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POLYSORBATE 80

Polysorbate 80 is a substance that has been studied in various clinical trials for different medical applications. Based on available clinical trial data, Polysorbate 80 has been primarily investigated for its role in drug absorption and transportation in the body, as well as a component in artificial tear formulations for treating dry eye syndrome. Research focuses on how this compound interacts with various medications and its effectiveness as part of eye drop solutions. These studies help scientists better understand how Polysorbate 80 affects the way drugs move through the body and how it can help relieve symptoms for people with dry eyes.

Table of Contents

What is Polysorbate 80?

Polysorbate 80 is a pharmaceutical compound used in various medical applications. It’s a nonionic surfactant and emulsifier commonly used in medications and medical products. Based on the clinical trial data, this substance plays important roles in multiple therapeutic areas, from eye treatments to improving drug absorption in the body [1].

Medical Applications

Polysorbate 80 has several medical applications that have been studied in clinical trials. The primary uses include:

  • Artificial tear formulations for treating dry eye syndrome
  • Drug absorption modulator affecting how certain medications are processed in the body
  • Virus inactivation agent in blood products such as coagulation factor concentrates

These diverse applications demonstrate the versatility of polysorbate 80 in medical treatments [2] [3].

Treatment of Dry Eye Syndrome

Dry eye syndrome (a condition where tears don’t provide adequate lubrication for the eyes) is one of the primary conditions treated with polysorbate 80-containing products. Clinical trials have evaluated artificial tears containing polysorbate 80, often in combination with other ingredients like glycerin and carboxymethylcellulose sodium [2].

These formulations work to relieve dry eye symptoms by:

  • Lubricating the eye surface
  • Stabilizing the tear film
  • Reducing dryness sensations

In one clinical trial, researchers measured improvement in patients using a standardized scale called the Subjective Evaluation of Symptom of Dryness (SESoD). This 5-point scale measures dryness from 0 (no dryness) to 4 (severe dryness). The goal of treatment was to decrease this score, indicating an improvement in symptoms [2].

Additional measures used to evaluate the effectiveness of these artificial tears included:

  • Ocular Surface Disease Index (OSDI) – a survey documenting dry eye symptoms on a scale of 0-100
  • Tear Break-up Time (TBUT) – measuring how quickly dry spots appear on the eye after blinking
  • Corneal and conjunctival staining – assessing damage to the eye surface using special dyes

These objective measurements help determine how well polysorbate 80-containing artificial tears address both the symptoms and underlying issues of dry eye syndrome [3].

Role in Drug Absorption

One of the more specialized uses of polysorbate 80 is its ability to influence how drugs are absorbed and processed in the body. Clinical research has investigated how polysorbate 80 affects the absorption of various medications, particularly those that rely on specific transport systems in the intestine [1].

In one clinical trial, researchers hypothesized that polysorbate 80 inhibits uptake transporters in the intestine, specifically those that absorb:

  • Valacyclovir – an antiviral medication absorbed via the peptide transporter 1 (PepT1)
  • Chenodeoxycholic acid – a bile acid absorbed via the apical sodium-bile acid transporter (ASBT)
  • Enalaprilat – a blood pressure medication that serves as a reference for passive absorption

The study measured how polysorbate 80 affected the pharmacokinetics (how drugs move through the body) of these medications, looking at factors such as:

  • Area-Under-the-Curve (AUC) – representing the total drug exposure over time
  • Peak Plasma Concentration (Cmax) – the highest concentration of drug in the bloodstream

Understanding these interactions is important because they can affect how well medications work in patients who may be taking multiple drugs simultaneously [1].

Virus Inactivation in Blood Products

Another critical medical application of polysorbate 80 is in the production of safer blood products, particularly for patients with bleeding disorders. In a clinical trial investigating a product called IMMUNATE S/D (a human plasma-derived coagulation factor VIII concentrate), polysorbate 80 was used as part of the virus inactivation process [4].

For patients with hemophilia A (a genetic disorder causing reduced blood clotting ability), plasma-derived clotting factors are essential treatments. However, these blood products must undergo rigorous purification to eliminate the risk of viral transmission.

The treatment with polysorbate 80, combined with vapor heat treatment, helps inactivate potential viruses in these products, making them safer for patients. This is particularly important for hemophilia patients who require regular infusions of clotting factors throughout their lives [4].

Dosage and Administration

The dosage and administration of polysorbate 80 vary depending on its medical application:

  • For dry eye treatments: Artificial tears containing polysorbate 80 are typically administered as 1-2 drops in each eye, as needed, but at least twice daily. Some clinical trials specified three times per day dosing [2] [3].
  • For drug absorption studies: A dosage of 400mg twice a day was used in clinical research [1].
  • For blood products: Polysorbate 80 is used in the manufacturing process rather than administered directly to patients [4].

The exact formulations and concentrations of polysorbate 80 in each product may vary depending on its intended use and the other ingredients it’s combined with.

Safety and Tolerability

Clinical trials have evaluated the safety and tolerability of polysorbate 80-containing products, particularly for ophthalmologic applications. Researchers assessed safety through:

  • Tolerability questionnaires – measuring patient comfort and acceptance
  • Biomicroscopy – examining the eye with a special microscope to detect any changes
  • Visual acuity testing – ensuring the product doesn’t negatively affect vision
  • Monitoring for adverse events – tracking any negative reactions or side effects

These assessments help determine whether products containing polysorbate 80 are well-tolerated by patients during short-term and long-term use [3].

For its use in drug absorption studies, safety monitoring included tracking how polysorbate 80 might affect the body’s handling of other substances, including endogenous (naturally occurring) bile acids [1].

In blood products, the safety of polysorbate 80 treatment was assessed by monitoring for inhibitor development (an immune response against the treatment) and evaluating the overall clinical safety profile of the product [4].

Aspect Details
Main Applications 1. Component in artificial tear formulations for dry eye syndrome
2. Agent affecting drug absorption and transportation
3. Virus inactivation in blood clotting factor products
Dry Eye Treatments • Used in combination with glycerin and carboxymethylcellulose sodium
• Multiple formulations tested for safety, efficacy, and tolerability
• Effectiveness measured by symptom improvement, tear break-up time, and eye surface staining
Drug Absorption Effects • Hypothesized to inhibit uptake transporters in the intestine
• Affects absorption of drugs like valacyclovir and chenodeoxycholic acid
• Studied at dosage of 400mg twice daily in drug interaction trials
Study Measurements • Pharmacokinetic parameters (AUC, Cmax)
• Subjective symptom scores (for dry eye)
• Clinical evaluations (TBUT, corneal and conjunctival staining)
• Tolerability questionnaires
Other Applications • Used in virus inactivation process for hemophilia A treatment (IMMUNATE S/D)
• Combined with vapor heat treatment for virus inactivation in blood products
Clinical Trial Design • Comparative studies with placebo or existing treatments
• Multiple arm studies with crossover designs
• Measurement of both objective and subjective outcomes

FAQ

  • What is Polysorbate 80 and how is it used in medicine? Polysorbate 80 is a synthetic compound that acts as an emulsifier and surfactant (helps mix substances that normally don't combine well). In medicine, it's used in various ways, including as a component in artificial tear formulations for dry eye syndrome and as an agent that can affect how drugs are absorbed and transported in the body. Clinical trials have studied it both as part of eye drop solutions and for its impact on drug absorption in the digestive system.
  • How does Polysorbate 80 work in artificial tears? In artificial tears, Polysorbate 80 functions as a surfactant that helps stabilize the tear film on the surface of the eye. It's often combined with other ingredients like glycerin and carboxymethylcellulose sodium to create formulations that relieve dry eye symptoms. These artificial tears help to lubricate the eye surface, reduce dryness, and improve overall eye comfort. Clinical trials have tested different formulations containing Polysorbate 80 to assess their effectiveness in treating dry eye syndrome.
  • What does research show about Polysorbate 80's effect on drug absorption? Research indicates that Polysorbate 80 may inhibit certain uptake transporters in the intestine, which affects how some drugs are absorbed in the digestive system. In one clinical trial, researchers hypothesized that Polysorbate 80 specifically inhibits transporters that absorb compounds like valacyclovir and chenodeoxycholic acid in the gut. This interaction can potentially change how effectively these medications are absorbed and how they work in the body.
  • Are there any side effects associated with Polysorbate 80 in eye drops? Clinical trials have specifically studied the tolerability and safety of artificial tears containing Polysorbate 80. Researchers evaluated factors like eye discomfort, burning sensation, blurred vision, and other potential issues. While specific side effects weren't explicitly mentioned in the trial summaries, the studies included measures of tolerability using questionnaires and biomicroscopy examinations to check for any adverse effects. The trials were designed to compare different formulations to ensure they're both effective and well-tolerated by patients.
  • In what other medical applications is Polysorbate 80 being studied? Beyond dry eye treatments and drug absorption studies, Polysorbate 80 has also been investigated in the context of blood clotting factor products. In one clinical trial, it was used as part of a virus inactivation process for Human Plasma-Derived Coagulation Factor VIII Concentrate (IMMUNATE S/D), a treatment for hemophilia A. This shows that Polysorbate 80 has applications in pharmaceutical manufacturing processes, particularly in making blood products safer by helping to inactivate potential viruses.

Ongoing Clinical Trials on POLYSORBATE 80

  • Testing HPV Vaccine to Prevent Return of Precancerous Lesions in Patients Treated for High-Grade Abnormal Cell Changes Caused by HPV

    Not yet recruiting

    1 1 1
    Investigated drugs:
    France

  • Study on Immune Responses to Influenza Vaccines in Health Care Workers Using Polysorbate 80, Sodium Citrate, and Citric Acid Anhydrous

    Not recruiting

    1 1 1 1
    Investigated diseases:
    Investigated drugs:
    Finland

Glossary

  • Polysorbate 80: A synthetic compound used as an emulsifier and surfactant in medications and food products. In medical applications, it's used in artificial tears and can affect drug absorption in the body.
  • Surfactant: A substance that reduces the surface tension between two liquids or between a liquid and a solid, helping them mix together when they normally would not.
  • Dry Eye Syndrome: A condition where the eyes don't produce enough tears or the tears evaporate too quickly, causing discomfort, irritation, and sometimes blurred vision.
  • Artificial Tears: Eye drop solutions designed to lubricate dry eyes and supplement natural tear production, often containing ingredients like Polysorbate 80, glycerin, and carboxymethylcellulose sodium.
  • Pharmacokinetics (PK): The study of how drugs move through the body, including how they're absorbed, distributed, metabolized, and excreted.
  • Area-Under-the-Curve (AUC): A measurement used in pharmacokinetics that shows the total exposure to a drug over time. Higher AUC values indicate greater overall exposure to the drug.
  • Peak Plasma Concentration (Cmax): The maximum concentration of a drug in the blood after administration, measured in units of concentration (e.g., ng/ml).
  • Uptake Transporters: Proteins in cell membranes that help move substances (like drugs) from outside the cell to inside, affecting how drugs are absorbed in the body.
  • Bile Salt Export Pump (BSEP): A transport protein in the liver that moves bile salts from liver cells into the bile duct system. Some drugs can affect how this pump works.
  • Ocular Surface Disease Index (OSDI): A 12-question survey used to measure the severity of dry eye symptoms. Scores range from 0-100, with higher scores indicating more severe symptoms.
  • Tear Break-up Time (TBUT): A test that measures how quickly the tear film breaks up on the surface of the eye after blinking. A shorter time indicates poorer tear film stability and dry eye.
  • Corneal Staining: A method to evaluate the health of the cornea (the clear front part of the eye) by applying a dye that highlights damaged areas. Higher staining scores indicate more damage.
  • Conjunctival Staining: Similar to corneal staining, this evaluates the health of the conjunctiva (the clear membrane covering the white of the eye) using dye to highlight damaged areas.
  • Biomicroscopy: Examination of the eye using a special microscope (slit lamp) that allows detailed view of eye structures to detect abnormalities or changes.
  • Hemophilia A: A genetic bleeding disorder caused by deficiency of clotting factor VIII, which can lead to prolonged bleeding after injuries and spontaneous bleeding.
  • Factor VIII: A blood clotting protein that plays a crucial role in the coagulation process. People with hemophilia A have insufficient levels of this protein.
  • Chenodeoxycholic Acid: A bile acid produced by the liver that helps with digestion. In clinical trials, it was used to study how drugs are transported in the body.
  • Valacyclovir: An antiviral medication used to treat infections caused by herpes viruses. It was used in studies to examine how Polysorbate 80 affects drug absorption.
  • Enalaprilat: An active form of the blood pressure medication enalapril. In studies, it was used as a reference drug for passive absorption.

References

  1. https://clinicaltrials.gov/study/NCT04640571
  2. https://clinicaltrials.gov/study/NCT01010282
  3. https://clinicaltrials.gov/study/NCT00932477
  4. https://clinicaltrials.gov/study/NCT00162019