Impact of solid lipid nanoparticles on 3T3 fibroblasts viability and lipid profile: The effect of curcumin and resveratrol loading

Abstract

This study focused on the impact in 3T3 fibroblasts of several types of empty and curcumin-and resveratrol-loaded solid lipid nanoparticles (SLN) on cell viability and lipid metabolism in relation to their lipid content and encapsulated drug. SLN, prepared by hot homogenization/ultrasonication, were characterized with respect to size, polydispersity index, and zeta potential. Compritol ® 888 ATO at different concentrations (4%, 5%, and 6% wt/wt) was chosen as lipid matrix while Poloxamer 188 (from 2.2% to 3.3% wt/wt) and Transcutol (TRC; 2% or 4%) were added as nanoparticle excipients. Prepared SLN were able to encapsulate high drug amount (encapsulation efficiency percentage of about 97-99%). All empty SLN did not show cytotoxicity (by MTT assay, at 24 h of incubation) in 3T3 cells independently of the lipid and TRC amount, while a viability reduction in the range 5-11% and 12-27% was observed in 3T3 cells treated with curcumin-loaded and resveratrol-loaded SLN, respectively. SLN without TRC did not affect cell lipid metabolism, independently from the lipid content. Empty and loaded SLN formulated with 4% of Compritol and 4% of TRC significantly affected, after 24 h of incubation at the dose of 5 μl/ml, cell polar lipids (phospholipids and free cholesterol) and fatty acid profile, with respect to control cells. Loaded compounds significantly modulated the impact of the corresponding empty formulation on cell lipids. Therefore, the combined impact on lipid metabolism of SLN and loaded drug should be taken in consideration in the evaluation of the toxicity, potential application, and therapeutic effects of new formulations.

Xanthomicrol Activity in Cancer HeLa Cells: Comparison with Other Natural Methoxylated Flavones

“…Lipids (phosphoacylglycerols, triacylglycerols, sphingolipids, sterols, and cholesteryl esters) and their main building block fatty acids (FA), have structural, energy, signaling, and immunoregulatory functions, regulating several complex biochemical processes [ 26 , 27 ]. Deregulation of lipid and FA metabolism is one of the most important metabolic hallmarks of cancer cells [ 24 ].…”

“…The impact on lipid profile was analyzed in XAN-treated cancer cells together with the investigation of the changes occurring in the cell growth, cell morphology, cell cycle, and apoptosis appearance. Finally, the XAN effect on cell viability was tested in 3T3 fibroblasts, a normal cell line previously used to assess the toxicity and biocompatibility of nanoparticles and natural compounds [ 26 ]. The bioactivity profile of XAN was compared to that of the anticancer flavones EUP [ 6 ], a XAN chemical analog, and ART, characterized by a higher extent of methoxylation in the A and C rings than XAN [ 3 ], in the perspective to underline structure–activity relationships.…”

Waste Citrus limon Leaves as Source of Essential Oil Rich in Limonene and Citral: Chemical Characterization, Antimicrobial and Antioxidant Properties, and Effects on Cancer Cell Viability

“…The cytotoxic effect of LLEO was evaluated in cancer HeLa cells, A375 melanoma cells, 3T3 fibroblasts, and HaCaT cells by the MTT colorimetric assay [ 34 , 35 ]. Cells were seeded in 96-well plates at a density of 3 × 10 4 cells/mL (HeLa and A375 cells), 10 5 cells/mL (HaCaT cells), and 3 × 10 5 cells/mL (3T3 fibroblasts) in 100 μL of complete culture medium and cultured for 48 h. Cells (at 80–90% cell confluence) were subsequently incubated (24 h) with various concentrations (2.5–500 μg/mL) of LLEO (from 50 mg/mL and 5 mg/mL solutions in DMSO) in a fresh medium (treated cells).…”

“…HeLa cells, a cell line derived from a human epithelioid cervix carcinoma, and A375 human melanoma cells represent cultured cancer cell models (Figure 3) amply used to assess the cytotoxic effect and potential antitumor properties of natural extracts and compounds [4,23,27,34,37]. Mouse 3T3 fibroblasts and human keratinocyte HaCaT cells were chosen as normal cell lines (Figure 3) as previously used to assess the biocompatibility of herbal extracts and natural-derived compounds [35,37].…”

Physicochemical Characterization, Stability, and In Vitro Evaluation of Curcumin-Loaded Solid Lipid Nanoparticles Prepared Using Biocompatible Synthetic Lipids

“…Thus, SLNs have emerged as a promising drug delivery system specifically for drugs of poor aqueous solubility. − SLNs have received massive attention because of their potential application in targeted drug delivery. SLNs usually consist of biocompatible lipids, such as fatty acids; mono-, di-, and triglycerides; and so on.…”