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At least 127 records · Page 7Linked to original sources
PubMed1995

Effects of polysorbates and Cremophor EL on vascular responses in rat aorta.

The effects of Tween 20, Tween 80, and Cremophor EL, surface active agents which are used for dispersion of water-insoluble substances, on vascular responsiveness were investigated using rat aortic rings. In high concentrations all these agents produced persistent contractions in aortic rings independent of the presence of endothelium. These contractions were not influenced by inhibitors of known endogenous contractile mediators. Incubation with these agents caused a concentration-dependent inhibition of the endothelium-dependent relaxant responses to acetylcholine in intact precontracted aortic rings. Endothelium-independent relaxations produced by sodium nitroprusside were not inhibited, but rather potentiated in the presence of Tween 80 (10(-1) ml/l). On the other hand, Tween 80 inhibited the contractile effects of 5-hydroxytryptamine, phenylephrine, and bradykinin significantly. The data suggests that these substances affect both endothelial cells and vascular smooth muscle.

Acetylcholine↗
PubMed2004

Combined effect of pH and polysorbates with cyclodextrins on solubilization of naringenin.

pH control and inclusion complex formation are commonly used as solubilization techniques in formulating ionizable drugs. Naringenin is a weakly acid compound with a low water solubility. The role of both ionized and unionized species of naringenin in solution by complexation with beta-cyclodextrin, 2-hydroxypropyl-beta-cyclodextrin and methyl-beta-cyclodextrin was investigated. This combined use of ionization and complexation increases not only the solubility of the unionized naringenin, but also that of the ionized one. This study puts on evidence the role of pH, pKa and complexation constants in increasing drug total aqueous solubility, determined by the single components in solution, as ionized and unionized naringenin both in free and complexed forms. Moreover, the presence of non-ionic surfactants in the media of complexation gives a positive contribution to the improvement of the solubility of naringenin, alone or in combination with beta-cyclodextrin.

Algorithms↗
PubMed2005

Composition analysis of two batches of polysorbate 60 using MS and NMR techniques.

Batch variation in Tween 60 has shown to influence the rheological properties of semisolid emulsions. MS (LC-MS, GC-MS, MS(n)) and NMR ((13)C, (1)H, (1)H COSY and HMBC) techniques were used to analyze and compare the composition of two batches of Tween 60 with particular emphasis on the number of POE groups and their distribution within the molecule. Acid and saponification values were also determined. The batches contained different proportions of components (sorbitan polyethoxylates, sorbitan monoester-diester-polyethoxylates and isosorbide monoester-diester-polyethoxylates). The number of POE groups were averaged over the four sites in sorbitan and the two sites in isosorbide molecules. The batches differed from each other in terms of (i) the POE sorbitan stearate/POE sorbitan palmitate ratios (batch 1, 3:2 and batch 2, 4:5), (ii) the ratio of sorbitans to isosorbides (batch 1, 2:3; batch 2, 7:13); and (iii) the acid values (batch 1, 3.1; batch 2, 0). It is concluded that liquid chromatography combined with electrospray mass spectrometry and ion trap separation is a useful tool for establishing the compositional profile of different batches of Tweens. (1)H NMR could provide a simple and rapid pharmacopoeial test for the ratio of sorbitan to isosorbide in Tweens.

Chromatography, High Pressure Liquid↗
PubMed2000

Comparison of UV spectrophotometric and LC methods for the determination of nortriptyline hydrochloride in polysorbate 80 based oil/water (o/w) microemulsions.

A new rapid, reliable and specific UV spectrophotometric method was developed for the determination of nortriptyline hydrochloride formulated into o/w microemulsions. The UV spectra of nortriptyline standard solution in methanol and placebo (microemulsion without nortriptyline) were recorded over the wavelength range 200-600 nm and the spectra for placebo and nortriptyline loaded microemulsion were recorded over the range 260-400 nm in order to determine the overlapping that might appears, and hence to set the wavelength that could be used for the quantitative analysis. This method was validated and compared with a liquid chromatography (LC) procedure used for the quantitative analysis of the drug. Both methods showed excellent precision and accuracy with RSD values of 2.37 and 1.41%, respectively, for the LC method, and values of 1.24 and 2.88%, respectively, for the UV spectrophotometric method. The established linearity range was 10-50 microg ml(-1) (r2 = 0.9985) and 20-60 microg ml(-1) (r2 = 0.9979) for the HPLC and UV spectrophotometric methods respectively. The recoveries of nortriptyline from spiked placebos were > 95% for both methods over the linear range. The methods have been successfully used for determining the nortriptyline content of microemulsions and for evaluating the chemical stability of the drug in nortriptyline-loaded microemulsions.

Antidepressive Agents, Tricyclic↗
PubMed1999

Solubilization of ionized and un-ionized flavopiridol by ethanol and polysorbate 20.

Because the ionized species is more polar than its un-ionized counterpart, it is often assumed that the ionized species of the drug does not make a meaningful contribution to solubilization by either cosolvents or surfactants. This report extends previous studies on solubilization of the ionic species by a combination of pH control and complexation to pH control and micellization and to pH control and cosolvency. The total aqueous solubility is expressed as the addition of the concentration of all contributing species: free un-ionized drug [Du], free ionized drug [Di], un-ionized drug micelle [DuM], and ionized drug micelle [DiM] for surfactant, and free un-ionized drug [Dcu] and free ionized drug [Dci] for cosolvent. The equations indicate that under certain conditions the ionized species can be more important in determining the drug total solubility than the un-ionized species. Flavopiridol, a weak base, is used to test these newly generated equations. As expected, the micellar partition coefficient and solubilization power for ionized flavopiridol are both less than those of the un-ionized species. However, at acidic pH, the solubilities of the ionized drug in surfactant micelles [DiM] and in cosolvent-water [Dci] are both much greater than that of the un-ionized drug. This difference is because the solubilization of the ionized drug is proportional to its aqueous solubility, and its solubility [Di] can be as much as 24-fold greater than that of the free un-ionized species [Du].

Antineoplastic Agents↗
PubMed1999

A polysorbate-based non-ionic surfactant can modulate loading and release of beta-lactoglobulin entrapped in multiphase poly(DL-lactide-co-glycolide) microspheres.

PURPOSE: The goal of the present paper was to investigate the role of a surfactant, Tween 20, in the modulation of the entrapment and release of beta-lactoglobulin (BLG) from poly (DL-lactide-co-glycolide) microspheres. METHODS: Poly(DL-lactide-co-glycolide) microspheres containing BLG were prepared by a water-in-oil-in-water emulsion solvent procedure. Tween 20 was used as a surfactant in the internal aqueous phase of the primary emulsion. BLG entrapment efficiency and burst release were determined. Displacement of BLG from microsphere surface was followed by confocal microscopy observations and zeta potential measurements, whereas morphological changes were observed by freeze-fracture electron microscopy. RESULTS: Tween 20 was shown to increase 2.8 fold the encapsulation efficiency of BLG without any modification of the stability of the first emulsion and the viscosity of the internal aqueous phase. In fact, Tween 20 was shown to be responsible for removing the BLG molecules that were adsorbed on the particle surface or very close to the surface as shown by confocal microscopy and zeta potential measurements. Tween 20 reduced the number of aqueous channels between the internal aqueous droplets as well as those communications with the external medium. Thus, the more dense structure of BLG microspheres could explain the decrease of the burst release. CONCLUSIONS: These results constitute a step forward in the improvement of existing technology in controlling protein encapsulation and delivery from microspheres prepared by the multiple emulsion solvent evaporation method.

Chemistry, Pharmaceutical↗