Nanostructured lipid carriers as a novel tool to deliver sclareol: physicochemical characterisation and evaluation in human cancer cell lines

Sclareol (SC) is arousing great interest due to its cytostatic and cytotoxic activities in several cancer cell lines. However, its hydrophobicity is a limiting factor for its in vivo administration. One way to solve this problem is through nanoencapsulation. Therefore, solid lipid nanoparticles (SLN-SC) and nanostructured lipid carriers (NLC-SC) loaded with SC were produced and compared regarding their physicochemical properties.

NLC-SC showed better SC encapsulation than SLN-SC and was chosen to be compared with free SC in human cancer cell lines (MDA-MB-231 and HCT-116). Free SC had slightly higher cytotoxicity than NLC-SC and produced subdiploid DNA content in both cell lines.

On the other hand, NLC-SC led to subdiploid content in MDA-MB-231 cells and G2/M checkpoint arrest in HCT-116 cells. These findings suggest that SC encapsulation in NLC is a way to allow the in vivo administration of SC and might alter its biological properties.

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Materials: Compritol^® 888 ATO (mixture of mono-, di- and triglycerides of behenic acid) was kindly provided by Gattefossé, France. Ethoxylated sorbitan monoleate (Tween^™ 80) and peanut oil were kindly provided by Croda, USA. Oleic acid, sodium citrate, dimethyl sulfoxide (DMSO), SC, propidium iodide, and Triton X-100 were purchased from Sigma-Aldrich, Germany. Cell Titer Blue^® (CTB) was purchased from Promega, USA. Triethanolamine was purchased from Merck, Germany. Dulbecco’s Modified Eagle’s Medium (DMEM), Fetal Bovine Serum (FBS), and streptomycin were purchased from Gibco Life Technologies, USA. The other substances used were of analytical grade without further purification.

Article information: Gabriel Silva Marques Borges, Pedro Henrique Dias Moura Prazeres, Ângelo Malachias de Souza, Maria Irene Yoshida, José Mario Carneiro Vilela, Aline Teixeira Maciel e Silva, Mariana Silva Oliveira, Dawidson Assis Gomes, Margareth Spangler Andrade, Elaine Maria de Souza-Fagundes, Lucas Antônio Miranda Ferreira. Braz. J. Pharm. Sci. 57, 2021. https://doi.org/10.1590/s2175-97902020000418497