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PubMed2004

Development of clinical dosage forms for a poorly water soluble drug I: Application of polyethylene glycol-polysorbate 80 solid dispersion carrier system.

Different formulation approaches were evaluated to ensure that the formulation of a poorly water soluble compound chosen during early development achieves optimum bioavailability. The insoluble compound has an aqueous solubility of 0.17 micro g/mL at 25 +/- 1 degrees C, a relatively high permeability (Caco2 P(app) = 6.1 x 10(-4) cm/min), and poor bioavailability in dogs (dry blend formulation). Based on the prediction by GastroPlus, the oral absorption of this compound is sensitive to its apparent solubility and particle size. The oral bioavailability of three different formulations was compared in a dog model: a cosolvent-surfactant solution, a solid dispersion in a mixture of polyethylene glycol 3350 and polysorbate 80, and a dry blend of micronized drug with microcrystalline cellulose. In absence of a parenteral injection, the bioavailability of the solution was considered to be 100%, and the relative oral bioavailability of the three formulations was 100, 99.1, 9.8, respectively. Comparable bioavailability was obtained with the solid dispersion and the cosolvent-surfactant solution, both of which showed a 10-fold higher bioavailability than the dry blend. Thus, a 20 mg dose strength capsule containing the solid dispersion formulation was selected for clinical development. The selected solid dispersion system was physically and chemically stable for at least 16 months at 25 degrees C/60% RH. In conclusion, the bioavailability of a poorly water soluble drug was greatly enhanced using the solid dispersion formulation containing a water soluble polymer with a surface active agent.

Animals↗

PubMed2007

Impact of cremophor-EL and polysorbate-80 on digoxin permeability across rat jejunum: delineation of thermodynamic and transporter related events using the reciprocal permeability approach.

The effect of Cremophor-EL (Cr-EL) and polysorbate-80 (PS-80) on the transepithelial permeability of digoxin (DIG) has been evaluated using the reciprocal permeability approach to delineate thermodynamic and transporter related events. Permeability data were corrected for solubilization using the micellar association constant (Ka) obtained from Papp data generated in the presence of the nonspecific ATPase inhibitor sodium orthovanadate. In the presence of mucosal Cr-EL, a concentration dependent decrease in serosal-mucosal (S-M) and increase in M-S transport was observed. Whilst serosal Cr-EL resulted in a reduction in S-M DIG transport, no impact on M-S transport was apparent. For PS-80, the presence of either serosal or mucosal surfactant led to a decrease in secretory (S-M) DIG transport, however no effect on absorptive transport was evident. The data confirm the potential P-gp inhibitory effects of Cr-EL, but suggest that in contrast to Cr-EL, PS-80 is not a potent inhibitor of P-gp and is incapable of increasing absorptive drug transport, at least in excised rat intestinal tissue and at the concentrations tested. The data are also consistent with the involvement of additional transporters (both apical and basolateral) in the intestinal permeability of DIG, although more definitive data is required to confirm this possibility.

ATP Binding Cassette Transporter, Subfamily B, Mem↗

PubMed1975

Interaction of substituted benzoic acids with polysorbate 20 micelles.

Equilibrium solubilities of a series of substituted benzoic acids in different concentrations of polysorbate 20 at controlled pH were measured. The maintenance of pH was achieved using a pH-stat assembly. A linear relationship was found between the amount of benzoic acid solubilized and surfactant concentration. As solubilizate polarity increased, the amount solubilized also increased. Solubility data were analyzed, and the interaction between solubilizate molecules and micelles was calculated in terms of partition coefficients of ionized and unionized molecules between aqueous and micellar phases. A linear relationship between pi values (log partition coefficients) of functional groups and aqueous-micellar partition coefficient was found.

Benzoates↗

PubMed1986

Influence of polysorbate 80 (Tween 80) and etoposide (VP-16-213) on the pharmacokinetics and urinary excretion of adriamycin and its metabolites in cancer patients.

Polysorbate 80 (Tween 80) is present in the IV pharmaceutical preparation of VP-16-213 marketed as VePesid (Bristol-Myers) (etoposide 100 mg, benzylalcohol 150 mg, polyethylene glycol 300 3250 mg, citric acid 10 mg, Tween 80 400 mg and absolute alcohol to 5 ml per 100 mg ampule of VP16), to increase its miscibility with blood. We have examined the effects of 400 mg/m2 Tween 80 IV and 100 mg/m2 VP16 on the pharmacokinetics of Adriamycin (ADR, 30 or 40 mg/m2). ADR and metabolite concentrations were measured by HPLC. ADR plasma profiles were best fitted to a bi-exponential decay and a two-compartment open model. Tween 80 did not alter the values of the two ADR half-lives, nor did it affect metabolite kinetics of their urinary excretion. However, in a similar manner and consistently in all patients, both Tween 80 and VP16 increased the volume of distribution of the central compartment for ADR up to 3-fold, decreased the AUC of ADR up to 2-fold and increased its clearance by exactly the same amount. These effects were due to reduced plasma ADR concentrations during the early phase of its kinetics. Urinary excretion of ADR was also increased. In conclusion, VP16 is likely to affect the kinetics of drugs administered with it: early plasma concentrations will fall due to a general physiological effect of Tween 80 on the apparent volume of circulation.

Adult↗

PubMed2004

Specific role of polysorbate 80 coating on the targeting of nanoparticles to the brain.

It was reported that nanoparticles with polysorbate 80 (Tween 80, T-80) coating represented tools used for delivering drugs to brain. Nevertheless, disputations were once aroused for some complications. Aimed to have a better understanding of the specific role of T-80 coating on nanoparticles and simplify the problem, the direct observation of brain targeting combined with in vivo experiments was carried out in this work using the model nanoparticles (MNPs). The presence of a complex composed by the model loading, T-80 and nanoparticles was found in the preparation of MNPs. The result was further supported by some surface properties of MNPs. Being bound to nanoparticles that were overcoated by T-80 later, was necessary for the loading to be delivered to brain. Partial coverage was enough for T-80 coating to play a specific role in brain targeting. It seemed that brain targeting of nanoparticles was concerned with the interaction between T-80 coating and brain micro-vessel endothelial cells. Therefore, the specific role of T-80 coating on nanoparticles in brain targeting was confirmed.

Animals↗

PubMed2002

Cosolubilization of non-polar drugs in polysorbate 80 solutions.

This study investigated the cosolubilization phenomenon of three non-polar drugs (hydrocortisone, beta-estradiol, and ethynylestradiol) in polysorbate 80 solutions. It was found that the solubility of any drug decreased in the presence of other steroidal compounds. In an attempt to understand the observation, the author proposed a model to describe and to predict the drug solubility in the presence of other non-polar drugs in a non-ionic surfactant. The model indicates that, in a non-ionic surfactant solution that contains both drugs D(a) and D(b), the total solubility [D(a)(tot)] is related not only to the physical chemical properties of D(a) (micellar equilibrium constant K(a), the intrinsic solubility [D(a)]), as well as the total surfactant concentration [S(tot)], it is also related to the physical chemical properties of the D(b). Mathematically, the [D(a)(tot)] decreases as the product of the micellar equilibrium constant K(b) and the intrinsic solubility [D(b)] increases. The model was also put to the test by comparing the cosolubilization data obtained experimentally with the data calculated from the proposed model. The fact that these two sets of data were in good agreement lent strong support to the newly proposed model.

Pharmaceutical Preparations↗

PubMed2002

Determination of the docetaxel vehicle, polysorbate 80, in patient samples by liquid chromatography-tandem mass spectrometry.

A new simple method was developed for the quantitative determination of the docetaxel (Taxotere) vehicle, polysorbate 80 (Tween 80), in human plasma. Calibration curves were constructed in the range of 1-100 microg/ml, using paclitaxel (0.01 mM) as internal standard, and were analyzed using a power fit with equal weighting. Sample pretreatment involved a one-step extraction with acetonitrile-n-butyl chloride (1:4, v/v). The analytes were separated on a Waters X-Terra MS column (50x2.1 mm I.D.) packed with 3.5-microm ODS material, and eluted with methanol-water (9:1, v/v) containing 0.1% formic acid. The column effluent was monitored by tandem mass spectrometry with electrospray ionization. The overall extraction efficiency was 50-60%, with values for precision and accuracy of < or =16% and <15% relative error, respectively. Our current method is approximately 60-100-fold more sensitive than previous assays, and will be used to define Tween 80 disposition in patients receiving Taxotere.

Antineoplastic Agents, Phytogenic↗

PubMed1999

The versatility of polysorbate 80 (Tween 80) as an ionophore.

A number of experiments were performed to illustrate the unusual versatility of Polysorbate 80 (Tween 80) as an ionophore. New ions shown to be transported by it from and to water layers through a model membrane (CH2Cl2) include H3O+, Li+, Pb2+, Co2+, piperidinium ion, guanidinium ion, and Paraquat, while two complex ions resisted transport under the conditions used. "Reverse" transport of lipophilic guests (azobenzene, azulene, ferrocene) from and to organic solvents through water was also promoted by Tween 80, but C60 was not carried. Three water molecules were transported per molecule of KSCN by the Tween.

Excipients↗

PubMed2006

"Sponge" nanoparticle dispersions in aqueous mixtures of diglycerol monooleate, glycerol dioleate, and polysorbate 80.

Lipid nanoparticles of nonlamellar lyotropic phases have a wide solubilizing and encapsulating spectrum for a range of substances thanks to their nanostructured interior featuring both lipophilic and hydrophilic domains. As a consequence, these systems have emerged as promising drug delivery systems in various pharmaceutical and diagnostic applications. Here we present the phase behavior and dispersion properties of a novel three-component lipid system composed of diglycerol monooleate (DGMO), glycerol dioleate (GDO), and polysorbate 80 (P80) which shows several advantageous features relating to drug delivery applications including: spontaneous dispersion formation with a narrow size distribution and tunable particle phase-structure. The obtained phase diagram shows the presence of lamellar (L(alpha)), hexagonal (H(2)), and reverse bicontinuous cubic (V(2)) liquid crystalline phases and an inverse micellar (L(2)) solution. A particularly interesting observation is the presence of a phase region where two liquid phases coexist, most likely the L(2) and L(3) ("sponge phase"). These two phase structures appear also to coexist in the submicron particles formed in the dilute water region, where the L(3) element appears to stabilize nanoparticles with inner L(2) structure. Increasing the fraction of the dispersing P80 component results in the growth of the more water rich L(3) "surface phase" at the expense of the size of the inner L(2) core.

Diglycerides↗

PubMed2005

Electrochemical studies on polysorbate-20 (Tween 20)-entrapped haemoglobin and its application in a hydrogen peroxide biosensor.

Haemoglobin (Hb) was entrapped in polysorbate 20 and then modified on a pyrolytic graphite electrode. Electrochemical studies revealed that a pair of stable and well-defined redox peaks attributed to the direct redox reaction of Hb could be observed in a phosphate buffer solution (pH 6.0). The anodic and cathodic peaks were located at -236 and -316 mV (versus a saturated calomel reference electrode) separately. The formal potential, E0', was linearly varied with pH in the range from 3.0 to 10.0 with a slope of -48.0 mV.pH-1. Moreover, the protein was capable of catalysing the reduction of H2O2. Accordingly, an unmediated biosensor for H2O2 was prepared with a linear range from 8.0x10(-7) to 1.0x10(-3) M. This biosensor exhibited good stability, sensitivity and reproducibility.

Biosensing Techniques↗

PubMedDate not supplied

Determination of polysorbate in ascites fluid from a premature infant.

A method is described for the determination of poly(oxy-1,2-ethanediyl)oligomers in body fluids using ammonium cobaltothiocyanate complexation in conjunction with high pressure liquid chromatography and visible spectrophotometry. Analysis of peritoneal fluid from a baby given E-ferol, a vitamin E supplement, revealed levels as high as 100 micrograms/mL polysorbate.

Ascitic Fluid↗

PubMed2005

Hypersensitivity reactions to the polysorbate contained in recombinant erythropoietin and darbepoietin.

The following case reports are of two patients who have developed hypersensitivity reactions to the red cell growth hormones, darbepoietin and erythropoietin. The subsequent skin testing and clinical course suggested that the cause of these reactions was due to the excipient polysorbate 80. This finding might have implications in the recent increase in the incidence of pure red cell aplasia.

Adult↗

PubMed1984

Cmc of mixtures of chlorpromazine hydrochloride and polysorbate 80 determined by pH measurements.

The cmc of mixtures of chlorpromazine hydrochloride and polysorbate 80 was determined by pH titration. The values thus obtained coincided with those determined by the surface tension method. The mixtures studied could be divided into two groups according to the shape of their pH concentration curves. For mixtures containing less than 0.8 mole fraction chlorpromazine, the curves suggest that some interaction occurs in the premicellar concentration range. For mixtures containing more than 0.8 mole fraction chlorpromazine, the curves suggest that the micellar process occurs in more than one step.

Chemistry, Pharmaceutical↗

PubMed1994

Enhanced rectal absorption of itazigrel formulated with polysorbate 80 micelle vehicle in rat: role of co-administered esterase.

We investigated the effect of esterase on rectal absorption in the rat of itazigrel using polysorbate 80 (PS-80) micelle as a vehicle to overcome the poor aqueous solubility of itazigrel. The itazigrel formulation prepared with PS-80 increased the absorption compared with a 0.25% carmellose sodium suspension, probably by supplying the itazigrel solute to keep a high concentration at the epithelial surface. When esterase was co-administered with the formulations containing PS-80, the absorption of itazigrel from rat rectum was accelerated further, by rapid release of itazigrel from the micelle vehicle after enzymatic degradation of the PS-80 micelle.

Absorption↗

PubMedDate not supplied

Polysorbate 80 and low-osmolality water-soluble contrast medium enema in diagnosis and treatment of faecal obstruction in malignant phaeochromocytoma. Report of a case.

Stercoral obstruction in a young woman with disseminated phaeochromocytoma was diagnosed and treated successfully using an enema of isosmolar iohexol (Omnipaque) and 1% polysorbate 80 (Tween 80) without complication. Surgical intervention was thus avoided. A low osmolality water-soluble contrast medium (iohexol 150 mg I/ml) with a wetting agent (1% Tween 80) was used because a barium suspension would have inspissated, exacerbating the constipation and a hyperosmolar contrast medium might have precipitated a hypertensive crisis and destabilized her critical salt and water balance.

Adrenal Gland Neoplasms↗

PubMed1983

Intestinal absorption of dl-alpha-tocopherol from bile salts and polysorbate 80 micellar solutions in rat.

The intestinal absorption of dl-alpha-tocopherol (VE) from various micellar solutions was studied by the in situ recirculating perfusion in rat small intestine. The perfused micellar solutions of VE were formed by sodium taurocholate (STC), sodium taurodeoxycholate (STDC) or polysorbate 80 (PS-80). The absorption ratio of VE was STC greater than STDC greater than PS-80 micellar solutions. The addition of egg lecithin (PC) to all micellar solutions caused the decrease of the absorption. The absorption ratio did not necessarily have a simple correlation with the VE solubilization in these micellar solutions. And it was also found that the absorption ratio correlated with the micellar size and with net water flux in the intestinal lumen.

Animals↗

PubMed2001

Development of hexachlorobenzene-dechlorinating mixed cultures using polysorbate surfactants as a carbon source.

The use of three nonionic polysorbate surfactants--Tween 60, 61 or 65--as the sole carbon source to sustain methanogenesis and dechlorination, as well as the effect of long-term exposure of enriched cultures to these surfactants, was investigated through the development of three sediment-derived cultures. Over a one-year period, the carbon source in these cultures was gradually switched from glucose and methanol to surfactant only, while the surfactant concentration was increased from an initial concentration of 100 mg/L to 400 mg/L. In each feeding cycle, the surfactants were partially degraded and converted to methane. Transition from glucose to Tween surfactants as the electron donor did not affect the rate, extent, and pathway of HCB transformation. These surfactants sustained the reductive dechlorination of HCB even after one year of continuous addition to the enriched cultures. This study demonstrated that reductive dechlorination of HCB sustained by the fermentation of Tween surfactants is feasible. The results support the use of anaerobically degradable Tween surfactants for the biotransformation of polychlorinated organic compounds. In principle, these surfactants could be used to simultaneously increase the bioavailability of subsurface contaminants while serving as the carbon and electron source for microbial reductive dechlorination.

Biological Availability↗

PubMedDate not supplied

A comparison of two commercially irradiated Trypticase Soy Agars containing lecithin and polysorbate 80.

Gamma-radiation sterilized Trypticase Soy Agar containing lecithin and polysorbate 80 (TSA++) (Becton Dickinson Microbiology Systems, Cockeysville, MD) and irradiated TSA++ (Adams Scientific, West Warwick, RI) were tested by a quantitative spread plate method. Four bacteria Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 10145, Staphylococcus aureus ATCC 25923, Streptococcus pyogenes ATCC 19615 and the yeast Candida albicans ATCC 10231 were tested in two separate experiments using different lots of media. A strain of Aspergillus niger ATCC 16404, was tested by a qualitative streak plate method. The Becton Dickinson Microbiology Systems (BDMS) irradiated TSA++ overall recovered a greater number of organisms than the Adams Scientific TSA++ in both experiments and allowed for the earlier recovery of S. pyogenes ATCC 19615. The growth of A. niger ATCC 16404, was comparable on both media. Efficacy of the media to neutralize 1, 2 and 3% phenol as well as 0.001, 0.01 and 0.1% benzalkonium chloride (BC) solutions was done by a disk diffusion method using 2 gram-positive and 4 gram-negative bacteria. Both media showed complete neutralization of the 0.001 and 0.01% BC solutions and partial neutralization of the 0.1% BC solution. The BDMS TSA++ showed better neutralization of the 2 and 3% phenol solutions than the Adams Scientific TSA++. This data indicates that not all irradiated TSA++ media perform in an equivalent manner.

Agar↗