Novel Strategies against Cancer: Dexibuprofen-Loaded Nanostructured Lipid Carriers

Abstract

The aim of this work was to design innovative nanostructured lipid carriers (NLCs) for the delivery of dexibuprofen (DXI) as an antiproliferative therapy against tumoral processes, and overcome its side effects. DXI-NLC samples were prepared with beeswax, Miglyol 812 and Tween 80 using high-pressure homogenization. A two-level factorial design 24 was applied to optimize the formulation, and physicochemical properties such as particle size, zeta potential, polydispersity index and entrapment efficiency were measured. Optimized parameters of DXI-NLCs exhibited a mean particle size of 152.3 nm, a polydispersity index below 0.2, and high DXI entrapment efficiency (higher than 99%). Moreover, DXI-NLCs provided a prolonged drug release, slower than the free DXI. DXI-NLCs were stable for 2 months and their morphology revealed that they possess a spherical shape. In vitro cytotoxicity and anticancer potential studies were performed towards prostate (PC-3) and breast (MDA-MB-468) cancer cell lines. The highest activity of DXI-NLCs was observed towards breast cancer cells, which were effectively inhibited at 3.4 μM. Therefore, DXI-NLCs constitute a promising antiproliferative therapy that has proven to be especially effective against breast cancer.

Diclofenac Loaded Biodegradable Nanoparticles as Antitumoral and Antiangiogenic Therapy

“…Moreover, data was adjusted to the most common kinetic models, showing that the release profile corresponds to a hyperbola equation [ 1 , 25 , 51 ]. Both DCF NPs and free DCF data were adjusted, and the results can be observed in Figure 4 .…”

“…In order to remove microbial contamination, DCF NPs were sterilized using 25 kGy of 60 Co as γ-irradiation source (Aragogamma, Barcelona, Spain) [ 1 ]. This corresponds to a standard dose to sterilize pharmaceutical products when bioburden is not known.…”

“…In case of cells of line A549 RPMI 1640+Opti-MEM (1:1) (IIET PAS, Poland and Gibco, UK) supplemented with 5% fetal bovine serum was used as the medium (Merck, Germany) whereas breast cancer cells line MCF-7 were cultured in Eagle medium (IIET PAS, Poland) containing 8 µg/mL of insulin and 1% of MEM non-essential amino acid (all Merck, Germany). Medium HAM’S F-12 medium (Corning) supplemented with 10% horse serum (Gibco), 20 ng/mL EGFh, 10 µg/mL insulin, 0.5 µg/mL hydrocortisone and 0.05 mg/mL cholera toxin from Vibrio cholerae (all from Merck, Germany) was used for MCF-10A cells [ 1 ]. Moreover, all used for cells growth media were supplemented with 2 mM L-glutamine (Merck, Germany), 100 units/mL penicillin, (Polfa Tarchomin S.A., Warszawa, Poland) and 100 µg/mL streptomycin (Merck, Germany).…”

“…Regardless of type, cancer is still considered as the second leading cause of death worldwide, representing a serious public health problem [ 1 ]. The changes of a healthy cell into a tumoral one follow a slow pathway that requires specific abilities (e.g., resistance against cell death, evasion of the immune system, induction of angiogenesis and/or activation of metastasis), all known as hallmarks of cancer [ 2 , 3 , 4 ].…”

Novel Strategies in the Development of New Therapies, Drug Substances, and Drug Carriers Volume II

“…The chiral metabolic inversion may cause the accumulation of one of the enantiomers, leading to toxicity. To overcome the side effects of dextrorotary ibuprofen (DXI), Thiruchenthooran et al [ 8 ] designed nanostructured lipid carriers (NLCs) of DXI to be used in anticancer therapy. The formulation was optimized by a two-level factorial design.…”