Superior Pharmacokinetic Profile of an Innovative, Next Generation Curcumin Formula
FASEB J. 2022 May;36 Suppl 1. doi: 10.1096/fasebj.2022.36.S1.R5807.
ABSTRACT
INTRODUCTION: Curcumin is the major bioactive component of turmeric or Curcuma longa L., a widely used spice, food colorant, preservative as well as medicinal agent in Indian and Chinese remedies. Numerous studies have demonstrated its potential benefits for heart health, immunity, diabetes, arthritis as well as joint health and mobility. Currently, curcumin-based products in capsules, ointments, tablets, and cosmetics are marketed worldwide. One important drawback of using curcumin is its poor bioavailability and hence the need to use it at high doses to achieve measurable plasma levels and efficacy – this limits both consumer compliance and product formulation. Curcumin’s poor solubility, low absorption from the gut, rapid metabolism and rapid systemic elimination contributes to its poor bioavailability. To help overcome this major limitation of curcumin, we developed a proprietary curcumin formulation (Curcuwin Ultra+) (CU+) to enhance its bioavailability. We hypothesized that the formulation would protect the curcuminoids from degradation at intestinal alkaline pH conditions, and through this mechanism, significantly increase the availability of curcuminoids in blood and at the tissue level.
GOAL: Our goal was to measure the pharmacokinetic profile of CU+ vs. a standard turmeric extract (STE).
METHOD: A randomized, double-blind, crossover study design involving 24 healthy volunteers under fasting conditions was implemented. Subjects received a single dose of 250 mg CU+, 500 mg CU+ and 1900 mg of STE. Blood samples before dosing, and at various time points post dosing up to 24 hours were collected. Total curcuminoids were measured using a validated LC-MS/MS method. Formulations were compared based on Cmax, AUC0-6, AUC0-24, Tmax, t1/2, and relative absorption.
RESULTS: Maximum serum concentration (Cmax) and total systemic exposure (AUC0-6 and AUC0-24) for total curcuminoids were significantly higher (p<0.05) for both doses of CU+ vs. STE. For example, AUC0-6 was 144 and 149 times greater for CU+ at 250 mg and 500 mg respectively compared to 1900 mg of STE. Additionally, CU+ showed 40% faster absorption as measured by Tmax vs. the STE (p<0.05). No adverse events were observed.
CONCLUSIONS: These pharmacokinetic data demonstrates the ability of this curcumin formulation to deliver superior bioavailability vs. STE, and, at doses that are considerably lower than STE and several other commercially available curcumin products. This has important relevance to consumer compliance in terms of lowering curcumin dose and frequency of dosing. Since maximizing bioavailability influences the therapeutic effects of a compound, the next phase of our research program is to determine if this enhanced bioavailability can be translated to an efficacious benefit of CU+.
PMID:35554097 | DOI:10.1096/fasebj.2022.36.S1.R5807