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PubMed1995

Superovulation of Holstein heifers by a single subcutaneous injection of FSH dissolved in polyvinylpyrrolidone.

This study was undertaken to determine whether a single injection of porcine FSH (pFSH) would induce a superovulatory response in cattle. Holstein heifers were given a single injection of pFSH (30 mg, s.c.) dissolved in saline (Group 1, n = 5); 50% polyvinylpyrrolidone (PVP; Group 2, n = 5); or 25% PVP (Group 3, n = 4). Group-4 heifers (n = 5) were given multiple intramuscular injections of pFSH every 12 h for 3 d at decreasing doses, for a total of 30 mg. All animals received a single injection of 750 microg PGF2 alpha 48 h after the initiation of pFSH treatment. Animals exhibiting estrus were artificially inseminated twice throughout estrus. Ova and embryos were recovered nonsurgically. Ovaries were examined by transrectal ultrasonography or by palpation per rectum on Day 7 or 8 of estrus. Plasma concentrations of pFSH, bovine FSH progesterone, estradiol-17 beta and inhibin were determined by specific radioimmunoassays. The number of corpora lutea (CL) and the numbers of total and transferable embryos which were detected and recovered in Groups 2 and 3 were equivalent to the numbers detected and recovered in Group 4. In Group 1, however, only 1 of 5 animals ovulated even a single oocyte. The present study demonstrated that only a single injection of pFSH dissolved in PVP was capable of inducing a superovulatory response by maintaining a high plasma FSH concentration to allow for the recovery of a sufficient number of embryos for transplantation.

Journal Article↗
PubMed1989

Spectroscopic study of the interaction of coumarin anticoagulant drugs with polyvinylpyrrolidone.

The interaction of coumarin anticoagulants with polyvinylpyrrolidone (PVP) was investigated using a fluorescence technique. The fluorescence intensities of warfarin and phenprocoumon were greatly enhanced following binding to PVP, while the fluorescence of 4-hydroxycoumarin was little enhanced in the presence of PVP. The enhanced fluorescence of warfarin and phenprocoumon bound to PVP can be explained by their incorporation into the hydrophobic environment in the PVP and by a decrease in the internal rotation of the alpha-substituted benzyl group in the drugs. The binding parameters of warfarin and phenprocoumon were estimated by the Klotz method; the binding constants for phenprocoumon and warfarin were found to be 2.6 X 10(4) and 2.2 X 10(4) M-1, respectively. The 13C-NMR measurements suggest the lactone moiety in the 4-hydroxycoumarin and the substituted benzene ring play an important role in the binding to PVP.

4-Hydroxycoumarins↗
PubMed1987

Radioprotection of sheep erythrocytes by polyvinylpyrrolidone.

The protective effect of polyvinylpyrrolidone of mol. wt 10,000 and 40,000, on sheep erythrocytes irradiated up to 13 kGy, and stored for one month at 4 degrees C was studied. Addition of these compounds at a level of 10-15% reduced hemolysis from 90% in irradiated erythrocyte solution to approximately 10%. The high efficiency of this protective agent is discussed.

Animals↗
PubMed2007

Separation of iron and cobalt using 59Fe and 60Co by dialysis of polyvinylpyrrolidone-metal complexes: a greener approach.

An environmentally benign method to separate iron and cobalt has been developed using a safe chemical, polyvinylpyrrolidone (PVP). The method involves dialysis of PVP-Fe and PVP-Co complexes against triple-distilled water. (59)Fe and (60)Co were used as radioactive tracers of iron and cobalt throughout the experiment. No other chemicals are required for clean separation of cobalt from iron. The optimum condition for separation has been obtained at pH 5 using 10% aqueous solution of PVP. The method is applicable from trace scale to macro-scale. Very high separation factors have been obtained.

Cobalt↗
PubMed2004

The targeting of anionized polyvinylpyrrolidone to the renal system.

We reported that the co-polymer composed of vinylpyrrolidone and maleic acid selectively distributed into the kidneys after i.v. injection. To further optimize the renal drug delivery system, we assessed the renal targeting capability of anionized polyvinylpyrrolidone (PVP) derivatives after intravenous administration in mice. The elimination of anionized PVP derivatives from the blood decreased with increasing anionic groups, and the clearance of carboxylated PVP and sulfonated PVP from the blood was almost similar. But carboxylated PVP efficiently accumulated in the kidney, whereas sulfonated PVP was rapidly excreted in the urine. The renal levels of carboxylated PVP were about five-fold higher than sulfonated PVP. Additionally, carboxylated PVP was effectively taken up by the renal proximal tubular epithelial cells in vivo after i.v. injection. These anionized PVP derivatives did not show any cytotoxicity against renal tubular cells and endothelial cells in vitro. Thus, these carboxylated and sulfonated PVPs may be useful polymeric carriers for drug delivery to the kidney and bladder, respectively.

Animals↗
PubMed2005

The resistance of polyvinylpyrrolidone-iodine-poly(-caprolactone) blends to adherence of Escherichia coli.

In this study, the resistance of biodegradable biomaterials, composed of blends of poly(-caprolactone) (PCL) and the polymeric antimicrobial complex, polyvinylpyrrolidone-iodine (PVP-I) to the adherence of a clinical isolate of Escherichia coli is described. Blends of PCL composed of a range of high (50,000 g mol(-1)) to low (5000 g mol(-1)) molecular weight ratios of polymer and either devoid of or containing PVP-I (1% w/w) were prepared by solvent evaporation. Following incubation (4 h), there was no relationship between m. wt. ratio of PCL in films devoid of PVP-I and adherence of E. coli. Conversely, microbial adherence to PCL containing PVP-I decreased as the ratio of high:low m. wt. polymer was decreased and was approximately 1000 fold lower than that to comparator films devoid of PVP-I. Following periods of immersion of PVP-I containing PCL films under sink conditions in phosphate buffered saline, subsequent adherence of E. coli was substantially reduced for 2 days (40:60 m. wt. ratio) and 6 days (100:0 m. wt. ratio). Concurrent exposure of PCL and E. coli to sub-minimum inhibitory concentrations (sub-MIC) of PVP-I significantly reduced microbial adherence to the biomaterial; however, the molecular weight ratio of PCL did not affect this outcome. Pretreatment of PCL with similar sub-MIC of PVP-I prior to inclusion within the microbial adherence assay significantly decreased the subsequent adherence of E. coli. Greatest reduction in adherence was observed following treatment of PCL (40:60 m. wt. ratio) with 0.0156% w/w PVP-I. In conclusion, this study has illustrated the utility of PVP-I as a suitable therapeutic agent for incorporation within PCL as a novel biomaterial. Due to the combined antimicrobial and biodegradable properties, these biomaterials offer a promising strategy for the reduction in medical device related infection.

Anti-Infective Agents, Local↗
PubMed2006

Ultra-low sized cross-linked polyvinylpyrrolidone nanoparticles as non-viral vectors for in vivo gene delivery.

In principle, the technique of gene delivery involves taking complete or parts of genes that can code specific message and delivering them to selected cells in the body. Such a transfer of plasmid DNA into mammalian cells has posed major challenges for gene therapy. This study shows the encapsulation of a plasmid DNA in cross-linked polyvinylpyrrolidone (PVP) nanoparticles of size less than 100 nm. This kind of encapsulation provides complete protection to the plasmid DNA from external DNase environment and generates the hope that the resulting formulation can be developed into a potential vector for effective gene delivery. In order to check this potentially, the reporter gene pSVbeta-gal was encapsulated and in vitro transfection efficiency of this system was found to be nearly 80% compared to the commercially available transfection reagent Polyfect. Further, in vivo biodistribution studies indicated that this system could be used safely for effective gene delivery.

Animals↗
PubMed2006

Chlorin e6-polyvinylpyrrolidone as a fluorescent marker for fluorescence diagnosis of human bladder cancer implanted on the chick chorioallantoic membrane model.

The use of fluorescence diagnosis as a modern cancer diagnostic modality is rapidly gaining importance in the field of urology. It is based on the detection of distinctive light emission of tissues sensitized by fluorescent dyes, commonly referred to as photosensitizers, after irradiation with a specific light source. Therefore, the search for specific fluorescent dyes with high sensitivity and specificity for bladder cancer is constantly being sought after. The aim of this study is to investigate the use of a new formulation consisting a mixture of chlorin e6 and polyvinylpyrrolidone (Ce6-PVP) for the detection of human bladder cancer cells (MGH) implanted on the chick chorioallantoic membrane (CAM) model. Uptake kinetics studies were quantitatively determined for both systemic and topical administrations of Ce6-PVP to the normal CAM as well as the MGH human bladder tumor implanted on CAM using fluorescence imaging technique. Rapid elimination of Ce6-PVP was displayed following topical application compared to systemic administration in the normal CAM system. Ce6-PVP was found to localize selectively in the xenografted bladder tumor in contrast to the CAM tissue. Neither dark toxicity nor irritancy was observed on the CAM tissue at the dose of 2 mg/kg Ce6-PVP. In conclusion, the Ce6-PVP formulation appeared to have the potential as a fluorescent marker for fluorescence diagnosis of human bladder cancer.

Animals↗
PubMed2006

Effect of hydrogen bonding interactions on the release mechanism of felodipine from nanodispersions with polyvinylpyrrolidone.

Solid dispersion systems are widely investigated for the dissolution enhancement of poorly water soluble drugs. Nevertheless, very limited commercial use has been achieved due to the poor predictability of such systems caused by the lack of a basic understanding of the dissolution optimization mechanism. In the present study an investigation of the release mechanism is performed for solid dispersion systems composed by polyvinylpyrrolidone (PVP) and felodipine (FEL), based on a correlation of their hydrophilicity with the intensity of interactions. The existing interactions were evaluated by using NMR and UV spectroscopy while molecular simulation techniques were also enabled. It was found that the interactions that take place correspond to the creation of hydrogen bonds. The correlation between the intensity of interactions and the concentration of PVP in the matrix showed a sigmoid function. The interactions are impressively increased for polymer concentration exceeding 75% (w/w). This phenomenon was well explained by using the molecular simulation technique. A similar sigmoid pattern was found for the function between dissolution profiles and polymer concentration in the matrix, indicating that the intensity of interactions promotes the dissolution enhancement. Investigation of the solubility and the particle size distribution of FEL in the binary system appeared to have similar behaviour indicating that the interactions affect the release profile through these two factors. The hydrophilicity of PVP does not significantly affect this enhancement as the contact angle was found to be linear to PVP concentration. Microscopic observation of the dissolution behaviour showed that FEL remains in fine dispersion in aqueous solution, verifying the release mechanism.

Felodipine↗
PubMed2006

Evaluation of the clinical behaviour of a polyvinylpyrrolidone and sodium hyalonurate gel (Gelclair) in patients subjected to surgical treatment with CO2 laser.

This experimental study was undertaken to evaluate the efficacy of Gelclair, a concentrated oral gel consisting of sodium hyalonurate and polyvinylpyrrolidone, in decreasing postoperative pain in patients subjected to surgical treatment by extirpation and/or vapourization of oral lesions with CO(2) laser. After the surgery, 60 consecutive patients (30 in control group and 30 in experimental group) were prescribed 600 mg ibuprofen 3 times per day for 4 days. In the experimental group a protocol was established for the application of 15 ml of Gelclair directly onto the wound 3 times per day, 1 h before meals, for 1 week. Spontaneous pain and pain on swallowing were evaluated using a visual analogue scale at 24 h and 7 days after the intervention. The experimental group had less spontaneous pain at 24h (P=0.000) and at 1 week (P=0.012), and also less pain on swallowing at 24 h and 1 week (P=0.029 and P=0.000, respectively) after the intervention. In conclusion, the effectiveness of the barrier mechanism that Gelclair provides improves the postoperative experience of patients who have undergone oral CO(2) laser surgery.

Administration, Oral↗
PubMed2006

HyperDSC studies of amorphous polyvinylpyrrolidone in a model wet granulation system.

Measurements of the properties of amorphous materials are very important to help in the understanding of how materials behave during manufacture, storage and use of medicines. However, there are few methods that are suited to the study of amorphous materials, especially if in multi-component systems or model formulations. The goal here was to explore the potential for the use of HyperDSC to study a model granulation system. It was found that the sensitivity of HyperDSC was such that the glass transition (Tg) of polyvinylpyrrolidone (PVP) could be detected in granules made with realistic levels of this binder. The measured Tg in the granules, even after drying, was very different to that of PVP alone and to PVP in physical mixtures with lactose. It is argued that the granulation process has resulted in the dissolution of some lactose and that the amorphous binder holding the granules together is in fact a solid dispersion of PVP and lactose. Based on the standard Gordon-Taylor equation it was estimated that the solid dispersion contained 50% of PVP and lactose. Given that solid dispersions have a tendency to crystallise on storage, it could be expected that changes in the binder properties will occur with time after granulation. We believe that this is the first measurement of in situ properties of a binder in this way and opens the possibility of studies on formulated systems.

Calorimetry, Differential Scanning↗
PubMed2004

Polyvinylpyrrolidone-drug conjugate: synthesis and release mechanism.

Covalent conjugates of polyvinylpyrrolidone (PVP) with para-nitroaniline (PNA) were synthesized as a model PVP-drug conjugate, and PNA release was evaluated in vitro. Pyrrolidone ring opening with subsequent t-BOC protection of the pyrrolidone nitrogen and reaction with PNA in methylene chloride (CH2Cl2) produced a PVP-PNA conjugate with 3% of the pyrrolidone groups modified. Rates of PNA release from N-deprotected conjugates were twofold greater than those that were N-protected, indicating participation of the pyrrolidone N in release. Additional studies with monomeric analogs supported intramolecular base catalysis rather than lactam formation as the mechanism of this involvement. The approach serves as a prototype for the conjugation of other drugs with primary and secondary amine functional groups with PVP, including peptides and proteins.

Chemistry, Pharmaceutical↗
PubMed2004

Determination of polyvinylpyrrolidone using high-performance liquid chromatography.

Polyvinylpyrrolidone (PVP) is a versatile polymer with innate surface activity. It is very difficult to accurately assay due to its wide molecular weight range and amphiphilic nature. This study evaluated a reversed-phase HPLC method to separate and quantify PVP K15. The assay used a Hicrome C18 150 mm x 3 microm HPLC column in combination with an 80/20 propanol-1-ol: deionised water, 0.01% TFA mobile phase, which resolved the polymer as a single peak, tR = 10.69+/-0.17 min (n=120) at 243 nm. The column's performance was constant throughout the study, N (theoretical plates) = 1729+/-22 and the peak symmetry remained good (As ranged from 0.74 to 0.92, n=10 over the calibration range). The developed assay proved to be accurate, sensitive and capable of recovering PVP K15 from pharmaceutical formulations. The limits of quantification and detection were calculated statistically as 2.40 and 0.72 mg ml(-1), respectively. Assay reproducibility assessed at five concentrations gave an average coefficient of variance <3.5% and the accuracy of the analytical method was 102.62+/-2.04%. The recovery of PVP K15 from directly compressed tablets and Refresh eye drops was 98.02+/-2.73 and 108.35+/-6.52%, respectively.

Chromatography, High Pressure Liquid↗
PubMed2004

Effect of binary and ternary polyvinylpyrrolidone and/or hydroxypropyl-beta-cyclodextrin complexes on the photochemical and photosensitizing properties of Naproxen.

The effect of the polyvinylpyrrolidone and/or hydroxypropyl-beta-cyclodextrin on the photo-lability of aqueous solutions of the anti-inflammatory drug Naproxen was studied. Kinetic studies revealed that the presence of all of these additives reduced drug photodegradation. In all cases, the presence of the different additives elicited a change in the photomixture composition, being the alcoholic derivative the major photoproduct formed. Nevertheless, the change in the efficiency of the process and the amount of the photoproducts formed in the different systems were not related with the biodamage produced by the drug. In this sense, the presence of free Naproxen clearly sensitized the photoperoxidation of linoleic acid. The photosensitizing effect decreased as the PVP concentration increased. Different protection provides the binary (Naproxen:HP-beta-CD) and ternary (Naproxen:HP-beta-CD:PVP) complexes. The binary complex formation had not effect on the prevention of photooxidation of linoleic acid sensitized by the drug, whereas the ternary complex formation suppresses the drug effect. The different behaviour observed with beta-CD and HP-beta-CD and the structural differences of both cyclodextrins seem to indicate that in the case of the HP-beta-CD the linoleic binds with the CD and takes contact with the drug. These results confirm that in these systems the prevention of biodamage would be due to a decrease in the contact between the short-lived species generated during Naproxen photodegradation and biological structures, rather than due to the nature or amount of the photoproducts. In addition, the ability of the complex to interact with the biological structure depends on the structure of both interacting species.

2-Hydroxypropyl-beta-cyclodextrin↗
PubMed2006

Fluorescence imaging and phototoxicity effects of new formulation of chlorin e6-polyvinylpyrrolidone.

Evaluations of the efficiency of a new formulation of chlorin consisting of a complex of trisodium salt chlorin e6 (Ce6) and polyvinylpyrrolidone (PVP) in photodynamic therapy (PDT) and fluorescence diagnosis was performed on poorly differentiated human bladder carcinoma murine model with the following specific aims: (i) to qualitatively evaluate the fluorescence accumulation in human bladder tumor, (ii) to determine fluorescence distribution of Ce6-PVP using the tissue extraction technique and fluorescence imaging technique, (iii) to compare the fluorescence distribution of Ce6, Ce6-PVP and Photofrin in skin of nude mice, and (iv) to investigate phototoxicity caused by different parameters (drug-light interval, drug dose, irradiation fluence rate and total light fluence) in PDT. The fluorescence of the Ce6-PVP formulation was determined either by fluorescence imaging measurements or by chemical extraction from the tissues displaying similar trends of distribution. Our results demonstrated that the Ce6-PVP formulation possesses less in vivo phototoxic effect compared to Ce6 alone. The phototoxicity revealed a strong dependence on the drug and light dosimetry as well as on the drug-light interval. In PDT, the Ce6-PVP compound was most toxic at the 1h drug-light interval at 200J/cm(2), while Ce6 alone was most toxic at a light dose of more that 50J/cm(2) at the 1 and 3h drug-light interval. We also confirmed that Ce6-PVP has a faster clearance compared to Ce6 alone or Photofrin. This eliminates the need for long-term photosensitivity precautions. In conclusion, the Ce6-PVP formulation seems to be a promising photosensitizer for fluorescence imaging as well as for photodynamic treatment.

Animals↗
PubMed2003

Induction of apoptosis and cell cycle arrest by polyvinylpyrrolidone K-30 and protective effect of alpha-tocopherol.

Polyvinylpyrrolidone is a macromolecular polymer with widespread use in industry as well as in medicine for various purposes. Its effect on cells cultured in vitro, however, has not been fully investigated. To elucidate this issue, we studied the influence of PVP K-30 on cultured HeLa cells. PVP K-30 treatment produced a dose- and time-dependent toxicity to HeLa cells. Cells exposed to PVP K-30 exhibited several morphological features of apoptosis. Gel electrophoresis of DNA from PVP K-30-treated cells showed typical apoptotic ladder. And flow cytometric analysis demonstrated that PVP K-30 induced cell cycle arrest at G2/M phase and the subsequent appearance of sub-G1 population. In addition, it was shown that procaspase-3 was activated in response to PVP K-30 treatment. We also found that alpha-tocopherol efficiently protected HeLa cells from PVP K-30 cytotoxicity. This is the first demonstration that PVP K-30 could induce apoptosis in HeLa cells and cell cycle arrest at G2/M phase, and that PVP K-30 toxicity could be attenuated by alpha-tocopherol.

Apoptosis↗
PubMed1976

Permeability of artificial membranes to a pluridisperse solution of 125I-polyvinylpyrrolidone.

The validity of the transport equation for uncharged macromolecules across a porous membrane developed by Verniory et al. (1973, J. Gen. Physiol. 62:489) has been tested on several types of artificial membranes (Amicon PM-30, XM-50, and XM-100 Diaflo ultrafilters) using a pluridisperse solution of polyvinylpyrrolidone as filtrand. The influence of the filtration pressure on the shape of the sieving curve predicted by the theory has been verified. A mean pore radius and the width of the pore demonstrated that the method used previously to determine the effective filtration pressure in the glomerulus from sieving data is valid. The transport equation previously proposed by Renkin (1954, J. Gen. Physiol. 38:225) gives results that are less consistent than those obtained with the new transport equation.

Iodine Radioisotopes↗
PubMed1984

Anomalous diffusion of erythrocytes in the presence of polyvinylpyrrolidone.

The diffusion coefficient of erythrocytes was measured using quasi-elastic light-scattering (QELS) techniques. The cells were suspended in phosphate-buffered saline solutions with and without a macromolecule, polyvinylpyrrolidone (PVP[360]). In the presence of the PVP(360) an anomalously high diffusion coefficient was measured for metabolizing cells with a normal transmembrane potential. The results are in agreement with experiments on rouleau formation by red blood cells and are supportive of the hypothesis of a long-range coherent interaction between metabolically active biological cells.

Cell Movement↗