Polysorbate 80

Identification

Brand Names
Clear Eyes Complete, Refresh Optive Advanced, Viva-drops Lubricating Eye Drops
Generic Name
Polysorbate 80
DrugBank Accession Number
DB11063
Background

Polysorbate, a substance formulated by the reaction of sorbitan fatty acid ester (a nonionic surfactant) with ethylene oxide, is used in many foreign countries, including the U.S. and the EU, where it acts as an emulsifier, a solubilizer in many foods, including bread, cake mix, salad dressing, shortening oil and chocolate 18.

Polysorbate 80 is a hydrophilic nonionic surfactant. It is utilized as a surfactant in soaps and cosmetics and also as a lubricant in eye drops. In food or pharmaceutical products, it can act as an emulsifier. Polysorbate 80 is an excipient that is used to stabilize aqueous formulations of medications for parenteral administration or vaccinations.15

A solubilizing agent acts as a surfactant and increases the solubility of one agent in another. A substance that would not normally dissolve in a particular solution is able to dissolve with the use of a solubilizing agent.15

It is also known as an emulsifier, which helps ingredients mix together and prevent separation, and water-containing small amounts of salts, and is included in several vaccines licensed in the USA.9

Type
Small Molecule
Groups
Approved
Synonyms
  • polyoxyethylene-sorbitan-20 mono-oleate
  • Polysorbate 80
  • Tween 80

Pharmacology

Indication

It is used as a solubilizer, antimicrobial preservative and disinfectant 16.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Polysorbates are widely used to protect biological drug products from protein unfolding, aggregation, and precipitation during both shipping and handling. The polysorbates are amphipathic, nonionic surfactants made of fatty acid esters of polyoxyethylene sorbitan. Polysorbate 80 is one of the most common surfactants currently used in the formulation of protein-based biopharmaceuticals 6.

Mechanism of action

Polysorbate 80 is one of the primary components of protein formulations. This drug inhibits interfacial damage of the protein molecule that undergoes mechanical stress during shipping and handling. Polysorbate 80 also affects the formulation photostability. Exposure to light of polysorbate 80 aqueous solution results in peroxide generation, which in turn may lead to oxidation of the susceptible amino acid residues in the protein molecule 6.

One study on rats found that Polysorbate 80 increased apical to basolateral membrane permeability of digoxin in Caco-2 cells suggesting that Ps 80 is an in vitro inhibitor of P-glycoprotein. It concluded that PS 80 may influence in vivo absorption of P-gp substrates, and this could be translated to human applications 5.

Absorption

Poorly absorbed 18.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Polysorbates undergo degradation by auto-oxidation, producing reactive peroxides, in addition to hydrolysis 13. Exposure to light of polysorbate 80 aqueous solution leads autoxidation of the alkyl polyoxyethylene chain leading to the production of hydroperoxide derivatives. The peroxides cause oxidative damage to the protein molecule that makes up the formulation. The residual peroxides and the rate of peroxide generation as a result of light exposure are found to vary for polysorbate 80 of different grades/from different sources 6.

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Medicalerrors
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Toxicity

Acute oral toxicity (LD50): 25000 mg/kg in Mouse MSDS

In general, study results of the polysorbates demonstrated no carcinogenicity and genotoxicity. In repeated-dose toxicity studies, diarrhea was observed as the major symptom of toxicity 18. Some studies, however, show conflicting findings.

In a 2-year dietary study of polysorbate 80 in rats, a higher incidence of adrenal medullary pheochromocytomas was found, mainly in male rats 18.

Polysorbate 80 is used as a solubilizing agent in IV infusions of the antiarrhythmic drug amiodarone. Rare case reports of liver toxicity have been published suggesting polysorbate 80 may contribute to liver toxicity with the IV formulation of amiodarone. The package labeling of amiodarone warns that polysorbate 80 is also known to leach DEHP (dioctyl phthalate) from PVC and dosing recommendations must be followed closely 15.

It was found that maternal toxicities such as loose stool, suppression of weight gain and reduced intake were seen, and poor lactation was noted in some studies of mother rats administered 7.5% solutions of polysorbates 18.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
No interactions found.

Products

Products
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Active Moieties
NameKindUNIICASInChI Key
SorbitanunknownAV0YTZ4E6J12441-09-7JNYAEWCLZODPBN-JGWLITMVSA-N
International/Other Brands
Tween-80
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
IV Solution StabilizerSolution6.5 mg/1mLIntravenousAstraZeneca Pharmaceuticals LP2018-10-24Not applicableUS flag
IV StabilizerSolution6.5 mg/1mLIntravenousInnate Pharma, Inc.2020-05-15Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AvitearsSolution / drops10 mg/1mLTopicalPinnacle Science, LLc2009-07-17Not applicableUS flag
PolysorbateSolution0.8 %OphthalmicPharma Stulln Inc.1994-12-31Not applicableCanada flag
VivaSolution / drops100 mg/10mLOphthalmicDakota Laboratories, Llc1987-02-19Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Clear Eyes Complete 7 Symptom ReliefPolysorbate 80 (1.25 mL/1mL) + Hypromellose (.5 mL/1mL) + Naphazoline hydrochloride (.0625 mL/1mL) + Zinc sulfate, unspecified form (.625 mL/1mL)LiquidOphthalmicPrestige Brands Holdings, Inc.2010-03-01Not applicableUS flag
Clear Eyes Complete 7 Sympton ReliefPolysorbate 80 (1.25 mg/1mL) + Hypromellose (.5 mg/1mL) + Naphazoline hydrochloride (.0625 mg/1mL) + Zinc sulfate, unspecified form (.625 mg/1mL)LiquidOphthalmicPrestige Brands Holdings, Inc.2013-06-12Not applicableUS flag
ENDURA LUBRICANT EYE DROPSPolysorbate 80 (4 MG/0.4ML) + Glycerin (4 MG/0.4ML)LiquidOphthalmicบริษัท แอลเลอร์แกน (ประเทศไทย) จำกัด2012-05-13Not applicableThailand flag
Eyellic Eye Drops (Sterile)Polysorbate 80 (0.5 g/100mL) + Hypromellose (0.2 g/100mL) + Naphazoline hydrochloride (0.025 g/100mL) + Zinc sulfate, unspecified form (0.25 g/100mL)Solution / dropsOphthalmicHi-Healthcare Inc2020-05-22Not applicableUS flag
i-Drops ARTIFICIAL TEARSPolysorbate 80 (5 mg/1mL) + Hypromellose (2 mg/1mL) + Naphazoline hydrochloride (0.25 mg/1mL) + Zinc sulfate, unspecified form (2.5 mg/1mL)Solution / dropsOphthalmicGLOBAL PHARMA HEALTHCARE PRIVATE LIMITED2021-04-01Not applicableUS flag
OPTIVE ADVANCE LUBRICANT EYE DROPSPolysorbate 80 (5 mg) + Carboxymethylcellulose sodium (5 mg) + Glycerin (10 mg)LiquidOphthalmicบริษัท แอลเลอร์แกน (ประเทศไทย) จำกัด2016-04-03Not applicableThailand flag
OPTIVE® ADVANCED EMULSION OFTALMICAPolysorbate 80 (5 mg) + Carboxymethylcellulose (5 mg) + Glycerin (10 mg)OintmentOphthalmic; TopicalALLERGAN DE COLOMBIA S.A.2013-12-132018-06-15Colombia flag
Refresh DigitalPolysorbate 80 (5 mg/1mL) + Carboxymethylcellulose sodium (5 mg/1mL) + Glycerin (10 mg/1mL)Solution / dropsOphthalmicAllergan, Inc.2020-08-01Not applicableUS flag
Refresh Digital PFPolysorbate 80 (5 mg/1mL) + Carboxymethylcellulose sodium (5 mg/1mL) + Glycerin (10 mg/1mL)Solution / dropsOphthalmicAllergan, Inc.2020-08-01Not applicableUS flag
REFRESH OPTIVE AdvancedPolysorbate 80 (5 mg/1mL) + Carboxymethylcellulose sodium (5 mg/1mL) + Glycerin (10 mg/1mL)Solution / dropsOphthalmicAllergan, Inc.2011-11-30Not applicableUS flag

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
6OZP39ZG8H
CAS number
9005-65-6
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Coors EA, Seybold H, Merk HF, Mahler V: Polysorbate 80 in medical products and nonimmunologic anaphylactoid reactions. Ann Allergy Asthma Immunol. 2005 Dec;95(6):593-9. doi: 10.1016/S1081-1206(10)61024-1. [Article]
  2. Sun W, Xie C, Wang H, Hu Y: Specific role of polysorbate 80 coating on the targeting of nanoparticles to the brain. Biomaterials. 2004 Jul;25(15):3065-71. doi: 10.1016/j.biomaterials.2003.09.087. [Article]
  3. Zhao YM, Xia AX, Wei YH, Ruan YP, Li FZ: [Polysorbate-80 modified neurotoxin nanoparticle with its transport and cytotoxicity against blood-brain barrier]. Yao Xue Xue Bao. 2010 Oct;45(10):1312-6. [Article]
  4. van Tellingen O, Beijnen JH, Verweij J, Scherrenburg EJ, Nooijen WJ, Sparreboom A: Rapid esterase-sensitive breakdown of polysorbate 80 and its impact on the plasma pharmacokinetics of docetaxel and metabolites in mice. Clin Cancer Res. 1999 Oct;5(10):2918-24. [Article]
  5. Zhang H, Yao M, Morrison RA, Chong S: Commonly used surfactant, Tween 80, improves absorption of P-glycoprotein substrate, digoxin, in rats. Arch Pharm Res. 2003 Sep;26(9):768-72. [Article]
  6. Wang CX, Huang LS, Hou LB, Jiang L, Yan ZT, Wang YL, Chen ZL: Antitumor effects of polysorbate-80 coated gemcitabine polybutylcyanoacrylate nanoparticles in vitro and its pharmacodynamics in vivo on C6 glioma cells of a brain tumor model. Brain Res. 2009 Mar 19;1261:91-9. doi: 10.1016/j.brainres.2009.01.011. Epub 2009 Jan 20. [Article]
  7. Polysorbate 80 [Link]
  8. Code of Federal Regulation [Link]
  9. Common Ingredients in U.S. Licensed Vaccines [Link]
  10. NTP Toxicology and Carcinogenesis Studies of Polysorbate 80 (CAS No. 9005-65-6) in F344/N Rats and B6C3F1 Mice (Feed Studies). [Link]
  11. Polysorbate 80 and Helicobacter pylori: a microbiological and ultrastructural study [Link]
  12. Food Emulsifier Polysorbate 80 Increases Intestinal Absorption of Di-(2-Ethylhexyl) Phthalate in Rats [Link]
  13. Polysorbates, peroxides, protein aggregation, and immuno- genicity – a growing concern. [Link]
  14. In uence of excipients on drug absorption via modulation of intestinal transporters activity [Link]
  15. Polysorbate 80 [Link]
  16. Overview of pharmaceutical excipients used in tablets and capsules [Link]
  17. Effect of Polysorbate 80 Quality on Photostability of a Monoclonal Antibody [Link]
  18. Evaluation reports of Polysorbates [Link]
  19. DailyMed: Aviteras (Polysorbate 80.1%) drops [Link]
PubChem Substance
347911102
RxNav
8560
Wikipedia
Polysorbate_80
MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentDry Eye Syndrome (DES)1
4CompletedTreatmentObstructive Sleep Apnea (OSA) / Psoriasis1
3CompletedDiagnosticHemophilia As1
3CompletedPreventionVaccines, Pneumococcal1
3TerminatedTreatmentNon-muscle Invasive Bladder Cancer (NMIBC)1
2CompletedTreatmentType 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableDry Eye Syndrome (DES)2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Solution / dropsTopical10 mg/1mL
LiquidOphthalmic
GelTopical
SuspensionConjunctival; Ophthalmic
SolutionIntravenous6.5 mg/1mL
OintmentOphthalmic; Topical
SolutionOphthalmic0.8 %
SolutionOphthalmic
EmulsionOphthalmic
Solution / dropsOphthalmic
Solution / dropsOphthalmic100 mg/10mL
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8932610No2015-01-132030-03-24US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)-20.556MSDS
boiling point (°C)100MSDS
water solubilityEasily soluble in cold water, hot waterMSDS
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Drug created on December 03, 2015 16:51 / Updated on July 29, 2021 06:27