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Encapsulation and Enhanced Release of Resveratrol from Mesoporous Silica Nanoparticles for Melanoma Therapy
Diogo Marinheiro1, Bárbara J M L Ferreira1, Párástu Oskoei2
1Department of Chemistry & CICECO-Aveiro Institute of Materials, University of Aveiro, 3810-193 Aveiro, Portugal.
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~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.
Insights
Resveratrol (RES)-loaded mesoporous silica nanoparticles show promise for treating melanoma. These nanoparticles enhance RES delivery and exhibit potent anti-cancer effects against human melanoma cells in vitro.
Area of Science:
- Nanotechnology
- Materials Science
- Pharmacology
Background:
- Chemotherapy for malignant melanoma is limited by drug resistance and poor bioavailability.
- Resveratrol (RES), a natural polyphenol, possesses anti-cancer properties but suffers from low solubility.
- Effective drug delivery systems are needed to improve RES efficacy for cancer treatment.
Purpose of the Study:
- To evaluate RES-loaded mesoporous silica nanoparticles (MSNs) as a potential treatment for human melanoma.
- To characterize RES encapsulation, release kinetics, and in vitro cytotoxicity of RES-MSNs.
Main Methods:
- Efficient loading of RES onto spheroidal MSNs (size ~60 nm) with >93% efficiency.
- In vitro release studies at different pH values (5.2 and 7.4) and cytotoxicity assays on A375 and MNT-1 melanoma cell lines.
- Analysis of RES amorphization and release kinetics using the Weibull model.
Main Results:
- RES encapsulation in MSNs enhanced its in vitro release, particularly at acidic pH (5.2).
- RES release from MSNs was gradual, without a burst effect, and followed Weibull kinetics.
- RES-MSNs demonstrated significant in vitro cytotoxicity against both amelanotic (A375) and melanotic (MNT-1) human melanoma cells, with A375 being more sensitive.
Conclusions:
- RES-loaded MSNs represent a promising nanocarrier system for improving RES delivery and anti-cancer activity against melanoma.
- The pH-dependent release profile of RES-MSNs could be advantageous for targeted tumor therapy.
- Further investigation into RES-MSNs for melanoma treatment is warranted based on these in vitro findings.
