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At least 19 recordsLinked to original sources
PubMed1984

Teratology of intravaginally administered contraceptive jelly containing octoxynol-9 in rats.

Octoxynol-9, a nonionic surfactant used as a spermicidal agent in ORTHO-GYNOL (registered trademark) Contraceptive Jelly (Ortho Pharmaceutical Corporation, Raritan, NJ), was administered intravaginally to pregnant Sprague Dawley COBS CD rats at dosages of 0.5 mg/kg/day and 5 mg/kg/day (two-thirds and six times the clinical dosage) on days 6-15 of gestation in order to assess its teratogenic potential. Untreated, sham, and vehicle control groups were also incorporated into the study protocol. No meaningful differences were observed between the treated and control groups in maternal toxicity, maternal reproductive parameters, fetal toxicity, and the incidence of external, visceral, and skeletal malformations or developmental variations. It is concluded that octoxynol-9 is not embryotoxic or teratogenic when administered intravaginally to rats during organogenesis.

Abnormalities, Drug-Induced↗
PubMed1986

Evaluation of the cytotoxicity and genotoxicity of the spermicides nonoxynol-9 and octoxynol-9.

The cytotoxic and genotoxic potentials of the spermicidal agents, nonoxynol-9 (N-9) and octoxynol-9 (0-9), were evaluated in in vitro test systems using rat liver cells. N-9 was also tested for the induction of sperm abnormalities in mice. Dose-related cytocidal effects were seen after the addition of N-9 and O-9 to the culture medium for 24 h. The mean concentrations of N-9 and O-9 necessary to decrease the number of viable cells by 50% (LC50) were 24 and 43 micrograms/ml of media, respectively. The spermicides neither induced DNA repair in freshly isolated hepatocytes, nor caused any mutations at HGPRT locus in the T51B rat liver cell line. There was also a lack of malignant transformation response in the low-calcium assay. Further, the germinal cells of mice remained unaffected by N-9.

Animals↗
PubMed1987

Immunotoxicology studies on octoxynol-9 and nonoxynol-9 in mice.

In a double-blind study, mice were injected intraperitoneally with 0.2 ml 0.2% octoxynol-9 (O-9), 0.2 ml 0.2% nonoxynol-9 (N-9), or 0.2 ml saline (control) daily for 24 days. Another control group received no treatment. All mice were immunized twice with sheep red blood cells (SRBC) and bled by caudal incision. Mice receiving N-9 lost weight (P less than 0.02), had smaller livers (P less than 0.05), and showed enlarged spleens (P less than 0.05). The N-9-treated mice did not differ from either control group in the primary or secondary anti-SRBC responses, leukocyte (WBC) counts, or in the sizes of the kidneys, hearts, lungs, or thymuses. Mice receiving O-9 showed no significant differences from either control group in any of these tests. Serum immunoglobulin M (IgM) and immunoglobulin G (IgG) levels were similar in mice treated with O-9, N-9, or saline. All 3 groups had higher levels of both classes of immunoglobulins on day 16 than did untreated controls. This study shows that O-9, given to mice in doses 3 times that used by humans, is nontoxic, whereas the same dose of N-9 has minor deleterious effects.

Animals↗
PubMed1983

Effect of inorganic additives on solutions of nonionic surfactants V: Emulsion stability.

Electrolytes often break emulsions to which they were added as active ingredients, adjuvants, or impurities. The stability of oil-in-water emulsions containing octoxynol 9 NF as the emulsifier and various added electrolytes was investigated by measuring droplet size, turbidity, and oil separation on storage at various temperatures and in a centrifugal field at 25 degrees. Electrolytes were added to hexadecane emulsions after emulsification (direct addition); alternatively, hexadecane was emulsified in octoxynol 9-electrolyte mixtures (reverse addition). Xylene emulsions were prepared by direct addition only. Hexadecane emulsions containing 0.10% octoxynol 9 were considerably more stable than xylene emulsions containing 0.60% because the surfactant is practically insoluble in hexadecane, but miscible in all proportions with xylene. An emulsifier soluble in the disperse phase as well as the continuous phase evidently forms less stable interfacial films. The electrolytes investigated were sulfuric and hydrochloric acids, magnesium nitrate, and aluminum nitrate, which salt octoxynol 9 in by complexation between its ether groups and their cations; sodium thiocyanate, which salts the surfactant in by destructuring water; and sodium chloride and sodium sulfate, which salt octoxynol 9 out. The addition of these electrolytes at concentrations up to 2 or 3 m to hexadecane emulsions produced fast and extensive creaming, little or no flocculation, no coalescence, and only minor changes in droplet size or turbidity on storage at room temperature. The extent of coalescence during centrifugation was actually reduced by the additives. Such stability is unusual. Droplet size and turbidity depended mainly on octoxynol 9 concentration. The greatest decrease in the former and increase in the latter occurred when the concentration was increased from 0.10 to approximately 0.4%. All emulsions became slightly coarser on storage at 25 degrees. Stability at 50 degrees was impaired by aluminum nitrate and magnesium nitrate and to a lesser extent by sodium sulfate and sodium chloride. Reverse-addition emulsions differentiated better between the electrolytes than direct-addition emulsions. Electrolytes salting octoxynol 9 in, especially by complexation, generally produced the finest and most stable emulsions. Similarly, xylene emulsions were destabilized more by the electrolytes which salted the emulsifier out than by those salting it in. Centrifugation of hexadecane emulsions at 7800 X g compressed the creamed emulsion layer into a plug of clear, transparent, isotropic gel from which coalesced hexadecane separated slowly on further centrifugation.(ABSTRACT TRUNCATED AT 400 WORDS)

Chemical Phenomena↗
PubMed1985

Effect of nonionic surfactants on aqueous primidone suspensions.

The following interactions between the soluble surfactant, octoxynol 9, and the very slightly soluble, finely powdered drug, primidone, in aqueous suspension were investigated: adsorption/desorption of the surfactant, micellar solubilization of the drug, and deflocculation of its particles. The last effect, measured by the sedimentation volume of the suspensions, was also investigated for other octoxynols. The adsorption of octoxynol 9 on solid primidone was proportional to the equilibrium surfactant concentration up to the critical micelle concentration. It leveled off at higher concentrations, reaching saturation at completion of a close-packed surfactant monolayer. The adsorption was essentially completely reversible. The solubility of primidone in water was very slight; its micellar solubilization was even less extensive. The sedimentation volume of primidone suspensions decreased with increasing equilibrium concentration of octoxynol 9 and began to level off at the critical micelle concentration of 0.018%. At about twice that concentration, the sedimentation volume became almost constant, but reached its lowest value only at less than or equal to 0.5%. Slow rotation of suspensions prior to sedimentation promoted flocculation and higher sedimentation volumes between 0.01 and 0.03% octoxynol 9. Octoxynols with higher hydrophilic-lipophilic balance than octoxynol 9 produced considerably larger sedimentation volumes at comparable concentrations, due to a lower surface activity and a lesser tendency to adsorb on primidone.

Micelles↗
PubMed1984

Effect of inorganic additives on solutions of nonionic surfactants VI: Further cloud point relations.

Disperse dosage forms stabilized with nonionic surfactants frequently contain electrolytes as active ingredients or adjuvants. Salting out of the surfactants by these electrolytes may cause breakdown of the dosage forms. The cloud point of an aqueous solution of octoxynol 9 was used to measure the salt effects. Electrolytes which salt octoxynol 9 out lower its cloud point, while salting-in electrolytes raise it. The observed cloud point effects are discussed according to the mechanisms involved. Salting out by dehydration in competition with octoxynol 9 for the available water was observed with sulfate and phosphate anions, sodium, potassium, and ammonium tribasications, and the nonelectrolyte sorbitol. The extensive self-association of water by hydrogen bonds at and below room temperature weakens its solvent power. Ions which reduce this self-association, breaking the structure of water, increased the cloud point of octoxynol 9. Among them were the iodide, thiocyanate, and nitroprusside anions. Ions which tighten the structure of water and enhance its self-association salted the surfactant out, lowering its cloud point. Among these were the fluoride and hydroxide anions. Complex formation between the ether linkages of octoxynol 9 and the following cations increased its cloud point: hydrogen (from strong acids), silver, magnesium, and zinc. Including published data, the only cations which do not form complexes with polyoxyethylated surfactants (and are, therefore, unable to salt them in) were the alkali metal ions sodium, potassium, and cesium and the ammonium ion.(ABSTRACT TRUNCATED AT 250 WORDS)

Acids↗
PubMed1982

The role of surfactants in the release of very slightly soluble drugs from tablets.

The ability of surfactants to accelerate the in vitro dissolution of very slightly soluble drugs has been ascribed to wetting and/or micellar solubilization. Deflocculation as a mechanism to accelerate dissolution has not been investigated. In the present study, the effect of a surfactant on the dissolution kinetics of prednisolone from tablets and the mode of action of the surfactant were investigated. The dissolution of prednisolone at 37 degrees in 0.1 N HCl containing different concentrations of the nonionic surfactant, octoxynol 9, followed zero-order kinetics. The rate constant was increased by 15, 150, and 950% when octoxynol was added to the dissolution medium at 0.0039 and 0.032% (approximately 0.5 and 4.0 times the critical micelle concentration) and incorporated into the tablets (for a final concentration of 0.0039%), respectively. The surface tensions of the dissolution media were 71, 35, and 31 dyne/cm for 0, 0.0039, and 0.032% octoxynol, respectively. The largest decrease in surface tension corresponded to the smallest increase in dissolution rate, indicating that wetting was unimportant. The micellar solubilization capacity of octoxynol was much too small to account for the increases in dissolution rate. Microscopic particle size measurements and sedimentation volume determinations showed the pronounced deflocculation of prednisolone by the surfactant. The observed increases in specific surface area at the two octoxynol concentrations were in good quantitative agreement with the increases in dissolution rate according to the Noyes-Whitney equation.

Chemistry, Pharmaceutical↗
PubMed1984

Colorimetric prednisolone assay and its application to dissolution studies.

The colorimetric method of Porter and Silber, originally developed for assaying cortisone and related corticosteroids, was adapted to the assay of prednisolone in the presence and absence of a surfactant, octoxynol 9. Optimal conditions for the colorimetric reaction between prednisolone and acidified phenylhydrazine solution were 30 min at 50 degrees C. The slight interference of octoxynol 9 with the absorbance of the yellow prednisolone-phenylhydrazine complex at 410 nm was corrected by adding an equal surfactant concentration to the blank. When freshly prepared acidified phenylhydrazine solutions were used, the colorimetric method had a sensitivity of 0.2 microgram/mL and a precision of 0.1 microgram/mL. Its averaged relative standard deviation was 3.7% in the prednisolone concentration range of 10-300 micrograms/mL.

Colorimetry↗
PubMed1976

Effect of inorganic additives on solutions of nonionic surfactants III: CMC's and surface properties.

Continuing work on the interaction of inorganic additives with nonionic surfactants in aqueous solution dealt with their effect on the CMC and surface tension. The surfactants were octoxynol and polyoxyethylated oleyl alcohol, containing an average of 9.5 and 10 ethylene oxide units, respectively. Their CMC values were lowered by most electrolytes studied, representing salting out of the surfactants. The steepest reductions in the CMC were produced by the nitrates of sodium and potassium, which had been found to lower the cloud points of nonionic surfactants, salting them out because of the inability of their cations to form complexes with the ether oxygen linkages of the polyoxyethylene moieties. However, even electrolytes with cations such as hydrogen, lithium, calcium, nickel, lead, and aluminum capable of forming complexes with the ether oxygens, thereby increasing the cloud points of the surfactants, lowered their CMC values. In the presence of increasing concentrations of the latter electrolytes, the CMC values frequently went through minima and approached the CMC of the surfactant in the absence of additives. Increases in the CMC over the entire range of additive concentrations investigated were produced by cadmium nitrate for octoxynol, urea for polyoxyethylated oleyl alcohol, and magnesium nitrate for both. Net increases in the plateau or micellar surface tension of polyoxyethylated oleyl alcohol, i.e., in the constant surface tension of surfactant solutions above the CMC, were brought about by the nitrates of cadmium, aluminum, and magnesium at low concentrations only and by urea at all concentrations. This increase is interpreted as salting in. The area per surfactant molecule adsorbed at the air-water interface was reduced by all added electrolytes. Urea caused no such reduction.

Adsorption↗
PubMed1983

An user acceptability study of vaginal spermicides in combination with barrier methods or an IUCD.

Ninety-eight women were entered into an open study of Staycept jelly (octoxynol 1% w/w) and Staycept pessaries (vaginal suppositories) (nonoxynol-9 6% w/w) in combination with other vaginal methods of contraception. Medical problems during use of either pessary or jelly were few and were restricted to genital irritation or increased vaginal discharge. This seemed more common with the pessaries than with the jelly, but this could have been related to the types of women entered. There were no unplanned pregnancies.

Contraceptive Devices, Female↗
PubMed1992

Virus inactivation of fresh frozen plasma by a solvent detergent procedure: biological results.

In order to increase the safety of blood products, we have developed a procedure for the virus inactivation of fresh frozen plasma. Several batches have been prepared and with the first 10 batches, each of them composed of 60 litres of plasma, we have determined a set of biological parameters. Virus inactivation was realised using TnBP (1%) and Octoxynol 9 (1%). After their elimination with castor oil using chromatography on insolubilized C18 resin, glycine was added and the pH of the plasma was adjusted to 7.4. Plastic bags were aseptically filled with a mean volume of 200 ml of plasma. The mean levels of coagulation factors were all over 0.7 U/ml and their recovery from initial plasma was nearly the same as total protein except for factor VIII:C. The net loss in factor VIII:C was 16%, when including the dilution of plasma. In vivo and in vitro tests demonstrated that in the final product there were no activated factors. As in fresh frozen plasma, the protein concentration was over 50 g/l and the potassium level lower than 5 mmol/l. According to these results, virus-inactivated plasma has the same qualities of fresh frozen plasma and could now replace it.

Blood Coagulation Factors↗
PubMed1977

Effect of symmetrical tetraalkylammonium salts on cloud point on nonionic surfactants.

The salting in and salting out of the nonionic surfactant octoxynol NF by halides of ammonium and the four lowest symmetrical tetraalkylammonium cations were investigated by measuring their effect on the cloud point at various salt concentrations. The chloride anion tended to salt the surfactant out, lowering its cloud point. The iodide anion tended to salt it in, raising the cloud point, while the bromide ion had no pronounced effect. The ammonium and tetramethylammonium cations tended to lower the cloud point, the latter more extensively than the former. The tetraethylammonium cation had no pronounced effect, while the tetra-n-propylammonium and tetra-n-butylammonium cations tended to raise the cloud point, the latter more extensively than the former. The salt effect on the cloud point generally increased with increasing salt concentration. Tetramethylammonium chloride was the most efficient salt in lowering the cloud point (by 4 degrees at the 0.10-molal level and by 20 degrees at the 1.00-molal level), while tetrabutylammonium halides were the most efficient salts in raising the cloud point (by 18-19 degrees at the 0.10-molal level for chloride and bromide). Cloud point increased were attributed to the formation of mixed micelles or to hydrotropy. The salting-out efficiency of tetramethylammonium chloride and bromide was ascribed to their ability to increase the structure of water.

Bromides↗
PubMed1983

Studies on spermicidal activity of surfactants. I. Correlation between spermicidal effect and physicochemical properties of p-menthanylphenyl polyoxyethylene (8.8) ether and related surfactants.

The spermicidal activities of seven nonionic surfactants against human spermatozoa were objectively determined by a statistical method, and two types of ionic surfactants were also studied for purposes of comparison. The nonionic surfactants, p-menthanylphenyl polyoxethylene adducts used in this work were synthesized from turpentine oil. These surfactants were used in the experiment after a careful confirmation of their chemical composition and molecular weight distribution. The spermicidal activities of the surfactants in terms of minimum concentrations to accomplish irreversible immobilization of all sperms in zero time was, in decreasing order, nonionic, cationic and anionic. When the most commonly used nonionics alone were considered, the sequence of decreasing spermicidal potency was isononylphenyl polyoxyethylene (9.0) ether (nonoxynol-9), p-menthanylphenyl polyoxyethylene (8.8) ether (menfegol), isooctylphenyl polyoxyethylene (9.0) ether (octoxynol-9). The surface tension and wetting time of these surfactants were determined with a view to finding physico-chemical measures of their spermicidal activity. In the statistical analysis regarding all the nine surfactants, there was a significant correlation (p less than 0.05) between spermicidal potency and critical micelle concentration (cmc) whereas there was no significant relationship between spermicidal potency and cmc regarding the seven nonionics. There was again no significant correlation between spermicidal potency and wetting time in all but nonionics with a common hydrophobic structure. As neither surface tension nor wetting time appeared to be a valid factor, general measure of spermicidal potency of nonionic surfactants, the partition ratios between n-octanol or n-hexane and water was determined. As a result, it was revealed that there was a significant correlation (p less than 0.05) between spermicidal potency and partition coefficient, when four types of nonionic surfactants with different hydrophobic group, which were chosen from among the seven nonionics, were tested with n-hexane. The close relationship between spermical activity and partition coefficient suggests that the spermicidal activities of these surfactants are associated with their structural affinity to the lipids of spermatozoal cell membrane.

Chemical Phenomena↗
PubMed1978

A reexamination of the potential comedogenicity of sulfur.

The present study was designed to reexamine the question of the potential comedogenicity of topical sulfur. Studies were done by two different investigators in two separate institutions with groups of 12 and 40 subjects, respectively. Biopsy specimens were obtained from the occluded test sites before and after a six-week period of treatment. Each subject received a patch test of 5% sulfur in either an octoxynol 9 (Triton X-100) or a carbomer 934P (Carbopol 934P) vehicle and one of two controls consisting of the Triton X-100 vehicle or a dry patch test. We conclude that no trend or correlation was noted between the presence or absence of sulfur in the formulation and the appearance of comedones. The Triton X-100 vehicle itself appeared to be comedogenic under the experimental conditions.

Acne Vulgaris↗
PubMedDate not supplied

Direct analysis of platinum in plasma and urine by electrothermal atomic absorption spectrophotometry.

An improved technique is described for analysis of platinum (Pt) concentrations in plasma and urine by electrothermal atomic absorption spectrophotometry (EAAS). The method is intended for use in therapeutic monitoring of cancer patients treated with platinum-containing antitumor drugs. Samples (0.1 ml) of plasma, urine, or Pt standards are diluted to two ml with a matrix solution that contains diammonium edetate, ammonium dihydrogen phosphate, ammonium hydroxide, and octoxynol detergent. Concentrations of Pt in the diluted samples are determined directly by EAAS analysis with Zeeman background correction. Standard additions are unnecessary; Pt concentrations are read from a calibration chart of peak heights, which is linear up to 1.6 mg per liter. The detection limit is 0.02 mg of Pt per liter. Day-to-day precision (coefficient of variation, based on 21 consecutive runs) ranges from 4.2 to 11.7 percent, depending upon the Pt concentration in the plasma and urine specimens. Recovery of Pt added to plasma and urine specimens averages 103 +/- 8 and 99 +/- 6 percent, respectively. Concentrations of Pt are stable in plasma and urine specimens stored at 4 degrees C or -20 degrees C for four weeks. Analyses of Pt concentrations in serial plasma and urine specimens from cancer patients receiving cisplatin chemotherapy demonstrate the clinical utility of the technique.

Cisplatin↗
PubMed1984

Interstitial 5'-nucleotidase stain for frozen biopsy specimens of skeletal muscle. A useful adjunct in the diagnosis of polymyositis.

We applied a simple lead salt-based stain for interstitial and vascular 5'-nucleotidase to 150 muscle biopsy specimens. No reaction was obtained with 2'- or 3'-adenosine monophosphate, indicating that the stain was specific, and distinct from phosphatases. Staining was not inhibited by alpha, beta-methylene adenosine 5'-diphosphate, but was prevented by formaldehyde fixation or by brief immersion in octoxynol 9 (Triton X-100). Nucleotidase stains the following specific histologic sites that distinguish it from alkaline phosphatase: the intima and adventitia of medium-sized and large arteries, perineural and muscle spindle sheaths, and tendon insertions. Aside from these structures, normal muscle shows little reaction, as the sarcoplasm and sarcolemma do not stain. Neither of these enzymes shows a compensatory increase, histochemically, in myo-adenylate deaminase deficiency. In Duchenne's muscular dystrophy, however, and particularly in inflammatory myopathy, interstitial staining of 5'-nucleotidase is increased, leading to investment of most muscle fibers in the affected area. The stain rarely identifies regenerating fibers. Although alkaline phosphatase commonly shows a corresponding increase in interstitial staining, we encountered six cases of inflammatory myopathy in which this was absent, despite pronounced endomysial staining in the 5'-nucleotidase reaction. 5'-Nucleotidase thus appears to provide a valuable adjunct in the diagnosis of inflammatory myopathy.

5'-Nucleotidase↗
PubMed1984

The use of specific antibodies to mediate fusion between Sendai virus envelopes and living cells.

Incubation of Sendai virus particles with non-ionic detergents such as Triton X-100 completely solubilizes the viral envelopes. Removal of the detergent from the supernatant (which contains the two main viral glycoproteins) leads to the formation of fusogenic, reconstituted viral envelopes. Soluble macromolecules such as DNA or proteins can be enclosed within the reconstituted vesicles, while membrane components can be inserted into the viral envelopes. Fusion of such loaded or 'hybrid' reconstituted envelopes with living cells in culture results in either microinjection or transfer of the viral components to the recipient cells. Thus such reconstituted envelopes can serve as efficient carriers for the introduction of macromolecules of biological interest into living cells in culture. A more specific vehicle has been constructed by chemically coupling anti-cell membrane antibodies (anti-human erythrocyte antibody) to the viral envelope. Such antibody-bearing intact virus particles or reconstituted envelopes bound to and fused with virus receptor-depleted cells. In addition, anti-Sendai virus antibodies were coupled to neuraminidase-treated human erythrocytes. Such antibodies mediated the binding and fusion of intact Sendai virus particles and their reconstituted envelopes to virus receptor-depleted cells.

Antibodies↗
PubMed1987

Presence of abundant filaments in apical caps of the nonciliated bronchiolar epithelial (Clara) cells.

The nonionic detergent Triton X-100 has often been used for the extraction of cytoplasmic materials. We used the detergent in a vascular perfusion medium when preparing rat lung in order to observe the cytoskeleton of the nonciliated bronchiolar epithelial (Clara) cells. To eliminate some cytoplasmic materials selectively and to maintain good fine cell structure simultaneously, the lungs were perfused sequentially with the detergent (0.2% Triton X-100) alone for 2 min, with a mixture of low-concentration (0.1%) glutaraldehyde and detergent (0.2% Triton X-100) for 15 min, and finally with 2.5% glutaraldehyde for 5-10 min. After fixation, the nonciliated bronchiolar epithelial (Clara) cells were observed by scanning and transmission electron microscopy. At the apical region of the cells, there were central cytoplasmic protuberances (apical caps) filled with microfilaments. These filaments were bound at one end to the cytoplasmic side of the cell membrane and ran into the interior of the cytoplasm at the other end. As a control, the Clara cells were observed by transmission electron microscopy after perfusion with 2.5% glutaraldehyde solution. The luminal surfaces of the cells were covered with short, thick microvilli. The apical caps also had microvillus-like protrusions. These results suggest that the apical cap is not an apocrine droplet but rather is a stable structure involved in the function of the Clara cells.

Actin Cytoskeleton↗