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

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Pharmacology

Indication

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

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Maintenance of	Eye lubrication		••• •••			•••••••• • •••••
Treatment of	Eye discomfort		••• •••			•••••••• • •••••

Contraindications & Blackbox Warnings

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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

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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

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Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">: 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

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Active Moieties

Name	Kind	UNII	CAS	InChI Key
Sorbitan	unknown	AV0YTZ4E6J	12441-09-7	JNYAEWCLZODPBN-JGWLITMVSA-N

International/Other Brands

Tween-80

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
IV Solution Stabilizer	Solution	6.5 mg/1mL	Intravenous	AstraZeneca Pharmaceuticals LP	2018-10-24	2024-02-29
IV Stabilizer	Solution	6.5 mg/1mL	Intravenous	Innate Pharma, Inc.	2020-05-15	Not applicable

Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Avitears	Solution / drops	10 mg/1mL	Topical	Pinnacle Science, LLc	2009-07-17	Not applicable
Polysorbate	Solution	0.8 %	Ophthalmic	Pharma Stulln Inc.	1994-12-31	Not applicable
Viva	Solution / drops	100 mg/10mL	Ophthalmic	Dakota Laboratories, Llc	1987-02-19	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Arepanrix H5n1	Polysorbate 80 (4.86 mg / 0.5 mL) + DL-alpha-Tocopherol (11.86 mg / 0.5 mL) + Influenza A virus A/Vietnam/1194/2004 (H5N1) antigen (formaldehyde inactivated) (3.75 mcg / 0.5 mL) + Squalene (10.69 mg / 0.5 mL)	Emulsion	Intramuscular	ID Biomedical Corporation of Quebec	Not applicable	Not applicable
Clear Eyes Complete 7 Symptom Relief	Polysorbate 80 (1.25 mL/1mL) + Hypromellose (.5 mL/1mL) + Naphazoline hydrochloride (.0625 mL/1mL) + Zinc sulfate, unspecified form (.625 mL/1mL)	Liquid	Ophthalmic	Prestige Brands Holdings, Inc.	2010-03-01	Not applicable
Clear Eyes Complete 7 Sympton Relief	Polysorbate 80 (1.25 mg/1mL) + Hypromellose (.5 mg/1mL) + Naphazoline hydrochloride (.0625 mg/1mL) + Zinc sulfate (.625 mg/1mL)	Liquid	Ophthalmic	Prestige Brands Holdings, Inc.	2013-06-12	Not applicable
ENDURA LUBRICANT EYE DROPS	Polysorbate 80 (4 MG/0.4ML) + Glycerin (4 MG/0.4ML)	Liquid	Ophthalmic	บริษัท แอลเลอร์แกน (ประเทศไทย) จำกัด	2012-05-13	Not applicable
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 / drops	Ophthalmic	Hi-Healthcare Inc	2020-05-22	Not applicable

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

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]
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]
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]
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]
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]
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]
Polysorbate 80 [Link]
Code of Federal Regulation [Link]
Common Ingredients in U.S. Licensed Vaccines [Link]
NTP Toxicology and Carcinogenesis Studies of Polysorbate 80 (CAS No. 9005-65-6) in F344/N Rats and B6C3F1 Mice (Feed Studies). [Link]
Polysorbate 80 and Helicobacter pylori: a microbiological and ultrastructural study [Link]
Food Emulsifier Polysorbate 80 Increases Intestinal Absorption of Di-(2-Ethylhexyl) Phthalate in Rats [Link]
Polysorbates, peroxides, protein aggregation, and immuno- genicity – a growing concern. [Link]
In uence of excipients on drug absorption via modulation of intestinal transporters activity [Link]
Polysorbate 80 [Link]
Overview of pharmaceutical excipients used in tablets and capsules [Link]
Effect of Polysorbate 80 Quality on Photostability of a Monoclonal Antibody [Link]
Evaluation reports of Polysorbates [Link]
DailyMed: Aviteras (Polysorbate 80.1%) drops [Link]

External Links

PubChem Substance: 347911102
RxNav: 8560
Wikipedia: Polysorbate_80

MSDS

Download (47.9 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Dry Eye Syndrome (DES)	1
4	Completed	Treatment	Dry Eyes	1
4	Completed	Treatment	Obstructive Sleep Apnea (OSA) / Psoriasis	1
3	Completed	Diagnostic	Hemophilia A	1
3	Completed	Prevention	Vaccines, Pneumococcal	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Emulsion	Intramuscular
Solution / drops	Topical	10 mg/1mL
Liquid	Ophthalmic
Gel	Topical
Suspension	Conjunctival; Ophthalmic
Injection, suspension	Intramuscular
Solution	Intravenous	6.5 mg/1mL
Ointment	Ophthalmic; Topical
Solution	Ophthalmic	0.8 %
Solution	Ophthalmic
Emulsion	Ophthalmic
Solution / drops	Ophthalmic
Solution / drops	Ophthalmic	100 mg/10mL

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US8932610	No	2015-01-13	2030-03-24

Properties

State

Liquid

Experimental Properties

Property	Value	Source
melting point (°C)	-20.556	MSDS
boiling point (°C)	100	MSDS
water solubility	Easily soluble in cold water, hot water	MSDS

Predicted Properties

Not Available

Predicted ADMET Features

Not Available

Spectra

Mass Spec (NIST): Not Available
Spectra: Not Available
Chromatographic Properties: Collision Cross Sections (CCS)
Not Available

Drug created at December 03, 2015 16:51 / Updated at February 20, 2024 23:55

Polysorbate 80

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Collision Cross Sections (CCS)