Polyethylene-polypropylene glycol

Description

Pluronic^® F-127 is a nonionic detergent widely used to solubilize hydrophobic molecules such as cell-permeable AM esters of Fluo-4, Fluorica-8 calcium indicators, and Di-4-ANEPS, Di-8-ANEPS potentiometric probes and facilitate their loading into cells. We offer Pluronic^® F-127 as a ready-to-use 10% solution in H₂O.

Below is a typical procedure for loading AM esters of ion indicators and other dyes into cells using a 10% solution of Pluronic^® F-127 in water. Cell loading conditions may vary depending on the cell types or compounds loaded.

Chemical Properties

Polyethylene-polypropylene glycol generally occur as white, waxy, free-flowing prilled granules, or as cast solids. They are practically odorless and tasteless. At room temperature, poloxamer 124 occurs as a colorless liquid.

Originator

Polykol ,Upjohn, US ,1958

Uses

Polyethylene-polypropylene glycol is a liquid surfactant polymer.

Uses

Hard and soft surface cleaners, defoamers in coatings and water treatment. Lubricant in metal working, anti-foaming aid and extender for linear and cross-linked polyesters and polyurethanes.

Uses

pyrethroid-based pesticide for use in mosquito control

Production Methods

Poloxamer polymers are prepared by reacting propylene oxide with propylene glycol to form polyoxypropylene glycol. Ethylene oxide is then added to form the block copolymer.

Definition

ChEBI: Poloxamer is an epoxide.

Manufacturing Process

(A) In a 1-liter 3-necked round bottom flask equipped with a mechanical stirrer, reflux condenser, thermometer and propylene oxide feed inlet, there were placed 57 g (0.75 mol) of propylene glycol and 7.5 g of anhydrous sodium hydroxide. The flask was purged with nitrogen to remove air and heated to 120°C with stirring and until the sodium hydroxide was dissolved. Then sufficient propylene oxide was introduced into the mixture as fast as it would react until the product possessed a calculated molecular weight of 2,380. The product was cooled under nitrogen, the NaOH catalyst neutralized with sulfuric acid and the product filtered. The final product was a waterinsoluble polyoxypropylene glycol having an average molecular weight of 1,620 as determined by hydroxyl number or acetylation analytical test procedures.
(B) The foregoing polyoxypropylene glycol having an average 1,620 molecular weight was placed in the same apparatus as described in procedure (A), in the amount of 500 g (0.308 mol), to which there was added 5 g of anhydrous sodium hydroxide. 105 g of ethylene oxide was added at an average temperature of 120°C, using the same technique as employed in (A). The amount of added ethylene oxide corresponded to 17.4% of the total weight of the polyoxypropylene glycol base plus the weight of added ethylene oxide.

brand name

Lutrol F (BASF); Pluracare (BASF); Pluronic (BASF).

Therapeutic Function

Pharmaceutic aid (surfactant)

General Description

Pluronic^? L-81 is a lipoprotein secretion inhibitor.

Pharmaceutical Applications

Polyethylene-polypropylene glycol is nonionic polyoxyethylene–polyoxypropylene copolymers used primarily in pharmaceutical formulations as emulsifying or solubilizing agents.The polyoxyethylene segment is hydrophilic while the polyoxypropylene segment is hydrophobic. All of the Polyethylene-polypropylene glycol is chemically similar in composition, differing only in the relative amounts of propylene and ethylene oxides added during manufacture. Their physical and surface-active properties vary over a wide range and a number of different types are commercially available;
Polyethylene-polypropylene glycol is used as emulsifying agents in intravenous fat emulsions, and as solubilizing and stabilizing agents to maintain the clarity of elixirs and syrups. Polyethylene-polypropylene glycol may also be used as wetting agents; in ointments, suppository bases, and gels; and as tablet binders and coatings.
Poloxamer 188 has also been used as an emulsifying agent for fluorocarbons used as artificial blood substitutes, and in the preparation of solid-dispersion systems. More recently,Polyethylene-polypropylene glycol has found use in drug-delivery systems.
Therapeutically, poloxamer 188 is administered orally as a wetting agent and stool lubricant in the treatment of constipation; it is usually used in combination with a laxative such as danthron. Polyethylene-polypropylene glycol may also be used therapeutically as wetting agents in eye-drop formulations, in the treatment of kidney stones, and as skin-wound cleansers.
Poloxamer 338 and 407 are used in solutions for contact lens care.

Biological Activity

Polyethylene-polypropylene glycol(Poloxamer 188) is a copolymer surfactant. Poloxamer 188 exhibits antithrombotic, anti-inflammatory and cytoprotective activities in various tissue injury models. It can be used to treat sickle cell disease in children and adults. It has also been shown to be protective against ischaemic injury, cardiomyopathy and cerebral haemorrhage.

Safety Profile

When heated to decomposition it emits acrid smoke and irritating fumes.

Safety

Polyethylene-polypropylene glycol is used in a variety of oral, parenteral, and topical pharmaceutical formulations, and are generally regarded as nontoxic and nonirritant materials.Polyethylene-polypropylene glycol is not metabolized in the body.
Animal toxicity studies, with dogs and rabbits, have shown Polyethylene-polypropylene glycol to be nonirritating and nonsensitizing when applied in 5% w/v and 10% w/v concentration to the eyes, gums, and skin.
In a 14-day study of intravenous administration at concentrations up to 0.5 g/kg/day to rabbits, no overt adverse effects were noted. A similar study with dogs also showed no adverse effects at dosage levels up to 0.5 g/kg/day. In a longer-term study, rats fed 3% w/w or 5% w/w of poloxamer in food for up to 2 years did not exhibit any significant symptoms of toxicity. However, rats receiving 7.5% w/w of poloxamer in their diet showed some decrease in growth rate.
No hemolysis of human blood cells was observed over 18 hours at 25°C, with 0.001–10% w/v poloxamer solutions.
(mouse, IV): 1 g/kg
(mouse, oral): 15 g/kg
(mouse, SC): 5.5 g/kg
(rat, IV): 7.5 g/kg
(rat, oral): 9.4 g/kg

storage

Polyethylene-polypropylene glycol is stable materials. Aqueous solutions are stable in the presence of acids, alkalis, and metal ions. However, aqueous solutions support mold growth.
The bulk material should be stored in a well-closed container in a cool, dry place.

Incompatibilities

Depending on the relative concentrations, poloxamer 188 is incompatible with phenols and parabens.

Toxics Screening Level

The ITSL for solvent black has been changed from 0.04 μg/m3 to 0.1 μg/m3 based on annual averaging time.

Regulatory Status

Included in the FDA Inactive Ingredients Database (IV injections; inhalations, ophthalmic preparations; oral powders, solutions, suspensions, and syrups; topical preparations). Included in nonparenteral medicines licensed in the UK. Included in the Canadian List of Acceptable Non-medicinal Ingredients.