Polysorbate 80 for pharmaceutical applications.
Chemical name:
Polysorbate 80, Polyoxyethylene (20) sorbitan monooleate
CAS number:
9005-65-6
Kolliphor PS 80 is an amber liquid with a faint characteristic odor.
Kolliphor PS 80 is used as a non-ionic surfactant and oil-in-water emulsifier, as plasticizer in a range of solid dispersions and oral dosage forms.
Kolliphor PS 80 is a non-ionic, hydrophilic emulsifier with broad pH range applicability and good skin tolerance in topical formulations.
Kolliphor PS 80 (Polyoxyethylene(20)sorbitanmonooleate) is a cGMP Pharmaceutical Grade Excipient that is a non-ionic, hydrophilic emulsifier, co-emulsifier and solubilizer.
With a broad pH range, Kolliphor PS 80 is suitable for lotions and creams, gels and foams.
Benefits of Kolliphor PS 80:
-Kolliphor PS 80 is suitable for oral, semi solid and liquid dosage forms as well as softgels
-Plasticizer in a range of solid dispersions and oral dosage forms
-Broad pH range applicability and good skin tolerance in topical formulations
-Solubilizing agent in a variety of pharmaceutical formulations
Features of Kolliphor PS 80:
-Nonionic hydrophilic solubilizer and co-emulsifier
-Well suited for SEDDS, SMEDDS, SNEEDS
-Non-ionic oil-in-water emulsifier and solubilizer
Kolliphor PS 80 is a nonionic surfactant and emulsifier often used in pharmaceuticals, foods, and cosmetics.
Kolliphor PS 80 is a viscous, water-soluble yellow liquid.
Chemistry of Kolliphor PS 80:
Polysorbate 80 is derived from polyethoxylated sorbitan and oleic acid.
The hydrophilic groups in this compound are polyethers also known as polyoxyethylene groups, which are polymers of ethylene oxide.
In the nomenclature of polysorbates, the numeric designation following polysorbate refers to the lipophilic group, in this case, the oleic acid.
The full chemical names for polysorbate 80 are:
Polyoxyethylene (20) sorbitan monooleate
(x)-sorbitan mono-9-octadecenoate poly(oxy-1,2-ethanediyl)
The critical micelle concentration of polysorbate 80 in pure water is reported as 0.012 mM.
Other names
E number: E433
Brand names:
Kolliphor PS 80
Alkest TW 80
Scattics
Canarcel
Poegasorb 80
Montanox 80 – Montanox is a registered trademark of Seppic
Tween 80 – Tween is a registered trademark of Croda Americas, Inc.
Kotilen-80 - Kotilen is a registered trademark of Kolb AG
Kolliphor PS 80 is a non-ionic, hydrophilic emulsifier with broad pH range applicability and good skin tolerance in topical formulations.
KEYWORDS:
9005-65-6, Polysorbate 80, Polyoxyethylene (20) sorbitan monooleate, Kolliphor PS, Kolliphor PS 80, Montanox 80, Alkest TW 80, Tween 80, PS 80, Kotilen-80
Uses of Kolliphor PS 80:
Food:
Kolliphor PS 80 is used as an emulsifier in foods.
For example, in ice cream, polysorbate is added up to 0.5% (v/v) concentration to make the ice cream smoother and easier to handle, as well as increasing its resistance to melting.
Adding this substance prevents milk proteins from completely coating the fat droplets.
This allows them to join in chains and nets, which hold air in the mixture, and provide a firmer texture that holds its shape as the ice cream melts.
Health and beauty:
Kolliphor PS 80 is also used as a surfactant in soaps and cosmetics (including eyedrops), or a solubilizer, such as in a mouthwash.
The cosmetic grade of Kolliphor PS 80 may have more impurities than the food grade.
Medical:
Kolliphor PS 80 is a surfactant and solubilizer used in a variety of oral and topical pharmaceutical products.
Kolliphor PS 80 is an excipient that is used to stabilize aqueous formulations of medications for parenteral administration, and used as an emulsifier in the making of the antiarrhythmic amiodarone.
Kolliphor PS 80 is also used as an excipient in some European and Canadian influenza vaccines.
Influenza vaccines contain 2.5 μg of polysorbate 80 per dose.
Kolliphor PS 80 is found in many vaccines used in the United States, including the Janssen COVID-19 vaccine.
Kolliphor PS 80 is used in the culture of Mycobacterium tuberculosis in Middlebrook 7H9 broth.
Kolliphor PS 80 is also used as an emulsifier in the estrogen-regulating drug Estrasorb.
Kolliphor PS 80 is also used in granulation for stabilization of drugs and excipients when IPA binding.
Laboratory:
Some mycobacteria contain a type of lipase (enzyme that breaks up lipid molecules); when these species are added to a mixture of Kolliphor PS 80 and phenol red, they cause the solution to change color, so this is used as a test to identify the phenotype of a strain or isolate.
On RODAC agar plates used in microbiological control, Kolliphor PS 80 counteracts disinfectants often found on sampled surfaces, thereby allowing the microbes found on these surfaces to grow.
Applications of Kolliphor PS 80:
Polysorbates are mainly used as solubilizers, emulsifiers, or suspension stabilizers for pharmaceutical applications.
Depending on the HLB value and the miscibility in water of the product, polysorbates either act more as a solubilizer or emulsifier.
Kolliphor PS 80 is more suitable for use as a solubilizer of poorly water soluble drug substances in either liquid or solid oral dosage forms.
This excipient also functions as a suspension stabilizer in addition to a skin penetration enhancer for topical applications.
Polysorbates are non-ionic surfactants and emulsifiers for pharmaceutical application, derived from polyethoxylation of sorbitan fatty acid esters.
Property Kolliphor PS 80 typical values:
Appearance: Colorless or yellow, clear liquid with a faint characteristic odor
Acid value: Max 2.0 mg KOH/g
Hydroxyl value: 65 to 80 mg KOH/g
Peroxide value: Max 5.0 meq O2/kg
Saponification value: 45 to 55 mg KOH/g
Dioxane: Max 1.0 ppm
Ethylene oxide: Max 310 mg/kg
Composition of fatty acids (Ph.Eur.):
Myristic acid (C14) Max 5.0%
Palmitic acid (C16) Max 16.0%
Pamitoleic acid (C16:1) Max 8.0%
Stearic acid (C18) Max 6.0%
Oleic acid (C18:2) Min 58.0%
Linoleic acid (C18:2) Max 18.0%
Linolenic acid (C18:3) Max 4.0%
Water: Max 3.0%
Total ash: Max 0.25%
Selected chemical and physical parameters:
HLB* 15
CMC 35 mg/L
Specific gravity: 1.06 to 1.09 g/cm3
Viscosity: 300 to 500 cSt
Solubility in water: Dispersible in water
Kolliphor PS 80 is an amber liquid with a faint characteristic odor.
Kolliphor PS 80 is used as a non-ionic, hydrophilic emulsifier for pharmaceutical creams and ointments.
-Suitable for use as solubilizer, emulsifier, suspension stabilizer or skin penetration enhancer
-Broad pH range
-Good skin tolerance
-Suitable for oral solid, semi solid and liquid dosage forms as well as softgels
Kolliphor PS 80 is a non-ionic, hydrophilic emulsifier, co-emulsifier and solubilizer for pharmaceutical preparations like emulsions and creams, gels and foams as well as softgels.
Polysorbates are non-ionic surfactants and emulsifiers derived from polyethoxylated sorbitan and stearic or oleic acid.
Polysorbates are mainly used as a solubilizer, emulsifier or suspension stabilizer for pharmaceutical application.
Depending on the HLB value of the product they can either act as solubilzer or emulsifier.
Kolliphor PS 80 is its high HLB value more suitable as a solubilizer of poorly water soluble drug substances in either liquid or solid dosage forms.
Kolliphor PS 80 is suitable for usage in physical mixing, melt granulation, spray drying and hot melt extrusion processes.
Solubilization of Kolliphor PS 80:
Solubilization performance based on model APIs
The formulation of poorly water soluble active pharmaceutical ingredients (APIs) poses a distinct challenge to pharmaceutical formulators.
With newly discovered APIs trending towards an increase in lipophilicity and complexity, drug solubilizers such as Kolliphor PS 80 have become essential for the development of stable and efficacious formulations.
A high-throughput screening robot was used to study the solubilizing performance of Kolliphor PS 80 based on model APIs with different physicochemical profiles.
Kolliphor PS 80 was tested as a drug solubilizer at concentrations of 0, 5, 10, 15, and 20%.
Kolliphor PS 80 demonstrated a significant improvement in the solubility.
Regardless of the physicochemical attributes of the model API, the solubilization of all APIs was concentration dependent.
The solubilization capacity of Kolliphor PS 80 can be attributed to its longer C18:1 chain length which offers greater fluidity, thus allowing for enhanced solubilization performance.
The upper-limit concentration of 20% which exceeds typical usage levels in standard pharmaceutical liquid or solid formulations was established to allow for an assessment of a potential saturation effect.
The selected model APIs differed in molecular weight, estimated logP values, estimated water solubility, and melting point.
The table below shows an overview of these attributes for all selected model compounds.
Drug solubilization via hot melt extrusion (HME):
The solubilizing performance of Kolliphor PS 80 for the API ritonavir was investigated in formulation obtained by hot melt extrusion (HME) employing Kollidon® VA 64 (copovidone) as a matrix.
The dissolution curves show the effectiveness of Kolliphor PS 80 on dissolution of ritonavir from a Kollidon VA 64-based matrix.
Even at the low concentration of 2.5%, Kolliphor PS 80 had a significant impact on increasing drug availability, demonstrating approximately 80% drug release within the first 30 minutes.
The release was independent of the tested concentrations (i.e., 2.5, 5.0, and 7.5%) of the solubilizers.
Procedure of Kolliphor PS 80:
Step 1: Surfactant solution Dissolve Kolliphor PS 80 in approx. half of the total water amount.
Heat the solution to a temperature of 70 – 80 °C.
Step 2: Emulsification Add Kolliwax GMS II and triethyl citrate while homogenizing with a high-shear mixer.
Keep homogenizing the mixture for 10 min.
Step 3: GMS emulsion Let the mixture cool under stirring while slowly adding the remaining half of the water amount.
Step 4: Spray suspension Slowly add the cold GMS emulsion to the coating dispersion.
Continue stirring to obtain a homogeneous mixture.
Polysorbate 80
Application Examples of Kolliphor PS 80:
Non-ionic solubilizer, emulsifier and co-emulsifier.
Special services associated with the product
Specialized technical assistance:
Application tests in our test laboratories
Necessary documentation for registration with COFEPRIS
Regulatory status :
Kolliphor PS 80 meets the current USP-NF, Ph. Eur., and JP monographs under its compendial name “Polysorbate 80”.
Furthermore, Kolliphor PS 80 meets the requirements of IPEC-PQG GMP for Excipients.
IUPAC name:
Polyoxyethylene (20) sorbitan monooleate
Other names:
Kolliphor PS 80
Montanox 80
Alkest TW 80
Tween 80
PS 80
Kotilen-80
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