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 | "Descrizione" about Mandenol Review Consensus 10 by A_Partyns (12463 pt) | 2023-Oct-26 11:32 |  |
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Mandenol (Ethyl linoleate) is an unsaturated essential fatty acid, ethyl ester of linoleic acid formed by the condensation of ethanol with linoleic acid, obtained by esterification of linoleic acid with ethanol by catalysing sulphuric acid.
The name describes the structure of the molecule:
Raw Materials Used in Production:
Ethyl Linoleate is produced via the esterification of linoleic acid, a common polyunsaturated fatty acid, with ethanol.
Step-by-step Summary of Industrial Production Process.
It occurs as a white grainy powder or as an amber liquid.
What it is used for and where
It is obtained from various plants including Allium sativum, Daphne papyracea, Cryptomeria japonica, Setaria italica and others.
Medical
Ethyl linoleate can be safely used in combination with antibacterial substances to achieve statistically significant wound healing (1). It has also been studied as an effective treatment for acne with mild to moderate features and exerts a positive effect on both inflamed and non-inflamed acne lesions (2). Other studies have also found the anti-inflammatory activity of Ethyl Linoleate to be of potential therapeutic use (3).
Ethyl linoleate is used as an anti-inflammatory in creams, lotions for rough and dry skin and prevents hyperkeratinisation.
Cosmetics
Skin conditioning agent - Emollient. Emollients have the characteristic of enhancing the skin barrier through a source of exogenous lipids that adhere to the skin, improving barrier properties by filling gaps in intercorneocyte clusters to improve hydration while protecting against inflammation. In practice, they have the ability to create a barrier that prevents transepidermal water loss. Emollients are described as degreasing or refreshing additives that improve the lipid content of the upper layers of the skin by preventing degreasing and drying of the skin. The problem with emollients is that many have a strong lipophilic character and are identified as occlusive ingredients; they are oily and fatty materials that remain on the skin surface and reduce transepidermal water loss. In cosmetics, emollients and moisturisers are often considered synonymous with humectants and occlusives.
Perfuming. Unlike fragrance, which can also contain slightly less pleasant or characteristic odours, the term perfume indicates only very pleasant fragrances. Used for perfumes and aromatic raw materials.
Commercial Applications
Cosmetic Industry. Ethyl Linoleate is used in skin care products, particularly for its moisturizing and soothing properties.
Skin Treatments. Known for improving skin texture, reducing the appearance of wrinkles and signs of aging.
Acne Products. Used in acne treatments for its anti-inflammatory properties and ability to help reduce inflammation and redness.
Hair Care Products. Can be included in hair care products to nourish and condition the scalp and hair.
Typical commercial product characteristics Ethyl linoleate
| Appearance | White powder |
| Boiling Point | 388.3±21.0°C at 760 mmHg |
| Flash Point | 96.3±20.4°C |
| Density | 0.9±0.1 g/cm3 |
| PSA | 26.30000 |
| LogP | 8.17 |
| Index of Refraction | 1.465 |
| Vapor Pressure | 0.0±0.9 mmHg at 25°C |
| Safety |  |
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Synonyms:
References______________________________________________________________________
(1) Jelenko C, Wheeler ML, Anderson AP, Callaway BD, McKinley JC. Studies in burns: XIV, Heling in burn wounds treated with Ethyl Linoleate alone or in combination with selected topical antibacterial agents. Ann Surg. 1975 Nov;182(5):562-6. doi: 10.1097/00000658-197511000-00005.
(2) Charakida A, Charakida M, Chu AC. Double-blind, randomized, placebo-controlled study of a lotion containing triethyl citrate and ethyl linoleate in the treatment of acne vulgaris. Br J Dermatol. 2007 Sep;157(3):569-74. doi: 10.1111/j.1365-2133.2007.08083.x.
(3) Park SY, Seetharaman R, Ko MJ, Kim DY, Kim TH, Yoon MK, Kwak JH, Lee SJ, Bae YS, Choi YW. Ethyl linoleate from garlic attenuates lipopolysaccharide-induced pro-inflammatory cytokine production by inducing heme oxygenase-1 in RAW264.7 cells. Int Immunopharmacol. 2014 Apr;19(2):253-61. doi: 10.1016/j.intimp.2014.01.017
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| "Descrizione" about all-rac-alpha-Tocopherol Review Consensus 10 by A_Partyns (12463 pt) | 2023-Oct-20 21:06 | |
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All-rac-alpha-Tocopherol is a synthetic form of vitamin E. It is often used in cosmetic products and skincare for its antioxidant and protective properties.
The name describes the structure of the molecule:
Raw Materials Used in Production.
All-rac-alpha-tocopherol is a synthetic form of vitamin E. The raw materials used for its synthesis include isophorone and trimethylhydroquinone.
Step-by-step Summary of Industrial Production Process.
Form and Color.
All-rac-alpha-tocopherol is generally a viscous, colorless to pale yellow liquid.
Alpha tocopherol is one of the four isomer components that constitute tocopherol: alpha-tocopherol, beta-tocopherol, delta-tocopherol and/or gamma-tocopherol.
Alpha tocopherol occurs naturally in cereals, in oils and, in particular in:
It is a fundamental antioxidant and can be created using a chemical process.
Its antioxidant action has effects on the brain (1), when, in the cardiovascular system, there are problems of diabetes caused by LDL cholesterol (2) and in liver diseases (3)
In the medical field it is an adjuvant to treat vascular diseases, as prevention for cellular diseases and for a correct functioning of the immune system.
No positive action, however, was found towards prostate cancer, as demonstrated by this study of very long duration on many samples (4).
What it is used for and where
Medical
Its antioxidant action has effects on the brain (1), when, in the cardiovascular system, there are problems of diabetes caused by LDL cholesterol (2) and in liver diseases (3)
In the medical field it is an adjuvant to treat vascular diseases, as prevention for cellular diseases and for a correct functioning of the immune system.
No positive action, however, was found towards prostate cancer, as demonstrated by this study of very long duration on many samples (4).
Food
Ingredient included in the list of European food additives as E307, antioxidant.
Cosmetics
Antioxidant agent. Ingredient that counteracts oxidative stress and prevents cell damage. Free radicals, pathological inflammatory processes, reactive nitrogen species and reactive oxygen species are responsible for the ageing process and many diseases caused by oxidation.
Fragrance. It plays a decisive and important role in the formulation of cosmetic products as it provides the possibility of enhancing, masking or adding fragrance to the final product, increasing its marketability. The consumer always expects to find a pleasant or distinctive scent in a cosmetic product.
Skin conditioning agent - Miscellaneous. This ingredient has the task of modifying the condition of the skin when it is damaged or dry by reducing its flakiness and restoring its elasticity.
Skin conditioning agent - Occlusive. This ingredient has the task of modifying the condition of the skin when it is damaged or dry by reducing flaking and restoring elasticity. It has a strong lipophilic character and is identified as an occlusive ingredient; it is generally composed of oily and fatty materials that remain on the skin surface and reduce trans epidermal water loss.
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| "Description" about FD&C RED #40 LAKE Review Consensus 10 by A_Partyns (12463 pt) | 2023-Oct-06 18:50 | |
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FD&C RED #40 or E129 or Allura Red AC is a chemical compound, a dye azo-derivative, water-soluble. (FDA clearance in 1971).
The name describes the structure of the molecule.
Description of raw materials used in production.
Step-by-step summary of industrial production process.
Form and color. FD&C Red No. 40 is a crystalline powder, water-soluble, and ranges in color from red to orange.
Commercial applications.
Food Industry. Widely used to color foods and beverages, providing a distinctive red hue.
Cosmetics and Personal Care Products. Applied in various products like lipsticks and shampoos to provide bright and appealing colors.
Pharmaceuticals. Used to color syrups, tablets, and capsules for easy differentiation and aesthetic reasons.
It has many synonyms, among which the most common is Red 40 or Allura Red AC and, in the list of dyes, CI 16035.
Safety
The US FDA (Food and Drug Administration) has approved the use of Red No. 40 and considers it generally safe when used according to guidelines. However, there are some concerns and studies suggesting it may cause allergic reactions in some people
The problem with azo dyes (monoazo or diazo) is photocatalytic degradation leading to oxidation and the subsequent formation of impurities such as aromatic amines, some of which have carcinogenic activity. (1)
Synonyms:
References________________________________________________________________________
(1) Barros, W. R., Steter, J. R., Lanza, M. R., & Motheo, A. J. (2014). Degradation of amaranth dye in alkaline medium by ultrasonic cavitation coupled with electrochemical oxidation using a boron-doped diamond anode. Electrochimica Acta, 143, 180-187.
Kobun Rovina, Shafiquzzaman Siddiquee and Sharifudin M. Shaarani Extraction, Analytical and Advanced Methods for Detection of Allura Red AC (E129) in Food and Beverages Products Front Microbiol. 2016 May 27;7:798. doi: 10.3389/fmicb.2016.00798.
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| "Descrizione" about FD&C RED #40 Review Consensus 10 by A_Partyns (12463 pt) | 2024-Apr-06 15:35 | |
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FD&C RED #40 or E129 or Allura Red AC is a chemical compound, a dye azo-derivative, water-soluble. (FDA clearance in 1971).
The name describes the structure of the molecule.
Description of raw materials used in production.
Step-by-step summary of industrial production process.
Form and color. FD&C Red No. 40 is a crystalline powder, water-soluble, and ranges in color from red to orange.
Commercial applications.
Food Industry. Widely used to color foods and beverages, providing a distinctive red hue.
Cosmetics and Personal Care Products. Applied in various products like lipsticks and shampoos to provide bright and appealing colors.
Pharmaceuticals. Used to color syrups, tablets, and capsules for easy differentiation and aesthetic reasons.
It has many synonyms, among which the most common is Red 40 or Allura Red AC and, in the list of dyes, CI 16035.
Safety
The US FDA (Food and Drug Administration) has approved the use of Red No. 40 and considers it generally safe when used according to guidelines. However, there are some concerns and studies suggesting it may cause allergic reactions in some people
The problem with azo dyes (monoazo or diazo) is photocatalytic degradation (1) leading to oxidation and the subsequent formation of impurities such as aromatic amines (2), some of which have carcinogenic activity. (1)
Synonyms:
References________________________________________________________________________
(1) Li M, He W, Liu Y, Wu H, Wamer WG, Lo YM, Yin JJ. FD&C Yellow No. 5 (tartrazine) degradation via reactive oxygen species triggered by TiO2 and Au/TiO2 nanoparticles exposed to simulated sunlight. J Agric Food Chem. 2014 Dec 10;62(49):12052-60. doi: 10.1021/jf5045052. Epub 2014 Nov 24. PMID: 25393426.
Abstract. When exposed to light, TiO2 nanoparticles (NPs) become photoactivated and create electron/hole pairs as well as reactive oxygen species (ROS). We examined the ROS production and degradation of a widely used azo dye, FD&C Yellow No. 5 (tartrazine), triggered by photoactivated TiO2 NPs. Degradation was found to follow pseudo-first order reaction kinetics where the rate constant increased with TiO2 NP concentration. Depositing Au on the surface of TiO2 largely enhanced electron transfer and ROS generation, which consequently accelerated dye degradation. Alkaline conditions promoted ROS generation and dye degradation. Results from electron spin resonance spin-trap spectroscopy suggested that at pH 7.4, both hydroxyl radical (•OH) and singlet oxygen ((1)O2) were responsible for dye discoloration, whereas at pH 5, the consumption of (1)O2 became dominant. Implications for dye degradation in foods and other consumer products that contain both TiO2 and FD&C Yellow No. 5 as ingredients are discussed.
(2) Belai N, White SR. Determination of Unsulfonated Aromatic Amines in FD&C Yellow No. 5 and FD&C Yellow No. 6 by Liquid Chromatography-Triple Quadrupole Mass Spectrometry. J AOAC Int. 2019 Mar 1;102(2):580-589. doi: 10.5740/jaoacint.18-0165.
Abstract. Background: This paper describes a simple and sensitive ultra-HPLC-triple quadrupole MS (LC-MS/MS) method for the determination of six unsulfonated aromatic amines in the color additives FD&C Yellow No. 5 (Y5) and FD&C Yellow No. 6 (Y6). The six amines determined by this method are aniline (ANL), benzidine (BNZ), 4-aminobiphenyl (4ABP), 4-aminoazobenzene (4AAB), 2-aminobiphenyl (2ABP), and 4-aminobenzonitrile (4ABN). Objective: This method is intended for use in batch certification of the color additives by the U.S. Food and Drug Administration (FDA) to ensure that each lot meets published specifications for coloring foods, drugs, and cosmetics. Methods: A modified quick, easy, cheap, effective, rugged, and safe (QuEChERS) procedure is used for extraction of the amines. Quantitative determination was performed in electrospray positive ionization and multiple-reaction monitoring modes. Results: Validation of the method demonstrated overall recovery of 101-115% and precision of 1.74-9.78% for all analytes. Excellent regression coefficients were obtained, with values >0.999. Conclusions: The validated method was successfully used for the analyses of 30 Y5 and Y6 samples and provided results that are consistent with results from the current method used by FDA, with greater sensitivity and low matrix effects. Highlights: The validation results demonstrate that the new LC-MS/MS method is applicable for use in routine batch certification.
Kobun Rovina, Shafiquzzaman Siddiquee and Sharifudin M. Shaarani Extraction, Analytical and Advanced Methods for Detection of Allura Red AC (E129) in Food and Beverages Products Front Microbiol. 2016 May 27;7:798. doi: 10.3389/fmicb.2016.00798.
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| "Descrizione" about Butylene Glycol Review Consensus 10 by A_Partyns (12463 pt) | 2023-Jul-28 15:25 | |
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Butylene Glycol (1,3-butanediol o 1,3-Butylene Glycol) is an organic alcohol, an organic chemical of the C4 platform, butanediol glycol. It is a compound of butanediol with two hydroxy groups in positions 1 and 3 derived from a butane hydride.
The name describes the structure of the molecule
Description of raw materials used in production
Synthesis process
It appears as a viscous, odourless liquid with a slightly bitter taste or as a fine white or yellowish powder. Highly soluble in water..
What it is used for and where
Cosmetics
Food
Flavouring agent. Antibacterial agent for cheese, meat, etc.
Medical
Intermediate chemical compound.
Other uses
Typical optimal commercial product characteristics 1,3-Butylene Glycol
| Appearance | Viscous liquid or fine white powder |
| Boiling Point | 207.0±0.0 °C at 760 mmHg |
| Melting Point | -54ºC |
| Flash Point | 121.1±0.0 °C |
| Density | 1.0±0.1 g/cm3 |
| Relative density (20℃/ 20℃, g/cm3) | 1.004-1.007 |
| Purity (%) | ≥99.5 |
| Water content | ≤0.5% |
| PSA | 40.46000 |
| Color APHA | ≤10 |
| Vapour density | 3.1 (20 °C) |
| Vapour Pressure | 0.1±0.8 mmHg at 25°C |
| Index of Refraction | 1.4390-1.4410 |
| Refractive Rate | n20/D1.44 |
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Synonyms:
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| "Descrizione" about Irganox 1040 Review Consensus 9 by A_Partyns (12463 pt) | 2023-Jul-24 10:17 | |
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Irganox 1040 is a chemical compound, a phenolic antioxidant.
The name describes the structure of the molecule:
Irganox is a trademark for a series of antioxidants produced by BASF.
Description of raw materials used in production:
Irganox 1040 is based on pentaerythritol. It's a phenolic antioxidant with the chemical name tetrakis[methylene-3-(3',5'-di-tert-butyl-4'-hydroxyphenyl)propionate]pentaerythritol. The raw materials are pentaerythritol and phenolic derivatives.
The industrial synthesis process takes place in different steps:
What it is for and where
Irganox 1040 is an antioxidant commonly used in the rubber, plastic and polymer industries to protect materials from deterioration caused by oxidation.
It is used in cosmetic facial and body care products as it acts as an antioxidant to prevent the product from degrading when exposed to air and thus oxygen.
This study examined the migration of Irganox 1010 as antioxidant from high density polyethylene and polypropylene (1).
Synonyms:
References___________________________________________________________________
(1) Lickly TD, Bell CD, Lehr KM.The migration of Irganox 1010 antioxidant from high-density polyethylene and polypropylene into a series of potential fatty-food simulants. Food Addit Contam. 1990 Nov-Dec;7(6):805-1
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| "Descrizione" about Pluronic F127 Review Consensus 10 by A_Partyns (12463 pt) | 2023-Jul-18 19:12 | |
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Pluronic™ F127 or Poloxamer 407 is a chemical compound, surfactant non ionic, copolymer consisting of three ethylene oxide blocks and one hydrophobic propylene oxide block, relatively non-toxic to cells at low concentrations.
"Pluronic 127" is a trade name for a specific type of polymer known as poloxamer 407. This name was given by the company that manufactures it, BASF. The term "Pluronic" is a registered trademark of BASF and is used for a range of polyethylene oxide-propylene oxide-polyethylene oxide (PEO-PPO-PEO) block polymers.
The numbering in the name "Pluronic 127" provides information about the structure of the polymer. The number "127" specifically indicates the length and proportion of the polyethylene oxide (PEO) and polypropylene oxide (PPO) blocks in the polymer. In general, the first number (or first two numbers) in a poloxamer's name indicates the length of the PPO block, while the last number multiplied by 10 indicates the weight percentage of PEO in the polymer.
In the case of Pluronic 127 (Poloxamer 407), the polymer has a central PPO block with a length of about 40 repeat units and PEO blocks on both sides with a length of about 70 repeat units each. The weight percentage of PEO in the polymer is 70%.
The name describes the structure of the molecule:
The raw materials for the production of Poloxamer 407 are:
It is obtained by polymerisation of ethylene oxide and propylene oxide in liquid form at a controlled temperature with a catalyst such as potassium hydroxide or sodium hydroxide. The synthesis process consists of the following steps:
It is obtained by polymerisation of ethylene oxide and propylene oxide in liquid form at a controlled temperature with a catalyst such as potassium hydroxide or sodium hydroxide. The synthesis process consists of the following steps:
It comes in the form of fine white powder.
What it is used for and where
Cosmetics
Surfactant - Cleansing agent. Cosmetic products used to cleanse the skin utilise the surface-active action that produces a lowering of the surface tension of the stratum corneum, facilitating the removal of dirt and impurities.
Surfactant - Emulsifying agent. Emulsions are thermodynamically unstable and are used to soothe or soften the skin and emulsify, so they need a specific, stabilising ingredient. This ingredient forms a film, lowers the surface tension and makes two immiscible liquids miscible. A very important factor affecting the stability of the emulsion is the amount of the emulsifying agent. Emulsifiers have the property of reducing the oil/water or water/oil interfacial tension, improving the stability of the emulsion and also directly influencing the stability, sensory properties and surface tension of sunscreens by modulating the filmometric performance.
Cosmetic safety. In cosmetics, Poloxamer 407 is considered safe, however, as with any cosmetic ingredient, some people may be sensitive or have individual allergic reactions, so it is always advisable to test products on the skin before particularly intensive use.
Food
Among a number of natural and synthetic polymers used to form polymeric micelles, Poloxamer 407, a US Food and Drug Administration-approved polymer, is the most attractive due to its biocompatibility, biodegradability, and low toxicity (1).
Poloxamer 407 is used as an emulsifier and stabiliser in creams, sauces, ice cream, fruit drinks where it improves appearance, stability and consistency, promotes solubilisation of lipophilic compounds, improves distribution and bioavailability.
Medical
On polyoxamers, scientific research has identified a potential use, thanks to their low toxicity, solubilising capacity, compatibility with various excipients and biomolecules, as a biomaterial to obtain hydrogels for drug release and in particular Poloxamer 407 is used as a carrier, thanks to its amphiphilic nature, to improve the solubility of poorly water-soluble drugs with particular warning on the solubilisation of active ingredients.
It is used, due to its viscosity and ability to form a protective film on the ocular surface as an ocular lubricant in eye drops that help alleviate dry eye symptoms, improve comfort and as an artificial tear.
Poloxamer 407 is a cleaning agent that can remove plaque and debris from ocular surfaces, contact lenses or medical devices.
It helps protect cells during the freezing and thawing process by acting as a cellular cryopreservative, reducing cell damage and preserving cell viability.
It also has a function as a stabiliser for emulsions, suspensions and colloidal systems improving the stability of pharmaceutical formulations and preventing phase separation and a gelling function with the ability to form reversible gels at room temperature useful in ophthalmology.
It is a non-ionic surfactant that facilitates the emulsification and homogeneous distribution of ingredients in pharmaceutical formulations.
The safety and efficacy of this polymer as a temporary embolic agent were analysed and evaluated positively in this study on temporary vascular occlusion (1).
Poloxamer 407 shows some thermoreversible properties of extreme interest in optimising drug formulation (3).
Poloxamer 407 and vitamin E TPG (D-α-tocopheryl polyethylene glycol succinate) are polymers widely used as drug carriers and excipients to improve drug retention and stability times (4) and oral delivery of antibiofilm peptides (5).
An interesting potential application of Poloxamer 407 concerns 'phacoemulsification' (ultrasound) to protect the corneal endothelium (6).
Safety
Available data show that Poloxamers introduced into the body through different routes than dermal exposure have a rapid clearance from the body, suggesting that they are safe as used (7).
The most relevant studies on this chemical compound have been selected with a summary of their contents:
Optimal typical characteristics of Poloxamer 407 commercial product
| Clarity and color of solution | Clear and colorless |
| Acid | Red solution |
| Average molecular weight | 9480 g/mol-14500 g/mol |
| Ph value (25g/l in water) | 5.0-7.0 |
| Ph value (100g/l in water) | 5.0-7.0 |
| Oxyethylene | 71.5%-74.9% |
| Total ash | <0.4% |
| Residue on ignition | <0.30 |
| Insaturation | 0.031mEq/G-0.65mEq/ |
| Water | <0.75% |
| Heavy metals | <0.002% |
| BHT stabilizer | 50ppm-25ppm |
| Congealing point | 50°C-62°C |
| 1.4 dioxane | <5.0ppm |
| Ethylene oxide | <1.0ppm |
| Propylene oxide | <5.0ppm |
| Arsenic | <2ppm |
Synonyms:
Adeka Pluronic F 108 Antarox Cirrasol ALN-WS Detalan Epan 485 Epan 710 Epan 785 Ethylene oxide-propylene oxide block copolymer dipropylene glycol ether Ethylene oxide-propylene oxide block copolymer ether with ethylene glycol F-108 Lutrol F Pluracare L 61 Poloxalene Poloxalkol Poloxamene Poloxamer 188 Poly(ethylene oxide-co-propylene oxide) Polyoxamer Polyoxyethylene - polyoxypropylene block copolymer Polyoxyethylene - polyoxypropylene copolymer Tergitol XH Therabloat
(1) Saxena V, Hussain MD. Poloxamer 407/TPGS mixed micelles for delivery of gambogic acid to breast and multidrug-resistant cancer. Int J Nanomedicine. 2012;7:713-21. doi: 10.2147/IJN.S28745.
Abstract. Background: Delivery of a high concentration of anticancer drugs specifically to cancer cells remains the biggest challenge for the treatment of multidrug-resistant cancer. Poloxamers and D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) are known inhibitors of P-glycoprotein (P-gp). Mixed micelles prepared from Poloxamer 407 and TPGS may increase the therapeutic efficacy of the drug by delivering high concentrations inside the cells and inhibiting P-gp. Gambogic acid (GA) is a naturally derived novel anticancer agent, but poor solubility and toxic side effects limit its use. In this study, we have developed Poloxamer 407 and TPGS mixed micelle-encapsulating GA for the treatment of breast and multidrug-resistant cancer.... Conclusion: This study suggests that Poloxamer 407/TPGS mixed micelles can be used as a delivery system for GA to treat breast and multidrug-resistant cancer.
(2) Raymond J, Metcalfe A, Salazkin I, Schwarz A. Temporary vascular occlusion with poloxamer 407. Biomaterials. 2004 Aug;25(18):3983-9. doi: 10.1016/j.biomaterials.2003.10.085.
Abstract. There is a need for safe and reversible occlusions during percutaneous endovascular procedures. Poloxamer 407 is a non-ionic surfactant with rapid reversible sol-gel transition behaviour. The safety and efficacy of this polymer as a temporary embolic agent was investigated. First, dissolution time after gelation of poloxamer was determined in an in vitro model. Then, transient poloxamer occlusion of renal and pulmonary arteries of seven dogs was followed by serial angiograms. Macroscopic and pathological changes were studied 1 week later. This experiment was repeated in similar arteries in one pig, and in auricular arteries of two rabbits. Poloxamer dissolution after in vitro polymerization was completed within 1-20 h, depending on concentrations. In vivo poloxamer 22% injections led to complete occlusion, followed by full recanalization within 10-90 min without complication. The only biochemical effect of poloxamer occlusions was transient elevation of triglyceride levels. There were no pathological abnormalities at 1 week. Poloxamer 407 could be used as an embolic material for temporary occlusions.
(3) Dumortier G, Grossiord JL, Agnely F, Chaumeil JC. A review of poloxamer 407 pharmaceutical and pharmacological characteristics. Pharm Res. 2006 Dec;23(12):2709-28. doi: 10.1007/s11095-006-9104-4.
Abstract. Poloxamer 407 copolymer (ethylene oxide and propylene oxide blocks) shows thermoreversible properties, which is of the utmost interest in optimising drug formulation (fluid state at room temperature facilitating administration and gel state above sol-gel transition temperature at body temperature promoting prolonged release of pharmacological agents). Pharmaceutical evaluation consists in determining the rheological behaviour (flow curve or oscillatory studies), sol-gel transition temperature, in vitro drug release using either synthetic or physiological membrane and (bio)adhesion characteristics. Poloxamer 407 formulations led to enhanced solubilisation of poorly water-soluble drugs and prolonged release profile for many galenic applications (e.g., oral, rectal, topical, ophthalmic, nasal and injectable preparations) but did not clearly show any relevant advantages when used alone. Combination with other excipients like Poloxamer 188 or mucoadhesive polymers promotes Poloxamer 407 action by optimising sol-gel transition temperature or increasing bioadhesive properties. Inclusion of liposomes or micro(nano)particles in Poloxamer 407 formulations offers interesting prospects, as well. Besides these promising data, Poloxamer 407 has been held responsible for lipidic profile alteration and possible renal toxicity, which compromises its development for parenteral applications. In addition, new findings have demonstrated immuno-modulation and cytotoxicity-promoting properties of Poloxamer 407 revealing significant pharmacological interest and, hence, human trials are in progress to specify these potential applications.
(4) Butt AM, Mohd Amin MC, Katas H. Synergistic effect of pH-responsive folate-functionalized poloxamer 407-TPGS-mixed micelles on targeted delivery of anticancer drugs. Int J Nanomedicine. 2015 Feb 13;10:1321-34. doi: 10.2147/IJN.S78438.
Abstract. Background: Doxorubicin (DOX), an anthracycline anticancer antibiotic, is used for treating various types of cancers. However, its use is associated with toxicity to normal cells and development of resistance due to overexpression of drug efflux pumps. Poloxamer 407 (P407) and vitamin E TPGS (D-α-tocopheryl polyethylene glycol succinate, TPGS) are widely used polymers as drug delivery carriers and excipients for enhancing the drug retention times and stability. TPGS reduces multidrug resistance, induces apoptosis, and shows selective anticancer activity against tumor cells. Keeping in view the problems, we designed a mixed micelle system encapsulating DOX comprising TPGS for its selective anticancer activity and P407 conjugated with folic acid (FA) for folate-mediated receptor targeting to cancer cells.....Conclusion: FA-P407-TPGS-DOX micelles show potential as a targeted nano-drug delivery system for DOX due to their multiple synergistic factors of selective anticancer activity, inhibition of multidrug resistance, and folate-mediated selective uptake.
(5) Bernegossi J, Calixto GM, Sanches PR, Fontana CR, Cilli EM, Garrido SS, Chorilli M. Peptide KSL-W-Loaded Mucoadhesive Liquid Crystalline Vehicle as an Alternative Treatment for Multispecies Oral Biofilm. Molecules. 2015 Dec 25;21(1):E37. doi: 10.3390/molecules21010037.
Abstract. Decapeptide KSL-W shows antibacterial activities and can be used in the oral cavity, however, it is easily degraded in aqueous solution and eliminated. Therefore, we aimed to develop liquid crystalline systems (F1 and F2) for KSL-W buccal administration to treat multispecies oral biofilms. The systems were prepared with oleic acid, polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol (PPG-5-CETETH-20), and a 1% poloxamer 407 dispersion as the oil phase (OP), surfactant (S), and aqueous phase (AP), respectively. We characterized them using polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheology, and in vitro bioadhesion, and performed in vitro biological analysis. PLM showed isotropy (F1) or anisotropy with lamellar mesophases (F2), confirmed by peak ratio quantification using SAXS. Rheological tests demonstrated that F1 exhibited Newtonian behavior but not F2, which showed a structured AP concentration-dependent system. Bioadhesion studies revealed an AP concentration-dependent increase in the system's bioadhesiveness (F2 = 15.50 ± 1.00 mN·s) to bovine teeth blocks. Antimicrobial testing revealed 100% inhibition of multispecies oral biofilm growth after KSL-W administration, which was incorporated in the F2 aqueous phase at a concentration of 1 mg/mL. Our results suggest that this system could serve as a potential vehicle for buccal administration of antibiofilm peptides.
(6) Galvis V, Tello A, Carreño NI, Berrospi RD, Niño CA. Potential use of thermoreversible hydrogel (poloxamer 407) to protect the corneal endothelium and the posterior capsule during phacoemulsification. J Cataract Refract Surg. 2019 Mar;45(3):389. doi: 10.1016/j.jcrs.2018.10.051.
(7) Singh-Joy SD, McLain VC. Safety assessment of poloxamers 101, 105, 108, 122, 123, 124, 181, 182, 183, 184, 185, 188, 212, 215, 217, 231, 234, 235, 237, 238, 282, 284, 288, 331, 333, 334, 335, 338, 401, 402, 403, and 407, poloxamer 105 benzoate, and poloxamer 182 dibenzoate as used in cosmetics. Int J Toxicol. 2008;27 Suppl 2:93-128. doi: 10.1080/10915810802244595.
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