Comparative bioavailability study of four different Curcumin formulations in 20 Healthy adult human male subjects under fasting conditions.

Phase 4

Completed

• Conditions: Healthy adult human male subjects meeting inclusion and exclusion criteria

• Registration Number: CTRI/2015/07/005993
• Lead Sponsor: Sanat Products Ltd

Brief Summary

BackgroundTurmeric, the source of the polyphenolic active compound curcumin (diferuloylmethane), has been used extensively in traditional medicine since ancient times as a household remedy against various diseases, including hepatic disorders, cough, sinusitis, rheumatism, and biliary disorders. Recently a large number of studies have shown that curcumin (CU) has a surprising array of antioxidant, antitumor, anti-inflammatory, anticancer, and other desirable medicinal properties.

There is scientific evidence suggesting that CU has a highly pleotropic structure, that physically interacts with a wide range of molecular targets, e.g., transcription factors, growth factors and their receptors, cytokines, enzymes, and genes regulating cell proliferation. Curcumin (CU) functions as an anti-cancer agent by activating apoptosis signaling and inhibiting cell proliferation. CU has been shown to suppress the expression of epidermal growth receptor and estrogen receptors, which are cancer-associated growth factors (Duvoix et al., 2003; Tapal and Tiku, 2012).

However, the main drawback associated with CU is its poor aqueous solubility (11 ng/mL) (Kaminaga et al., 2003), stability in gastrointestinal fluids, low permeability and first pass metabolism which leads to poor bioavailability (~1% in rat) (Pan et al., 1999; Yang et al., 2007). CU is a BCS Class IV (low solubility low permeability) molecule (Wahlang et al., 2011). In order to deliver CU to targeted organs, its hydrophobic property needs to be modified. The small size of carriers is very important for the biodistribution in the body. The capillaries are so small that red blood cells can only travel through them in single file. The capillaries measure approximately 5–10 μm in diameter. Particles larger than this size cannot be circulated in the body and become entrapped in the capillary bed. Thus, the particle diameter should be generally smaller than micrometers for the particles to be circulated in the blood vessels. In addition, reduction in the particle diameter to less than 100 nm is thought to decrease their removal by  thereticuloendothelial system and increase their extravasations from the smallest capillaries. Thus, nanotechnology is one of the effective methods to be used for the delivery of CU.

  Study Rationale:The rational for the present study was to increase the bioavailability of Curcumin for increasing the therapeutic effectiveness against different ailments using Nano particle size of Curcumin in tablet form through oral route as the drug delivery approach.

The study has been designed to augment the in vitro release by improving solubility and permeability using Curcumin Nanoparticles and to enhance the bioavailability of Curcumin by delivering it at the molecular level in the form of nano particles.

Detailed Description

Not available

Study Timeline

• Study Completion: 2015-09-21
• Study Start: 2015-12-08
• Last Update Posted: 2019-11-28

Recruitment & Eligibility

• Status: Completed
• Sex: Male
• Target Recruitment: 20

Inclusion Criteria

• i.Subject who are able and ready to provide written informed consent.
• ii.Subjects must be healthy male human beings within 18-45 years of age (both inclusive).
• iii.Subjects should be having Body Mass Index (BMI) in the range 18.5-30 kg/m2, weighing at least 50 kg.
• iv.Subjects must be of normal health as determined by medical history, physical examination, ECG and laboratory tests performed within 21 days prior to the commencement of the study.
• v.Subjects whose screening laboratory values are within normal limits or considered by the physician / Principal Investigator to be of no clinical significance.

Exclusion Criteria

• i.Subjects incapable of understanding the informed consent process or not ready to sign informed consent.
• ii.Subjects with significant history of hypersensitivity to Curcumin or any ingredients of the formulation or any related products as well as severe hypersensitivity reactions (like angioedema) to any drugs.
• iii.Subject with of presence or history of significant gastrointestinal, liver or kidney disease, or any conditions known to interfere with the absorption, distribution, metabolism or excretion of drugs or known to potentiate or predispose to undesired effects.
• iv.Subjects with active peptic ulceration or a history of peptic ulceration.
• v.Subject with resting hypotension (BP <90 /60) or hypertension (BP > 139 /89).
• vi.Subject with Pulse rate 50/ min.
• and above 99/min.
• vii.Subjects with or prior history of clinically significant, Cardiovascular, pulmonary, hepatic, renal, hematological, gastrointestinal, endocrine, immunologic, dermatologic, musculoskeletal, neurological or psychiatric disease.
• viii.Subjects with a history of MI, Stroke, Peripheral Arterial Disease, GI Bleeding, Hepatic-Impairment, Renal Impairment, Epilepsy and Intracranial hemorrhage.
• ix.Subjects with a history of known food allergy.
• x.Subjects who have suffered any illness or who have been hospitalized within the last 4 weeks preceding the start of the study.

Study & Design

• Study Type: BA/BE
• Study Design: Not specified

Primary Outcome Measures

Name	Time	Method
To assess the bioavailability of single oral formulation of four different Curcumin formulations (containing Curcumin 600mg) of Sanat Products Ltd., India in 20 Healthy adult human male subjects under fasting conditions.	Pre dose (00.00 hour) sample will be collected within 02 hours prior to Investigational Product administration and the post dose samples will be collected at 00.25, 00.50, 00.75, 01.00, 01.25, 01.50, 01.75, 02.00, 02.50, 03.00, 04.00, 06.00, 08.00 and 10.00 hours respectively.

Secondary Outcome Measures

Name	Time	Method
To monitor adverse events and assess safety and tolerability of Curcumin under fasting condition.	Vital signs - sitting blood pressure, radial pulse rate, oral temperature will be assessed at admission, prior to dosing (00.00 hrs) and at 02.00, 06.00 and 12.00 hours post-dose and at the time of checkout (24.00 hrs).

Trial Locations

Locations (1)

Auriga Research Limited,; 🇮🇳 West, DELHI, India

Auriga Research Limited,

🇮🇳West, DELHI, India

Dr Pankaj Bablani

Principal investigator

011-45754546

pankaj.bablani@aurigaresearch.com