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PubMed2000

Relationship between polysorbate 80 solubilization descriptors and octanol-water partition coefficients of drugs.

The molar solubilization capacities (kappa) and the molar micelle-water partition coefficients (K(M)(N)) in Polysorbate 80 of several drugs (including barbiturates, steroids, and benzoic acid derivatives) are related to their log octanol-water partition coefficients (logP). Both kappa and K(M)(N) values were calculated from solubility versus Polysorbate 80 concentration profiles, which were either experimentally determined or obtained from the literature. There is a linear relationship between logP of the tested compounds and the logarithm of the molar micelle-water partition coefficient (logK(M)(N)). On the other hand molar solubilization capacities are nearly independent of logP. It is shown that the ability of Polysorbate 80 to solubilize a drug can be predicted from its logP value.

Octanols↗

PubMed1998

Quantitative determination of polysorbate 20 in nasal pharmaceutical preparations by high-performance liquid chromatography.

A specific reverse-phase HPLC method has been developed for the quantitative determination of polysorbate 20 in various compositions of nasal solutions. This method is based on the acidic hydrolysis of the sorbitan laurate ester followed by the HPLC determination of the free lauric acid. Using this method, polysorbate 20 can effectively be separated and quantitatively determined in matrices containing a wide variety of preservatives, surfactants, and viscosity agents. Sample preparation involves a one-step hydrolysis with sulfuric acid and then a dilution with acetonitrile, prior to injection. The sample is analyzed on a 5-microm octadecylsilane reverse-phase column with a mobile phase of acetonitrile: 0.025 M aqueous di-Sodium hydrogen phosphate, pH = 2.8 (75:25). The column effluent is monitored by UV detection at 210 nm. The validity of the method has been verified with specificity, linearity, recovery, method- and system precisions data. The method is linear for polysorbate 20 from 2.5 to 125 mg ml(-1) range. The limit of detection and limit of quantitation are 0.41 and 0.61 mg ml(-1), respectively.

Administration, Intranasal↗

PubMed1979

Additivity of action between polysorbate 80 and polymyxin B towards spheroplasts of Pseudomonas aeruginosa NCTC 6750.

When polymyxin B and polysorbate 80 were used together against spheroplasts of Pseudomonas aeruginosa, the activities were found to be additive. These substances have previously been reported to act synergistically against P. aeruginosa, but little or no intrinsic activity towards intact cells has been attributed to polysorbate 80. We suggest that in addition to enhancing polymyxin B penetration to the cytoplasmic membrane, polysorbate 80 may also act as an antimicrobial agent when polymyxin-induced damage to the outer membrane facilitates the surfactant's passage through the cell envelope.

Polyethylene Glycols↗

PubMed1986

Polysorbate 20 as a drug release regulator in ethyl cellulose film coatings.

Tablet coatings of hydrophobic ethyl cellulose have been made more hydrophilic by the addition of a non-ionic surfactant, polysorbate (Tween) 20, to the film. As its content increased, so did the release of sodium salicylate from the coated tablets. With a certain content of surfactant and specific thickness of the tablet coat, zero order release kinetics were observed. Leaching of the polysorbate 20 occurred from all formulations. Scanning and transmission electron micrographs showed that the structure of the coats consisted of several layers parallel to the tablet surface. Polysorbate 20 was seen as small drops in some coats.

Cellulose↗

PubMed1989

Solubilization of indomethacin by polysorbate 80 in mixed water-sorbitol solvents.

The effect of indomethacin on the micellar properties of the non-ionic surfactant, polysorbate 80, in water-sorbitol mixtures containing up to 25% w/v sorbitol has been investigated by light scattering, photon correlation spectroscopy and viscometric techniques. The molecular weight of polysorbate 80 micelles containing solubilized indomethacin increased linearly with increase of sorbitol concentration. Solubilization of indomethacin resulted in an increase of micellar weight due not only to the incorporation of solubilizate but also to an increase in the number of polysorbate molecules per micelle. The micelles in all systems were most satisfactorily represented as oblate ellipsoids, the asymmetry and hydration of which increased with increase of sorbitol concentration. Indomethacin solubilization caused a restructuring of the micelle to produce a more symmetrical micelle of increased hydration.

Indomethacin↗

PubMedDate not supplied

The effect of niosomes and polysorbate 80 on the metabolism and excretion of methotrexate in the mouse.

The effect of non-ionic surfactant vesicle (niosome) encapsulation on the metabolism and urinary and faecal excretion of methotrexate (MTX) in mice has been studied following oral and intravenous administration, and compared with the effects of co-administration of free drug and polysorbate 80, which does not form vesicles. Niosome entrapment reduces the excretion of MTX into urine and bile whereas polysorbate 80 increases its excretion. Monitoring of the levels of MTX and its 7-hydroxy metabolite indicates that entrapped MTX is protected from rapid metabolism in vivo, particularly in niosomes but to a small degree in the micellar systems formed by polysorbate.

Administration, Oral↗

PubMed2002

Influence of some polysorbates on hydrocortisone release from hydrophilic gels considered as two-compartment models.

Hydrocortisone release from hydrogels containing of 1% and 3% polysorbate 20 or polysorbate 80, in the presence of 1,2-propylene glycol or PEG 200 has two stages. In the first one the release rates are higher than those of the second stage. Half-release times in the first stage are in the range 0.31 h to 0.48 h and in the second stage 16.65 h to 23.22 h. Hydrocortisone release from the gels containing of 1% to 3% of polysorbate 21 or 81, in the presence of 1,2-propylene glycol or PEG 200 conform to second order kinetics. Release rates in this stage are in the range from 3.80 x 10(-4)%.h-1 to 5.97 x 10(-4)%.h-1.

Anti-Inflammatory Agents↗

PubMed1985

Lack of efficacy of polysorbate 60 in the treatment of male pattern baldness.

Anecdotal reports have indicated that the nonionic detergent polysorbate 60 may be of some value in male pattern baldness. In this double-blind placebo-controlled trial, a photographic and objective scalp measurement system was developed to assess new hair growth. No significant difference was detected between subjects treated for 16 weeks with polysorbate 60 and control subjects treated with glycerin, indicating that polysorbate 60 is ineffective. Of the 141 subjects who completed the trial, 25% perceived that they grew new hair, 67% said they did not, and 8% were uncertain. Subject-reported new hair growth did not correlate with measurements, indicating that the placebo effect may be a major factor in reports of baldness "cures".

Adult↗

PubMed1986

Polysorbate 80 and E-Ferol toxicity.

The relatively recent introduction and use of an intravenous form of a vitamin E preparation (E-Ferol) has been associated with the development of an unusual syndrome and fatalities among low birth weight (less than 1,500 g), premature infants in neonatal intensive care units. We have observed an inhibitory effect by this vitamin E preparation on the in vitro response of human lymphocytes to phytohemagglutinin (PHA). E-Ferol suppressed the expected response to low doses of PHA. However, this suppression was not due to the alpha-tocopherol acetate (vitamin E) component, because alpha-tocopherol acetate by itself was not inhibitory; in fact, it often enhanced the PHA response. Because a mixture of polysorbate 80 and polysorbate 20 is used as a carrier in E-Ferol, these components were also tested and were found to be responsible for the suppression, especially the polysorbate 80. Concurrent with this suppression of PHA-induced mitogenesis was a decrease in the percentage of T11 lymphocytes.

Humans↗

PubMed1975

Effect of polysorbate 60 on interphase transport of cholesterol.

Interphase cholesterol transport was investigated at 24 +/- 1 degrees in a stirred diffusion cell and in various oil-in-water emulsions. Cholesterol uptake by vegetable oil from a cholesterol-surfactant-rich aqueous phase was extremely slow in the stirred cell; no measurable transport had occurred after 500 hr. Cholesterol transport in oil-in-water emulsions following dilution with a cholesterol-surfactant-rich aqueous phase was much faster due to the greatly increased interfacial area available for mass transfer. Equilibration half-lives, t(50), varied from 2.02 to 28.1 hr. Variations in the t(50) were due to: (a) differences in the mean oil droplet diameter among various emulsions, and (b) differences in cholesterol-polysorbate 60 micelle sizes among various dilution media. When polysorbate 60 was omitted from the dilution medium, transport occurred in a two-stage process. In the first stage, transport was extremely rapid, with the t(50) less than 30 sec; in the second stage, transport was comparable to previous emulsion rates, with the t(50) varying from 7.9 to 8.1 hr. The significance of this two-stage transport to mechanisms of interphase cholesterol transport is briefly discussed.

Cholesterol↗

PubMed1977

Effect of sorbitol on interaction of phenolic preservatives with polysorbate 80.

The effect of sorbital on the binding of several commonly used phenolic preservatives (i.e., p-hydroxybenzoic acid, methylparaben, ethylparaben, and propylparaben) with the nonionic surfactant polysorbate 80 was investigated using an equilibrium dialysis technique. The binding data were expressed in the form of Scatchard plots utilizing a modified form of the Scatchard equation. The data analysis indicated that all four phenolic preservatives were bound to two distinct loci within the polysorbate micelle; one exhibited a high affinity and a low capacity for the preservative molecules, while the other appeared to have a near-zero affinity but an almost infinite binding capacity. The high affinity site was assumed to be located near the junction of the hydrocarbon core with the polyoxyethylene region of the micelle. The interaction of the preservatives with the second class of sites apparently involved a non-specific and nonsaturable partitioning of the preservative molecules into the polyoxyethylene region of the micelle. Sorbitol was ineffective in displacing significant amounts of bound preservative from either binding site, presumably because it was too polar to partition into the micelle sufficiently to displace bound preservative.

Chemical Phenomena↗

PubMed1978

Autoxidation of polysorbates.

Aqueous solutions of polysorbate 20 undergo autoxidation on storage, with the peroxide number increasing and subsequently decreasing again, the acidity increasing continuously, the pH and surface tension falling and tending to level off, and the cloud point dropping sharply until turbidity begins at room temperature. The changes are accelerated by light, elevation of temperature, and a copper sulfate catalyst. At the same time, hydrolysis occurs, liberating lauric acid. Analysis of the alterations in these properties leads to the conclusion that hydrolysis has the major influence near room temperature and that oxyethylene undergoes chain shortening at temperatures above 40 degrees. However, evidence of degradation is detectable even in previously unopened commercial samples of polysorbates 20, 40, and 60, warranting attention to the stability of and standards for these surfactants as compared with the solid alkyl ether type of nonionic surfactant.

Chemical Phenomena↗

PubMed1980

Effect of polyols on interaction of paraben preservatives with polysorbate 80.

A quantitative study of the interaction of the methyl, ethyl, propyl, and butyl esters of p-hydroxybenzoic acid with polysorbate 80 in the presence and absence of two polyols (propylene glycol and glycerol), which were potential competitors, was performed. The results indicate that neither competitor displaced significant amounts of the parabens from their binding sites on polysorbate 80. The previously observed synergistic antimicrobial effects of these polyols appear to be due to a mechanism other than the displacement of the parabens from their micellar binding sites.

Alcohols↗

PubMed1986

Ionophoric properties of polysorbate 80.

Polysorbate 80, a surfactant often assumed to be inert, was found to bind a number of biochemically important ions (K+, Na+, NH4+, Ca2+) and transport them through a model membrane (CH2Cl2). The rates and fluxes of potassium ions were found to depend on the initial concentration of potassium ion, the polysorbate 80 concentration, the temperature, and the stirring rate. The thermodynamic constants for the process were determined and its mechanism is discussed.

Chemical Phenomena↗

PubMed2001

Investigating the molecular heterogeneity of polysorbate emulsifiers by MALDI-TOF MS.

Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS) is a new technique that can be used to determine the molecular composition of polysorbate emulsifiers, which are commonly used as food additives. This is the first study to offer such a detailed examination of these heterogeneous compounds. MALDI-TOF MS is a powerful tool that can provide a polysorbate mass profile in less than two minutes. 2',4',6'-Trihydroxyacetophenone monohydrate was chosen to be an ideal matrix, as it easily facilitated desorption and ionization, provided good resolution, and allowed for fast and simple preparation of the sample. By addition of aqueous 0.01 M potassium chloride, species were resolved exclusively as potassium adducts in the positive ion mode. MALDI-TOF MS analysis before and after saponification indicated the presence of unbound ethylene oxide polymers, as well as free and esterified sorbitan- and sorbide-based species. Some evidence for the presence of disorbitan-based species was provided. Also illustrated were the polydispersity of the oxyethylene chains, the degree of esterification, and the identity of esterified fatty acids.

Emulsions↗

PubMed2000

Cardiopulmonary side-effects and pharmacokinetics of an emulsion of propofol (Disoprivan) in comparison to propofol solved in polysorbate 80 in goats.

The aim of this study was to determine whether any pharmacokinetic or pharmacodynamic differences exist in goats between propofol in its currently licensed form (Disoprivan) and a new 1% solution of propofol (NSP) containing polysorbate 80. Nine goats received, on two different occasions in a randomized double-blinded order, 4 mg/kg propofol intravenously (i.v.; Disoprivan or NSP). To detect differences in cardiopulmonary effects and pharmacokinetics, the Wilcoxon signed rank test for paired data was used. In the NSP group the duration of initial apnoea was significantly longer, and 6 and 12 min after drug application PaO2 levels were significantly lower than in the Disoprivan group. Mean cardiovascular parameters did not differ significantly between the groups but in the NSP group in six goats marked changes in blood pressure occurred: systolic arterial pressures fell to a minimum of 40-60 mmHg within the first 10 min. This was followed by a marked increase in blood pressure, with maxima exceeding 300 mmHg. In the NSP group the half-life of propofol was significantly longer, the clearance rate was smaller and the areas under the drug concentration-time curves were larger than in the Disoprivan group. The cardiopulmonary side-effects of NSP suggest that propofol dissolved in polysorbate 80 is not a suitable alternative to the current formulation of propofol.

Anesthetics, Intravenous↗

PubMed2000

Polysorbate-80 coating enhances uptake of polybutylcyanoacrylate (PBCA)-nanoparticles by human and bovine primary brain capillary endothelial cells.

Certain drugs such as dalargin, loperamide or tubocurarine are not transported across the blood-brain barrier (BBB) and therefore exhibit no effects on the central nervous system. However, effects on the central nervous system can be observed when these drugs are loaded onto polybutylcyanoacrylate (PBCA)-nanoparticles and coated with polysorbate 80. The mechanism by which these complexed nanoparticles cross the BBB and exhibit their effects has not been elucidated. Cultured microvessel brain endothelial cells of human and bovine origin were used as an in vitro model for the BBB to gain further insight into the mechanism of uptake of nanoparticles. With cells from these species we were able to show that polysorbate 80-coated nanoparticles were taken up by brain endothelial cells much more rapidly and in significantly higher amounts (20-fold) than uncoated nanoparticles. The process of uptake was followed by fluorescence and confocal laser scanning microscopy. The results demonstrate that the nanoparticles are taken up by cells and that this uptake occurs via an endocytotic mechanism.

Animals↗

PubMed2004

Influence of formaldehyde impurity in polysorbate 80 and PEG-300 on the stability of a parenteral formulation of BMS-204352: identification and control of the degradation product.

The purpose of this study was to identify a degradation product formed in the clinical parenteral formulation of BMS-204352, investigate the role of excipients in its formation, and develop a strategy to minimize/control its formation. The degradant was identified as the hydroxy methyl derivative (formaldehyde adduct, BMS-215842) of the drug substance based upon liquid chromatography/mass spectroscopy (LC/MS), liquid chromatography/mass spectroscopy/mass spectroscopy (LC/MS/MS), nuclear magnetic resonance (NMR), and chromatographic comparison to an authentic sample of hydroxymethyl degradation product, BMS-215842. An assay method for the detection of formaldehyde based on HPLC quantitation of formaldehyde dinitrophenylhydrazone was developed to quantitate its levels in various Polysorbate 80 and PEG 300 excipient lots. A direct relationship between the levels of formaldehyde in the excipients and the formation of the hydroxymethyl degradant was found. To confirm the hypothesis that the formaldehyde impurity in these two excipients contributed to the formation of the hydroxymethyl degradant, several clinical formulation lots were spiked with formaldehyde equivalent to 1, 10, and 100 mg/g of BMS-204352. A correlation was found between the formaldehyde level and the quantity of the hydroxymethyl degradant formed upon storage at 5 and 25 degrees C. From these experiments, a limit test on the formaldehyde content in polysorbate 80 and PEG 300 can be set as part of a strategy to limit the formation of the degradation product.

Chromatography, High Pressure Liquid↗