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PubMed1985

Antifertility effect of polyvinylpyrrolidone-gossypol and gossypol in male rats.

Thirty-nine adult male Wistar rats were administered 20 mg/kg or 24.3 mg/kg polyvinylpyrrolidone-gossypol (PVP-G) and 20 mg/kg gossypol acetic acid (G-A) 6 times a week for 6 weeks. Mating test was taken to evaluate the antifertility effect. Caudal sperm count, body weight, sex and accessory sex organ weights were recorded. At the end of 6 weeks treatment, the recovery period of 6 weeks was investigated. The results showed that the onset of antifertility action and recovery with PVP-G are faster than with G-A.

Animals↗

PubMed1997

Vaginal delivery of new formulations of nonoxynol-9 coprecipitated with polyvinylpyrrolidone in rabbits. Comparisons between two formulation delivery systems.

The objective of this study was to assess the efficacy of two formulation delivery systems (FDS) in preventing the onset of pregnancy in rabbits. Nonoxynol-9 (N-9) was coprecipitated with polyvinylpyrrolidone (PVP), which yields PVP/ N-9, and prepared as capsules or tablets. Semen specimens were collected (from eight male rabbits), pooled, and used for in vitro spermicidal assessment or artificial insemination (AI). In vitro spermicidal assessment was performed by introducing and mixing the FDS containing PVP or PVP/N-9 with 1.0 mL of semen, followed by incubation at 37 degrees C for 6 h. Semen samples were taken at various time intervals to determine killing of spermatozoa and dissolution of the FDS. The efficacy of the FDS in preventing the onset of pregnancy was assessed by inserting the FDS vaginally. The does were artificially inseminated at 0, 0.5, and 6 h after insertion of the FDS vaginally. The number of pregnant does and newborn rabbits was recorded. In the in vitro spermicidal trial, semen specimens exposed to both FDS containing PVP/N-9 were killed within 10 to 15 min of incubation. Tablets containing PVP only or PVP/N-9 dissolved completely after 3 h of incubation. However, capsules did not dissolve completely by 6 h of incubation. The results obtained in the in vivo trial showed that both FDS exhibited some variations in preventing the onset of pregnancy over the various time intervals following the insertion of tablets or capsules and AI. The tablet seemed to be a more efficient delivery system than the capsule, yielding significantly lower pregnancy rates at all three time intervals assessed. The tablet FDS, as applied in this study, was found to be the most efficient mode of delivery of the tested spermicidal formulations.

Administration, Intravaginal↗

PubMed1979

Temporary sterility induced by intrascrotal deposition of silastic-polyvinylpyrrolidone-prostaglandin F2alpha tubes in the rabbit: effect on fetal survival after regain of fertility.

In male rabbits of proven fertility, the intrascrotal deposition of two Silastic-polyvinylpyrrolidone tubes containing 3 mg of prostaglandin F2alpha (PGF2alpha)/tube induced within 2 to 4 weeks temporary sterility which lasted for 10 to 14 weeks. Associated with induced sterility were reduction in testicular weight, increase in abnormal spermatozoa (8% to 78% versus 0 to 3.7%), and reduction in sperm motility along the reproductive tract and in the semen for a period of 6 to 7 weeks. During the period of temporary sterility the weight of the epididymis, the sexual drive, and semen volume remained unaltered. Normal fertility was associated with an increase in testicular weight, reduction in the proportion of abnormal sperm, and improved sperm motility. In addition to an altered spermatogenesis, the integrity of mature spermatozoa seemed to be severely affected after PGF2alpha treatment. The reduced number of viable young sired by males that recovered from temporary sterility (pregnancy wastage 35%) as compared with sham-treated controls (pregnancy wastage 3%) suggests that a small percentage of spermatozoa might still be defective at the time of testing. A longer waiting period might be needed to ensure a completely normal reproductive process.

Animals↗

PubMed1976

Separation of polycyclic aromatic hydrocarbons by liquid chromatography on cross-linked polyvinylpyrrolidone.

Polycyclic aromatic hydrocarbons (PAHs) can be separated by liquid chromatography on cross-linked polyvinylpyrrolidone (PVP) stationary phase using a polar solvent as eluent. The order of elution is determined primarily by the number of condensed aromatic rings Efficient separations were obtained with a column packed with 63-90 mum particles of PVP and isopropanol as eluent. Capacity factors (k') ranged from 0.3-10 for PAHS having from one to five aromatic rings, and theoretical plate heights were between 0.3 and 0.5 mm. This technique is being used to assist in the characterization of products from coal liquifaction processes.

Chromatography, Liquid↗

PubMed2003

Cross-linked polyvinylpyrrolidone nanoparticles: a potential carrier for hydrophilic drugs.

Injectable hydrogel polymeric nanoparticles of polyvinylpyrrolidone cross-linked with N,N'-methylene bis-acrylamide and encapsulating water-soluble macromolecules such as FITC-dextran (FITC-Dx) have been prepared in the aqueous cores of reverse micellar droplets. These particles are 100 nm and below in diameter with a narrow size distribution. When dispersed in aqueous buffer these particles appear to be transparent and give an optically clear solution. Lyophilized powder of these nanoparticles is redispersable in aqueous buffer without any change in the size and morphology of the particles. The efficiency of FITC-Dx entrapment by these nanoparticles is high (>70%) and depends on the amount of cross-linking agent present in the polymeric material. The release of the entrapped molecules from these nanoparticles depends on the degree of cross-linking of the polymer, particle size, pH of the medium, and extent of loading, as well as temperature.

Colloids↗

PubMed1989

EDTA-polyvinylpyrrolidone as a preservation medium for immunohistochemistry.

In a solution on 7% EDTA and 5% polyvinylpyrrolidone in 0.1 mol/l. Tris buffer, pH = 6.95, tissues samples can be stored at room temperature for 1 week without detectable loss of structural integrity or antigenicity (as demonstrated in immunohistochemistry with monoclonal antibodies to intermediate filament proteins).

Biomarkers, Tumor↗

PubMed2004

Nanoscopic behavior of polyvinylpyrrolidone particles on polysulfone/polyvinylpyrrolidone film.

We revealed morphology and physicochemical behavior of a widely used powerful hydrophilizing agent, polyvinylpyrrolidone (PVP), present on polysulfone (PS)/PVP films by atomic force microscopy (AFM). This is the first time such clear PS/PVP phase-separated morphology was observed by nanoscopic technique. The film surfaces were observed by the identical observation mode, probe and scanning conditions to reveal the change of PVP morphology and behavior between dry and wet conditions. Morphology was related to biocompatibility by combining AFM data with results of surface element composition, contact angle, adhesion amount of rabbit platelet and relative amount of adsorbed fibrinogen. PVP nano-particles of one or several molecules were formed on the dry PS/PVP film surfaces. Amount of PVP present on the surfaces increased with the molecular weight of PVP. At a mixed amount of 1-5 wt%, PVP K90 formed crowded particles on the dry surface. When wet, they swelled, followed by their union to produce a smooth surface leading to improved biocompatibility. The highest biocompatibility with excellent mechanical strength is achieved by blending the highest molecular weight PVP K90 at 1-5 wt%.

Adsorption↗

PubMed2000

Molecular design of polyvinylpyrrolidone-conjugated interleukin-6 for enhancement of in vivo thrombopoietic activity in mice.

Functional polyvinylpyrrolidone (PVP) was synthesized as a novel polymeric modifier for polymer-conjugated cytokines, and its efficiency and applicability as a drug delivery system (DDS) were evaluated. PVP with a carboxyl group at one end of the main chain was prepared by radical polymerization (M(n): 6000, M(w)/M(n): 1.14) with the aid of 4,4'-azobis(4-cyanovaleric acid) as a radical initiator and 3-mercaptopropionic acid as a transfer agent. Interleukin-6 (IL-6) was covalently conjugated via the formation of amino bonds between the lysine amino groups of IL-6 and PVP. PVP-conjugated IL-6, in which 60% of the fourteen lysine amino groups of IL-6 were estimated to be coupled with PVP (M-PVP-IL-6), showed more than 50-fold greater thrombopoietic potency in vivo than native IL-6. No side effects, such as body weight loss, were observed in the M-PVP-IL-6 treated mice. These results indicate that PVP as a polymeric modifier is a promising DDS for clinical application of cytokines and other therapeutic agents.

Animals↗

PubMed2001

An investigation of pulsatile release tablets with ethylcellulose and Eudragit L as film coating materials and cross-linked polyvinylpyrrolidone in the core tablets.

To develop new pulsatile release tablets, which can suppress drug release in stomach and release the drug rapidly after a predetermined lag time of about 3 h in intestine, the use of tablets with ethylcellulose/Eudragit L as a coating film and cross-linked polyvinylpyrrolidone in the core tablets was investigated. The release of diltiazem hydrochloride (DIL) as a model drug in the core tablets was investigated in vitro. The lag time (t10) was prolonged with an increase of the coating level, whereas the drug release rate was almost constant, irrespective of the coating level. The water-uptake study and electron microscope photographs suggested the mechanism of pulsatile release of drug. Pulsatile release tablets containing 60 mg DIL with 4.4 h of lag time (t10) in vitro were administrated to eight volunteers. The mean plasma concentration curves showed 4.9 h of lag time (tlag), 8.0 h of time to maximum concentration (tmax) and 3.1 h of time between tmax and tlag (t(psi)) in vivo. Relative bioavailability was 1.05 for pulsatile release tablets compared to conventional tablets.

Adult↗

PubMed1993

'Mucoid dissolution' of bones and multiple pathologic fractures in a patient with past history of intravenous administration of polyvinylpyrrolidone (PVP). A case report.

Polyvinylpyrrolidone (PVP) has been used in industry as well as in medicine for various purposes, e.g. as a component of hair-sprays, 'retardant' for subcutaneous injections, and given intravenously as a plasma expander. The latter usage results in deposition of PVP in the reticulo-endothelial system and other mesenchymal cells, including osteocytes. A middle aged woman in Taiwan, who for 10 years received repeated intravenous injections of PVP, suffered pathologic fractures of both femora and her right humerus with additional destructive lesions seen radiologically in other bones. Biopsies of the fracture sites showed both intracellular PVP deposits and mucoid changes in the involved cells, a characteristic secondary complication of PVP deposition. This phenomenon, if of sufficient severity, may cause, as in this case, a virtual 'melting down' of osseous tissue with pathological fractures as a consequence.

Bone and Bones↗

PubMed1985

Studies of hepatic tolerance of polyvinylpyrrolidone in the rat.

Intraperitoneal polyvinylpyrrolidone in amounts much larger than used in povidone-iodine for peritonitis or for adhesion prophylaxis was administered to rats. No adverse effects on hepatic reticulo-endothelial function could be detected using dynamic hepatic scintigraphy and fewer histochemical changes occurred than expected.

Animals↗

PubMed2001

Superovulation in ewes by a single injection of pFSH dissolved in polyvinylpyrrolidone (PVP): effects of PVP molecular weight, concentration and schedule of treatment.

Three experiments were carried out to evaluate induction in ewes of superovulation and embryo production by a single injection of a porcine pituitary extract (pFSH) dissolved in polyvinylpyrrolidone (PVP), investigating the effects of PVP molecular weight and its concentration (Experiment I), time and method of treatment (Experiments II and III). All ewes were synchronized for estrus by vaginal sponges impregnated with fluorogestone acetate (FGA; 30 mg, 9 days) plus PGF(2alpha) (Cloprostenol, 50 microg, 48h before sponge removal - s.r.), and superovulated by 250 IU pFSH. In Experiment I, 60 Gentile di Puglia ewes were subdivided into five experimental groups (n = 12): Group A, the control, received six decreasing intramuscular (i.m.) doses of pFSH, 12 h apart, beginning 48h before s.r.; Groups B and C were given 48 h before s.r. a single i.m. injection of pFSH dissolved in PVP with MW = 10,000, respectively, at concentrations of 15 and 30% w/v; Groups D and E received the same treatments as for B and C using PVP with MW = 40,000. None of the pFSH-PVP treatments were effective in inducing superovulation. In Experiment II, 22 Leccese ewes were subdivided into two groups (n = 11): Group A, control received i.m. four decreasing doses of pFSH, beginning 24 h before s.r., 12h apart; Group B was given a single i.m. injection of pFSH dissolved in PVP (MW = 40,000 at 30% w/v), 24 h before s.r. The pFSH-PVP treatment provided an ovulation rate similar to the control and tended to enhance embryo yield (4.4 versus 2.4, P>0.05). In Experiment III, 60 Leccese ewes were subdivided into six treatment groups (n = 10). Groups A and D served as controls and received i.m. 12 h apart, six doses (from 48 h before s.r.) and four doses (from 24h before s.r.) of pFSH, respectively. Groups B and C were treated by a single injection of pFSH in PVP (MW = 10,000; 30% w/v) 48 h before s.r., respectively by i.m. or subcutaneous (s.c.) administration. Groups E and F received the same treatments as for B and C 24 h before s.r. Intramuscular pFSH-PVP administration 24 h before s.r. provided an ovulation rate (8.1), mean numbers of ova recovered (5.6) and fertilized (4.2) comparable to the six or four dose treatments and significantly higher (P <0.01) compared to the pFSH-PVP treatment carried out i.m. 48 h before s.r. These results show that a single injection of pFSH dissolved in PVP at 30% w/v, performed i.m. 24 h before s.r., is able to induce a superovulatory response comparable to that following multiple injection treatment, regardless of PVP molecular weight.

Animals↗

PubMed1999

Superovulation induction in Japanese Black cattle by a single intramuscular injection of hMG or FSH dissolved in polyvinylpyrrolidone.

The efficacy of a single intramuscular dose of 450 or 600 international units (IU) of human menopausal gonadotropin (hMG) or 30 mg of follicle stimulating hormone (FSH), each dissolved in 30% polyvinylpyrrolidone K-30 (PVP), for superovulation treatment was compared to that of superovulation induction by administration of a total dose of 600 IU hMG given in declining doses twice daily over a 3-day period. A total of 48 Japanese Black cows were used for the investigation. Oestrus was observed within 60 h after PGF2alpha administration in all cows in the hMG groups. In the hMG group that received a single dose of 600 IU hMG (n = 12), oestrus was observed less than 36 h after treatment in one cow. In contrast, oestrus was not observed in 3 of the 12 cows (25%) in the FSH group. Neither the average number of recovered ova/embryos nor the number of transferable embryos per collection differed significantly among the hMG groups. However, the average number of transferable embryos was not significantly higher in cows treated with a single dose of 600 IU of hMG than in cows treated with a single 30 mg dose of FSH (7.5+/-4.5 vs. 2.1+/-2.8). The number of cows from which more than three excellent grade embryos were collected was highest in the group that received a single dose of 600 IU hMG (9/12, 75%) and lowest in the group that received a single 30 mg dose of FSH (2/9, 22%). The differences between groups in the percentages of cows with three or more excellent embryos between treatments were not statistically significant. The proportion of recovered ova/embryos classified as excellent was highest in the group that received 600 IU hMG in declining doses and lowest in the group that received a single 30 mg dose of FSH (55.2% vs. 30.2%; P < 0.05). The recovery rate of unfertilized ova was lowest in the group that received a single dose of 600 IU hMG and highest in the group received a single 30 mg dose of FSH (18.3% vs. 48.8%; P < 0.05). Although the differences in recovery results between the groups were not statistically significant, the recovery rates in hMG groups were higher than that the FSH group. These findings suggest that superovulation can be induced adequately in Japanese Black cows using one injection of 450 to 600 IU hMG dissolved in PVP.

Animals↗

PubMed2001

Effects of molecular weight of polyvinylpyrrolidone on the glass transition and crystallization of co-lyophilized sucrose.

The purpose of the present study was to investigate the effects of molecular weight (MW) of polyvinylpyrrolidone (PVP) on glass transition and crystallization of sucrose. Thus, sucrose was co-lyophilized with 2.5 and 5.0% w/w PVP of different molecular weights, which were characterized using gel permeation chromatography. Freeze drying was carried out for 48 h at a shelf temperature of -40 degrees C and a pressure of about 36 Pa. The samples were then dried in a vacuum oven at 24 degrees C for 12 h before drying for a further 12 h at 40 degrees C. Differential scanning calorimetry (DSC) was employed to measure the glass transition temperature (Tg), dynamic crystallization temperature (Tc) and isothermal crystallization induction time (tc) at 85 degrees C of sucrose. Isothermal water vapour sorption of each sample was also measured at different relative humidities. Tg values of sucrose varied from 48.3+/-0.8 degrees C for freeze-dried (FD) sucrose alone to 58.8+/-0.8 degrees C for the mixture containing 5.0% PVP of nominal MW 300 K. PVP increased sucrose T(g) significantly (ANOVA P<0.05). Although there was no significant difference (P>0.05) in Tg of the mixtures containing 2.5% w/w PVP of different MW, samples with 5.0% PVP of MW 300 K produced a significantly higher (P<0.05) Tg than the other mixtures. All mixtures were shown to possess higher (P<0.01) Tc than FD sucrose alone, which exhibited a T(c) of approximately 85 degrees C. PVP of MW 300 K consistently induced a significantly (P<0.05) higher Tc of sucrose than PVP of smaller MW. Increasing PVP concentration from 2.5 to 5.0% also resulted in a substantial increase in sucrose Tc. Using isothermal water vapour absorption, sucrose tc was found to increase up to over 10 times when it was co-lyophilized with 2.5% PVP, the actual value of tc being dependent upon the MW of the PVP. For example, PVP of MW 300 K resulted in a sucrose tc at 85 degrees C (89.1-95.6 min), which was approximately seven times higher than that of 2.5% PVP of MW 24 or 40 K. A longer tc of sucrose was also observed for mixtures containing PVP of MW 300 K than when sucrose was mixed with PVP of smaller MW. Thus the effect of PVP on sucrose Tg, Tc and tc was found to be dependent upon MW. PVP of higher MW was more efficient in inhibiting sucrose crystallization and by stabilizing glassy structures of the sugar, these polymers may improve the stability of co-lyophilized proteins and peptides.

Calorimetry, Differential Scanning↗

PubMed2001

Dissolution properties and anticonvulsant activity of phenytoin-polyethylene glycol 6000 and -polyvinylpyrrolidone K-30 solid dispersions.

Solid dispersions of phenytoin in polyethylene glycol 6000 and polyvinylpyrrolidone K-30 with different drug-to-carrier ratios were prepared by the solvent method with the aim of increasing dissolution rate and bioavailability of the drug. These new formulations were characterized in the solid state by FT-IR spectroscopy, X-ray powder diffraction, and differential scanning calorimetry. Drug solubility and dissolution rate are improved by these formulations, particularly with SDPEG 1/20 and SDPVP 1/20 systems. Storage was found to influence the stability of the solid dispersions. By maximal electroshock test, it was found that the intraperitoneal administration in mice of the SDPEG 1/20 and SDPVP 1/20 systems exhibited anticonvulsant activity similar to diphenylhydantoin sodium salt.

Animals↗

PubMed2002

Influence of polyvinylpyrrolidone on aggregation propensity of coated spheroids.

The influence of polyvinylpyrrolidone (PVP), a commonly used binder and adhesive, on the aggregation of spheroids coated with hydroxypropylmethylcellulose (HPMC) was studied. The aggregation propensities of spheroids coated by HPMC alone and by HPMC with polyethylene glycol (PEG) were compared with those coated by HPMC with PVP and the viscosity of the coating solutions determined. The coating was conducted at a maximum spray rate of 11 g/min to avoid premature termination of the coating process at higher spray rates due to uncontrollable aggregation of spheroids. PVP was able to reduce the extent of aggregation of spheroids. It was more effective in reducing spheroid aggregation than PEG. The reduction in spheroid aggregation propensity was ascribed to viscosity lowering effects of PVP. The viscosity of the coating solutions determined over the temperature range of 28-58 degrees C was found to increase in the following order: HPMC-PVP<HPMC-PEG<HPMC.

Excipients↗

PubMed2002

Effect of moisture on polyvinylpyrrolidone in accelerated stability testing.

Accelerated stability studies are a common approach for predicting the long-term stability of pharmaceutical formulations. However, in this study, a slowing of dissolution was observed for a formulation following storage at elevated temperature and humidity. The moisture sorption isotherm for the binder, polyvinylpyrrolidone (PVP), shows absorption of a significant quantity of water on exposure to elevated humidity. Modulated temperature differential scanning calorimetry (mDSC) has been used to demonstrate that moisture uptake will depress the glass transition temperature (Tg) of PVP to the conditions used in accelerated stability studies. Exposure to elevated temperature and humidity resulted in a change in the PVP from the glassy to the rubbery state. This conversion produces a change in the dissolution profile. Long-term stability studies conducted at temperatures and humidities below the Tg, would not have induced this change.

Cellulose↗

PubMed2003

Comparison between polyvinylpyrrolidone and silica nanoparticles as carriers for indomethacin in a solid state dispersion.

States of interaction between indomethacin (IM) and polyvinylpyrrolidone (PVP) in an amorphous solid dispersion prepared by co-grinding were compared with those between IM and silica nanoparticles. Changes in the carbon chemical states of the solid dispersions were evaluated based on the chemical shift in the 13C-CP/MAS-NMR. Hydrogen bonds between the amide carbonyl of PVP particles and the carboxyl groups of IM molecules were formed by co-grinding. Despite the wide difference in carrier properties, the apparent equilibrium solubility (AES) of IM in the ground IM-PVP mixture was predicted by solid state NMR on the basis of the relationship previously established for IM with SiO(2). This indicates that AES is affected solely by the state of IM, irrespective of the carrier species, and despite carrier-dependent chemical interactions.

Drug Carriers↗