanoparticles (MSNs) for human melanoma treatment. RES was efficiently loaded (efficiency > 93%) onto spheroidal (size similar to 60 nm) MSNs. The encapsulation promoted the amorphization of RES and enhanced the release in vitro compared to non-encapsulated RES. The RES release was pH-dependent and markedly faster at pH 5.2 (acid environment in some tumorous tissues) than at pH 7.4 in both encapsulated and bulk forms. The RES release from loaded MSNs was gradual with time, without a burst effect, and well-described by the Weibull model. In vitro cytotoxicity studies on human A375 and MNT-1 melanoma cellular cultures showed a decrease in the cell viability with increasing concentration of RES-loaded MSNs, indicating the potent action of the released RES in both cell lines. The amelanotic cell line A375 was more sensitive to RES concentration than the melanotic MNT-1 cells.

subject category

Chemistry, Physical; Materials Science, Multidisciplinary; Metallurgy & Metallurgical Engineering; Physics, Applied; Physics, Condensed Matter

authors

Marinheiro, D; Ferreira, BJML; Oskoei, P; Oliveira, H; Daniel-da-Silva, AL

Groups

G1 - Porous Materials and Nanosystems

Projects

CICECO - Aveiro Institute of Materials (UIDB/50011/2020)

CICECO - Aveiro Institute of Materials (UIDP/50011/2020)

HOTsPOT - Novel upconversion nanoparticles for multimodal therapy of melanoma: pHOtothermal Therapy, PhOtodynamic therapy and chemoTherapy (HOTsPOT)

Projeto de Investigação Exploratória: Ana Luísa Silva (IF/00405/2014)

acknowledgements

The costs resulting from the FCT hiring is funded by national funds (OE), through FCTFundacao para a Ciencia e a Tecnologia, I.P., in the scope of the framework contract foreseen in the numbers 4, 5 and 6 of the article 23, of the Decree-Law 57/2016, of August 29, changed by Law 57/2017, of July 19. This work was developed within the scope of the projects CICECO-Aveiro Institute of Materials, UIDB/50011/2020 & UIDP/50011/2020, and CESAM UIDB/50017/2020 & UIDP/50017/2020, financed by national funds through the FCT/MEC and when appropriate co-financed by FEDER under the PT2020 Partnership Agreement. This work was supported by the project PTDC/BTM-MAT/31794/2017 (POCI-01-0145-FEDER-031794) funded by FEDER, through COMPETE2020-Programa Operacional Competitividade e Internacionalizacao (POCI), and by national funds (OE), through FCT/MCTES. A. L. Daniel-da-Silva thanks Portuguese Foundation for Science and Technology (FCT) for funding in the frame of the program IF2014 (project IF/00405/2014). H. Oliveira thanks FCT for the research contract under Scientific Employment Stimulus (CEECIND/04050/2017).