Advertisement

Topics

Cocrystals of quercetin with improved solubility and oral bioavailability.

Summary of "Cocrystals of quercetin with improved solubility and oral bioavailability."

Flavonoids have been studied extensively due to the observation that diets rich in these compounds are associated with lower incidences of many diseases. One of the most studied flavonoids, quercetin, is also the most abundant of these compounds in the plant kingdom. Numerous therapeutic bioactivities have been identified in vitro. However, its in vivo efficacy in pure form is limited by poor bioavailability, primarily due to its low solubility and consequent low absorption in the gut. Cocrystallization has gained attention recently as a means for improving the physicochemical characteristics of a compound. Here, we synthesized and evaluated four new cocrystals of quercetin (QUE): quercetin:caffeine (QUECAF), quercetin:caffeine:methanol (QUECAF·MeOH), quercetin:isonicotinamide (QUEINM), and quercetin:theobromine dihydrate (QUETBR·2H(2)O). Each of these cocrystals exhibited pharmacokinetic properties that are vastly superior to those of quercetin alone. Cocrystallization was able to overcome the water insolubility of quercetin, with all four cocrystals exhibiting some degree of solubility. The QUECAF and QUECAF·MeOH cocrystals increased the solubility of QUE by 14- and 8-fold when compared to QUE dihydrate. We hypothesized that this improved solubility would translate into enhanced systemic absorption of QUE. This hypothesis was supported in our pharmacokinetic study. The cocrystals outperformed QUE dihydrate with increases in bioavailability up to nearly 10-fold.

Affiliation

Center of Excellence for Aging and Brain Repair, Department of Neurosurgery and Brain Repair, USF Health College of Medicine, ‡Neuroimmunology Laboratory, Silver Child Development Center, Department of Psychiatry and Neurosciences, USF Health College of

Journal Details

This article was published in the following journal.

Name: Molecular pharmaceutics
ISSN: 1543-8392
Pages: 1867-76

Links

DeepDyve research library

PubMed Articles [10209 Associated PubMed Articles listed on BioPortfolio]

Research progress on berberine with a special focus on its oral bioavailability.

The natural product berberine (BBR) has become a potential drug in the treatment of diabetes, hyperlipidemia, and cancer. However, the oral delivery of BBR is challenged by its poor bioavailability. I...

Lipid-based nanocarrier for quercetin delivery: System characterization and molecular interactions studies.

The flavonoid quercetin is a naturally occurring compound with several biological activities. However, the oral bioavailability of this compound is very low due to the high pre-systemic metabolism in ...

Quercetin does not alter the oral bioavailability of Atorvastatin in rats.

The study was undertaken to evaluate the effect of Quercetin on the pharmacokinetics of Atorvastatin Calcium. In-vivo Pharmacokinetic studies were performed on rats in a single dose study and multiple...

Cocrystal transition points: Role of cocrystal solubility, drug solubility, and solubilizing agents.

In this manuscript we bring together concepts that are relevant to the solubilization and thermodynamic stability of cocrystals in the presence of drug solubilizing agents. Simple equations are derive...

Nanosuspensions Containing Oridonin/HP-β-Cyclodextrin Inclusion Complexes for Oral Bioavailability Enhancement via Improved Dissolution and Permeability.

Chemotherapy via oral route of anticancer drugs offers much convenience and compliance to patients. However, oral chemotherapy has been challenged by limited absorption due to poor drug solubility and...

Clinical Trials [3602 Associated Clinical Trials listed on BioPortfolio]

Q-Trial in Patients With Hepatitis C

The goal of this study is to translate laboratory findings that Quercetin, a bioflavonoid, is safe and has antiviral activity in people with hepatitis C.

The Effect of Quercetin in Sarcoidosis

The exact cause of the chronic lung disease sarcoidosis is still unknown. Consequently, a complete efficacious treatment is still not available. Earlier studies indicate an important key r...

Sulindac and Plant Compounds in Preventing Colon Cancer

RATIONALE: Chemoprevention therapy is the use of certain drugs to try to prevent the development or recurrence of cancer. The use of sulindac may be an effective way to prevent colon cance...

Phase-I Study Evaluating the Pharmacokinetic Profile of RhuDex®

The drug that is under investigation during this study is RhuDex® and is expected to be used as an oral treatment for rheumatoid arthritis. Normal stomach juices contain acid and previous...

Pharmacokinetic Study to Investigate the Bioavailability and Tolerability of 3 Oral Formulations of Sodium Thiosulfate

Chronic treatment and prophylaxis of vessel and soft tissue calcification as well as of renal calculi could be a future indication for sodium thiosulfate (STS). Using an oral formulation m...

Medical and Biotech [MESH] Definitions

A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.

A branch of dentistry dealing with diseases of the oral and paraoral structures and the oral management of systemic diseases. (Hall, What is Oral Medicine, Anyway? Clinical Update: National Naval Dental Center, March 1991, p7-8)

The practice of personal hygiene of the mouth. It includes the maintenance of oral cleanliness, tissue tone, and general preservation of oral health.

A plant genus of the family ROSACEAE. Members contain esculetin and QUERCETIN.

A plant genus of the family MYRTACEAE that bears an edible fruit and contains guavin B and quercetin glycosides.

Quick Search
Advertisement
 


DeepDyve research library

Relevant Topics

Alzheimer's Disease
Of all the types of Dementia, Alzheimer's disease is the most common, affecting around 465,000 people in the UK. Neurons in the brain die, becuase  'plaques' and 'tangles' (mis-folded proteins) form in the brain. People with Al...

Neurology - Central Nervous System (CNS)
Alzheimer's Disease Anesthesia Anxiety Disorders Autism Bipolar Disorders Dementia Epilepsy Multiple Sclerosis (MS) Neurology Pain Parkinson's Disease Sleep Disorders Neurology is the branch of me...

Nutrition
Within medicine, nutrition (the study of food and the effect of its components on the body) has many different roles. Appropriate nutrition can help prevent certain diseases, or treat others. In critically ill patients, artificial feeding by tubes need t...


Searches Linking to this Article