Rutin: A Comprehensive Overview of Pharmaceutical Applications

Written by Emmanuella Ogbonna, BPharm; Reviewed by Danielle Kelvas, MD, for PTcell for Pharmaceutical Industries LL.C

Rutin, also referred to as vitamin P, is a natural flavonoid found in various plants like buckwheat, as well as foods like apples, citrus fruit, tea, and red wine. (1)

Today, rutin is a major ingredient in several nutraceuticals and is considered one of the major therapeutically active compounds found in nature. (2)

Rutin is well known for its antioxidant effect and is one of the best-known antioxidants in its category. It is also believed to have anti-inflammatory, neuroprotective, and cytoprotective properties. (3)

This article will examine rutin use in the pharmaceutical industry, medicinal uses, chemical composition, and quality control.

Botanical Classification and Characteristics

Rutin is a potent bioflavonoid found in certain fruits, vegetables, and plant flavonoids. (1) It was first isolated from Rutina graveolens, commonly known as rue or herb of grace. However, it is now commonly found in plants like:
● Cassia auriculata (Tanner’s cassia)
● Capparis spinosa (caper bush)
● Fagopyrum esculentum (buckwheat)
● Passiflora incarnata (passion flower)

Fagopyrum esculentum and Capparis spinosa are considered some of the best sources of rutin. (4)

Chemical Composition

The chemical name for rutin is quercetin-3-O-rutinoside. This name is derived from its structure, which consists of the flavonol quercetin bonded to the disaccharide rutinoside. It can also be denoted as (3′,4′,5,7-tetrahydroxy-flavone-3-rutinoside). (5)

Studies show that rutin has demonstrated several pharmacological properties, including antioxidant, anti-viral, antithrombotic, cytoprotective, vasoprotective, neuroprotective, and cardioprotective activities. (6,7)

However, despite its medicinal value, its potential application in the pharmaceutical and cosmetic industry is limited by its low water solubility and poor bioavailability. (1)

Pharmaceutical Uses of Rutin

Rutin’s medicinal properties make it helpful in managing several health conditions.

Some benefits of rutin include:

Support wound healing

Many rutin supplements in the market are promoted to support wound healing due to their antioxidant and anti-inflammatory properties. (1) These properties of rutin have also been found to help heal diabetes wounds. (8)

A study carried out in hyperglycemic rats found that rutin reduces oxidative stress and inflammation, which helps promote wound healing and subsequently reduces the risk of wound ulcers. (9, 10)

Strengthens blood vessels

Rutin supplement is sometimes recommended for treating blood vessel and capillary-related conditions like varicose veins, internal bleeding, or hemorrhoids.
(11) This therapeutic benefit is mainly attributed to rutin’s ability to strengthen blood vessels and prevent blood clots, owing to its high antioxidant and free radical scavenging activity. (3)

Studies have also found that rutin helps reduce the symptoms of venous insufficiency (swelling and puffiness in the legs) due to its effect in decreasing blood viscosity. (12, 13)

Lowers cholesterol

Studies also suggest that rutin can help reduce cholesterol levels. (14) In one study with about 50 participants, researchers found that supplementing with 500 milligrams (mg) of rutin daily for about 3 months significantly decreased total cholesterol, low-density cholesterol (LDL) or “bad” cholesterol, and the ratio to LDL to HDL (“good”) cholesterol. (15)

A study also found that combining rutin and metformin significantly restored blood sugar and lipid levels. (16) Rutin is currently being explored as a natural hypolipidemic agent. (17)

Lowers Blood pressure

Rutin supplements may also help reduce blood pressure. (18) One study found that rutin consumption significantly reduced diastolic and systolic blood pressure in patients with type 2 diabetes. (19)

Quality Control and Standardization of Rutin

The biological and pharmacological activity of rutin can vary depending on the plant’s origin and geographical location.

The major sources of rutin used for medical purposes include buckwheat, Japanese pagoda tree, and Eucalyptus macrorhyncha. (18, 20) Some researchers consider buckwheat to be one of the best dietary sources of rutin. (18)

For quality control and standardization of rutin, recommended analytical techniques include:
● High-performance liquid chromatography (HPLC)
● Thin layer chromatography (TLC)
● Reversed-phase HPLC

Some studies suggest that HPLC using the C18 column is one of the most used methods of standardization. (21)

Regulatory Status and Safety Considerations

There is no general regulatory body for rutin in Europe as it is considered a natural compound commonly found in food sources rather than a medicine. As a result, there is no centralized approval by the European Medicines Agency (EMA). However, the European Food and Safety Authority (EFSA) regulates rutin as a food supplement. (22)

Regarding safety, a dose-toxicity study of rutin revealed that the compound is safe in doses up to 5000 mg/kg daily. (23)

Future Prospects of Rutin Extract

Rutin's poor water solubility and low bioavailability have led researchers to develop different dosage forms to improve this chemical property.

Some dosage forms that have been explored include: (5,21)
● Nanoparticle-Based Formulations
● Liposome hydrogel
● Cyclodextrin Complexation
● Phospholipid Complexes (Phytosomes)

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