Next Article in Journal
Constructed Wetland Revealed Efficient Sulfamethoxazole Removal but Enhanced the Spread of Antibiotic Resistance Genes
Next Article in Special Issue
Phage Display-Based Nanotechnology Applications in Cancer Immunotherapy
Previous Article in Journal
Measuring Sulforaphane and Its Metabolites in Human Plasma: A High Throughput Method
Previous Article in Special Issue
Nanomedicine and Immunotherapy: A Step Further towards Precision Medicine for Glioblastoma
Open AccessArticle

Encapsulation of Variabilin in Stearic Acid Solid Lipid Nanoparticles Enhances Its Anticancer Activity in Vitro

1
School of Pharmacy, University of the Western Cape, Bellville 7535, South Africa
2
Department of Science and Technology/Mintek Nanotechnology Innovation Centre (DST/Mintek NIC), Biolabels Node, Department of Biotechnology, University of the Western Cape, Bellville 7535, South Africa
3
Department of Environmental Affairs, Oceans and Coasts Research Chief Directorate, Marine Biodiversity and Ecosystems Research, Victoria & Alfred Waterfront, P.O. Box 52126, Cape Town 8000, South Africa
4
Department of Biodiversity and Conservation Biology, University of the Western Cape, Bellville 7535, South Africa
5
Department of Biological Sciences, University of Cape Town, Private Bag X3, Rondebosch, Cape Town 7701, South Africa
6
Department of Chemistry, University of the Western Cape, Bellville 7535, South Africa
*
Author to whom correspondence should be addressed.
Molecules 2020, 25(4), 830; https://doi.org/10.3390/molecules25040830
Received: 10 January 2020 / Revised: 3 February 2020 / Accepted: 6 February 2020 / Published: 14 February 2020
(This article belongs to the Special Issue Recent Advances in Precision Nanomedicine for Cancer)
The use of natural products as chemotherapeutic agents is well established; however, many of these are associated with undesirable side effects, including high toxicity and instability. Furthermore, the development of drug resistant cancers makes the search for new anticancer lead compounds a priority. In this study, the extraction of an Ircinia sp. sponge resulted in the isolation of an inseparable mixture of (7E,12E,20Z)-variabilin (1) and (7E,12Z,20Z)-variabilin (2) and structural assignment was established using standard 1D and 2D NMR experiments. The cytotoxic activity of the compound against three solid tumour cell lines displayed moderate anti-cancer activity through apoptosis, together with a general lack of selectivity among the cancer cell lines studied. Structural assignment and cytotoxic evaluation of variabilin was complicated and further aggravated by its inherent instability. Variabilin was therefore incorporated into solid lipid nanoparticles (SLNs) and the stability and cytotoxic activity evaluated. Encapsulation of variabilin into SLNs led to a marked improvement in stability of the natural product coupled with enhanced cytotoxic activity, particularly against the prostate (PC-3) cancer cell line, with IC50 values of 87.74 μM vs. 8.94 μM for the variabilin alone and Var-SLN, respectively. Both variabilin and Var-SLN revealed comparable activity to Ceramide against the MCF-7 breast cancer cell line, revealing IC50 values of 34.8, 38.1 and 33.6 μM for variabilin, Var-SLN and Ceramide, respectively. These samples revealed no activity (>100 μM for all) against HT-29 (colon) cell lines and MCF-12 (normal breast) cell lines. Var-SLNs induced 47, 48 and 59% of apoptosis in HT-29, MCF-7 and PC-3 cells, respectively, while variabilin alone revealed 38, 29 and 29% apoptotic cells for HT-29, MCF-7 and PC-3 cell lines, respectively. The encapsulation of natural products into SLNs may provide a promising approach to overcome some of the issues hindering the development of new anticancer drugs from natural products. View Full-Text
Keywords: marine natural products; variabilin; Ircinia sp.; sponge; solid lipid nanoparticles; anti-cancer activity marine natural products; variabilin; Ircinia sp.; sponge; solid lipid nanoparticles; anti-cancer activity
Show Figures

Figure 1

MDPI and ACS Style

Lerata, M.S.; D’Souza, S.; Sibuyi, N.R.; Dube, A.; Meyer, M.; Samaai, T.; Antunes, E.M.; Beukes, D.R. Encapsulation of Variabilin in Stearic Acid Solid Lipid Nanoparticles Enhances Its Anticancer Activity in Vitro. Molecules 2020, 25, 830.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop