Curcumin-loaded lipid nanocarrier for improving bioavailability, stability and cytotoxicity against malignant glioma cells

Abstract

Objective: In the present study, Curcumin (CU)-loaded nanocarrier (NC) such as nanoemulsion (NE) was developed with the objective of increasing its cytotoxicity and bioavailability through lymphatic transport by enhancing its solubility and intestinal permeability. Materials and methods: Based on the area obtained in pseudoternary phase diagram, various % combination of Labrafac Lipophile WL 1349, Solutol HS 15, Transcutol HP and distilled water were selected. Formulations which passed physical stability studies were selected for further studies such as globule size, zeta potential, in vitro release, ex vivo permeation, in vitro lipolysis studies, bioavailability studies and cytotoxicity against glioblastoma cells (U-87). Result and discussion: The optimized NC (NE-SB1) had small average globule diameter of 67 ± 6 nm with zeta potential of À37 ± 2.5 mv which indicated long-term dispersion stability. During in vitro lipolysis study, the digestion rate of medium chain triglycerides increased with decreased globule diameter. Statistically significant difference was found in AUC 0Àinf of NC formulation (p50.05) compared to CU suspension. The relative bioavailability of NC was found 11.88 ± 0.47 with respect to CU suspension. During cytotoxicity studies, IC 50 of CU solution on U87 cells was found 24.23 mM, while for the NE-SB1 it was 16.41 mM. The optimized formulation was found to be stable during 6 months of accelerated stability. Conclusion:The overall results revealed that the CU-loaded NC is a very effective approach for enhancing the oral absorption of poorly water-soluble drug CU and have great potential for future clinical application.

Intratumoral Concentrations and Effects of Orally Administered Micellar Curcuminoids in Glioblastoma Patients

“…A mean intratumoral tissue concentration of 56 pg/mg represents an intratumoral concentration of approximately 0.15 mmol/l. The published glioma cell culture models reported cytotoxic effects of curcumin beginning at concentrations of at least 10 mmol/l and up to 20 mmol/l, depending on the cell type and formulation (29)(30)(31)(32)(33)(34)(35)(36), which is much higher than 0.15 mmol/l. While the resulting intratumoral concentration might not be sufficient to cause significant short-term antitumor effects, it may be high enough to achieve long-term tumor control.…”

Nanomedicine to overcome radioresistance in glioblastoma stem-like cells and surviving clones

“…Gadolinum represents another class of radiation sensitizers that are also very practical because they can also be easily viewed in vivo through the use of magnetic High cytotoxic effect on T-98G Not yet studied [202] Polymeric nanoparticle formulation of curcumin Decreased growth of multiple brain tumor cell cultures through modulation of cell proliferation, survival, and stem cell phenotype Not yet studied [203] Nanoemulsion of curcumin Improvement of bioavailability and cytotoxicity against malignant glioma cells Not yet studied [200] Dendrosomal curcumin nanoformulation Suppression of U87MG proliferation and downregulation of pluripotency genes via miR-145 activation Not yet studied [201] Endostatin…”

“…Given the possibility of doping the GNP with radionuclides [196], or to use gold as a means to influence dose deposition [197,198], gold nanoparticle functionalization may represent an opportune tool for GBM targeting and therapy that remains to be evaluated. Other strategies for radiosensitization by use of nanomedicines can include vectorization of endostatin [199], curcumin [200][201][202][203], TMZ [204], and action on NF-kB [205].…”

Phytobioactive compound-based nanodelivery systems for the treatment of type 2 diabetes mellitus – current status

“…[132][133][134][135][136] Nanodelivery systems are an alternative approach that can improve the stability of those compounds with improved bioavailability of curcumin. [137][138][139][140][141][142][143][144][145][146][147][148][149][150] Curcumin-loaded PLGA NPs were constructed with a particle size of 281 nm, and these have shown a higher bioavailability through oral delivery in the diabetic rat model, delaying cataracts. 151 The self-nanoemulsifying curcumin delivery system was developed, has a particle size of ~213 nm, and has shown improved protection of diabetic neuropathy through oral delivery systems in male Sprague Dawley rats.…”