Nanostructured lipid carriers enhance the bioavailability and brain cancer inhibitory efficacy of curcumin both in vitro and in vivo

Abstract

Brain cancer is a kind of tough carcinoma because the blood-brain barrier (BBB) remains a formidable obstacle in medicine. Curcumin (Cur) was determined to have anticancer potency on several kinds of carcinoma. However, its medical application was limited because of its poor bioavailability, unsatisfying dispersity and rapid metabolism in vivo. In this study, Cur was delivered by nanostructured lipid carriers (NLCs) for brain cancer treatment. The physiochemical characters of NLC-Cur were detected by using high-performance liquid chromatography, Transmission electron microscopy and photon correlation spectrum analyses. The cellular uptake and the anticancer efficiency were determined both in vitro and in vivo by flow cytometry detection, MTT assay, AO/EB, Annexin-V/PI, DCFDA and tumor-bearing mice. NLC-Cur was synthesized by using sol-gel method and with the size around 100 nm. After loaded in NLC, the IC 50 of NLC-Cur was 20 mg/mL, only one-fourth of the plain drug. The plasmid concentration of Cur was highly increased (6.4-folds) in mice via intraperitoneally after loaded with NLC. Furthermore, NLC-Cur enhanced the targeting effect of Cur to brain and tumor, which finally increased the inhibition efficiency of Cur from 19.5% to 82.3%. The FITC analysis confirmed that the inhibition effect mostly came from apoptosis, but not necrosis. The time depending cellular uptake, reactive oxygen species production, markedly increased bio-availability and tumor targeting effect played an important role in the efficacy of NLC-Cur. Our work indicated the medical application of NLC-Cur on brain cancer treatment, and also provided a novel method for new anticancer agents' development.

Nanostructured Lipid Carriers for Delivery of Chemotherapeutics: A Review

“…This is due to breakage of the hydrogen bonds between the surfactant molecules at the lipid/water interface as a result of increasing temperature [73]. It was also noticed that the ZP of particles stored at 22 • C was decreased at longer storage duration, which is associated to agglomeration and aggregation of the particles [19].…”

“…Glyceryl monostearate [9,[15][16][17] Glyceryl tridecanoate [18] Glyceryl tripalmitate [18,19] Glyceryl behenate (Compritol ® 888 ATO) [20][21][22][23] Stearic acid [16,24,25] Glyceryl distearate (Precirol ® ATO 5) [21,23,[26][27][28] Liquid lipids…”

Therapeutic Potential of Curcumin for the Treatment of Brain Tumors

“…Nanostructured lipid carriers (tripalmitin-oleic acid) loaded with curcumin had IC 50 of approximately 20  μ g/mL against A172 GBM cells compared to IC 50 of 80  μ g/mL with curcumin alone. Further, the authors showed that curcumin delivered with the lipid carriers to subcutaneous flank tumor bearing nude mice decreased tumor volume by 82% [74]. Polymeric micelles have also been studied for curcumin delivery.…”

High drug payload curcumin nanosuspensions stabilized by mPEG-DSPE and SPC: in vitro and in vivo evaluation

“…Figure 5(f) showed that both CUR-NSps and injections group had obvious drug distribution in brain, which demonstrated that both CUR-NSps and injections group could pass through the blood brain barrier (BBB) into brain tissue. But CUR-NSps demonstrated a higher CUR concentration in brain at all time-points, which might be the result of transport of the CUR-NSps through the blood-brain barrier by endocytosis and sustained diffusion release of CUR from nanosuspensions (Minagawa et al, 1996;Tsai et al, 2011;Chen et al, 2016).…”