Enhanced systemic bioavailability of curcumin through transmucosal administration of a novel microgranular formulation
Anticancer Res. 2015;35(12):6411–6418. PMID: 26637850
Head and neck cancer is the cancer of the head and neck portion of the body and is developed through a multi-step process of genetic, epigenetic, and metabolic changes resulting from carcinogen exposure. Curcumin is a promising nutraceutical for chemoprevention of head and neck squamous cell carcinoma (HNSCC). However, the bioavailability of the capsular formulations of curcumin is one of the limiting factors for its proper application in the treatment of the same. Various formulations have been developed aiming to improve the systemic bioavailability of the curcumin. The microgranular curcumin is one such formulation devised to improve the curcumin bioavailability.
To determine the bioavailability, efficacy, and safety of microgranular curcumin formulation, with transmucosal absorption property, in cancer subjects and healthy volunteers.
The study was carried out in 8 healthy volunteers and 15 head and neck squamous cell carcinoma patients. The curcumin formulation consists of curcumin C3 Complex™ in the form of small beadlets (microgranules), manufactured by Sabinsa. Following the standard diagnostic incisional biopsy, patients were self-administered C3 Complex™ microgranules (4 g) and were instructed to hold it in the mouth for 10 minutes. Serum was collected at 15 min, 30 min, 1 h, 2 h, and 4 h after administration. The final serum collection occurred between days 21-28 after patients completed a 3-4 week regimen of 4 g twice-daily dosing of curcumin. Serum levels of curcumin were measured by HPLC. The biological activity of curcumin was assessed with Multiplex Immunoassay and immunohistochemistry.
- Higher serum levels of curcumin were observed compared to other trials using capsular formulation
- In cancer patients, a significant decrease in expression of fibroblast growth factor-2 (FGF-2) in post-biopsy samples and decreased serum levels of FGF-2, granulocyte-macrophage colony-stimulating factor (GM-CSF) and interleukin-17 (IL-17) (p<0.05) were observed
Transmucosal administration of microgranular curcumin leads to enhanced curcumin bioavailability, which is associated with significant biological effects.