scholarly journals Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation

Antioxidants ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 86 ◽  
Author(s):  
Kengo Banshoya ◽  
Tetsuya Nakamura ◽  
Tetsuro Tanaka ◽  
Yoshiharu Kaneo
Keyword(s):  
Polyethylene Glycol ◽  
Coenzyme Q10 ◽  
Blood Circulation ◽  
Oxidant Stress ◽  
Aqueous Media ◽  
Molecular Size ◽  
Water Soluble ◽  
Scattering Method ◽  
Dynamic Light Scattering Method

Therapeutic applications of coenzyme Q10 (CoQ10) are greatly limited by its lack of solubility in aqueous media. In this study, polyethylene glycol monostearate (stPEG) was used to construct micelles containing CoQ10 as a new formulation. The micellar formulations (stPEG/CoQ10) were prepared using five types of stPEG with 10, 25, 40, 55, and 140 PEG repeat units, respectively. The micellar preparation was simple, consisting of only stPEG and CoQ10. Next, we compared the physical properties and blood circulation of these micelles. The CoQ10 load of this formulation was approximately 15 w/w%. Based on the dynamic light scattering method, the average molecular size of the stPEG/CoQ10 micelles was approximately 15 to 60 nm. The zeta potentials of these micelles were approximately −10 to −25 mV. The micelles using stPEG25, 40, and 55 demonstrated high solubility in water. Furthermore, these micelles had in vitro antioxidant activity. On comparing the blood circulation of micelles using stPEG25, 40, 55, and 140, micelles using stPEG55 had a significantly higher circulation in blood. The stPEG55/CoQ10 micelle demonstrated a protective effect against acetaminophen-induced liver injury in mice. In conclusion, these data indicate that the intravenous administration of the stPEG/CoQ10 micellar aqueous formulation is of great value against oxidant stress.

scholarly journals DEVELOPMENT AND IN VITRO DISSOLUTION STUDY OF BINARY AND TERNARY SOLID DISPERSIONS OF ACECLOFENAC

2019 ◽  
Author(s):  
Md. Shahidul Islam ◽  
Rasheda Akter Lucky
Keyword(s):  
Polyethylene Glycol ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 6000

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.

The Myospherulotic Potential of Water-Soluble Ointments

1995 ◽  
Vol 9 (4) ◽  
pp. 215-218 ◽  
Author(s):  
David F. Moore ◽  
James B. Grogan ◽  
William H. Lindsey ◽  
Vinod K. Anand ◽  
Charles W. Gross
Keyword(s):  
Polyethylene Glycol ◽  
Paranasal Sinus ◽  
In Vitro Model ◽  
Water Soluble ◽  
Sinus Surgery ◽  
Inflammatory Condition ◽  
Paranasal Sinus Surgery ◽  
Vitro Model

Myospherulosis is a submucosal inflammatory condition that has been linked to the use of petrolatum-based ointment in the sinus cavities of patients after paranasal sinus surgery. To avoid this problem, several investigators have suggested using water-soluble ointments. Polyethylene glycol, a vehicle commonly used for water miscible ointments, has not been examined previously with regard to its potential to cause a myospherulotic lesion. Using an in vitro model, we confirmed the potential of petrolatum ointment to produce the myospherulotic lesion and examined the myospherulotic potential of polyethylene glycol ointment.

scholarly journals Selection of Water-Soluble Chitosan by Microwave-Assisted Degradation and pH-Controlled Precipitation

Polymers ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 1274 ◽  
Author(s):  
Céline M. A. Journot ◽  
Laura Nicolle ◽  
Yann Lavanchy ◽  
Sandrine Gerber-Lemaire
Keyword(s):  
Molecular Weight ◽  
Average Molecular Weight ◽  
Aqueous Media ◽  
Phase Changes ◽  
Water Soluble ◽  
In Vivo Evaluation ◽  
Microwave Assisted ◽  
Selection Of

In the field of gene therapy, chitosan (CS) gained interest for its promise as a non-viral DNA vector. However, commercial sources of CS lack precise characterization and do not generally reach sufficient solubility in aqueous media for in vitro and in vivo evaluation. As low molecular weight CS showed improved solubility, we investigated the process of CS depolymerization by acidic hydrolysis, using either long time heating at 80 °C or short time microwave-enhanced heating. The resulting depolymerized chitosan (dCS) were analyzed by gel permeation chromatography (GPC) and 1H nuclear magnetic resonance (NMR) to determine their average molecular weight (Mn, Mp and Mw), polydispersity index (PD) and degree of deacetylation (DD). We emphasized the production of water-soluble CS (solubility > 5 mg/mL), obtained in reproducible yield and characteristics, and suitable for downstream functionalization. Optimal microwave-assisted conditions provided dCS with a molecular weight (MW) = 12.6 ± 0.6 kDa, PD = 1.41 ± 0.05 and DD = 85%. While almost never discussed in the literature, we observed the partial post-production aggregation of dCS when exposed to phase changes (from liquid to solid). Repeated cycles of freezing/thawing allowed the selection of dCS fractions which were exempt of crystalline particles formation upon solubilization from frozen samples.

Reliable size determination of nanoparticles using dynamic light scattering method for in vitro toxicology assessment

2009 ◽  
Vol 23 (5) ◽  
pp. 927-934 ◽  
Author(s):  
Haruhisa Kato ◽  
Mie Suzuki ◽  
Katsuhide Fujita ◽  
Masanori Horie ◽  
Shigehisa Endoh ◽  
...  
Keyword(s):  
Light Scattering ◽  
Dynamic Light Scattering ◽  
Scattering Method ◽  
Size Determination ◽  
In Vitro Toxicology ◽  
Dynamic Light Scattering Method ◽  
Toxicology Assessment

Combined conservation of jack bean and velvet bean with sorghum: evaluation of lab-scale silages and in vitro assessment of their nutritive value

2014 ◽  
Vol 152 (6) ◽  
pp. 967-980 ◽  
Author(s):  
R. LIMA-OROZCO ◽  
I. VAN DAELE ◽  
U. ÁLVAREZ-HERNÁNDEZ ◽  
V. FIEVEZ
Keyword(s):  
Polyethylene Glycol ◽  
Nutritive Value ◽  
Water Soluble ◽  
Mucuna Pruriens ◽  
Soluble Carbohydrates ◽  
Velvet Bean ◽  
Jack Bean ◽  
Tropical Conditions ◽  
Silage Quality

SUMMARYThe potential of ensiled sorghum–soybean as a ruminant feed has already been demonstrated; however, alternatives for soybean should be considered because other legumes such as jack bean (JB; Canavalia ensiformis (L.) DC.) and velvet bean (VB; Mucuna pruriens (L.) DC) might produce better yields under tropical conditions. First, the possibility for a qualitative conservation of these legumes in combination with sorghum was studied using lab-scale silages. Furthermore, the potential of additional molasses as a source of water-soluble carbohydrates (WSC) and a microbial inoculant (BIOPRANAL) to improve silage quality were assessed. As sorghum or legume tannins may influence the silage nutritive value, their importance was assessed through the addition of polyethylene glycol (PEG), which reduces tannin activity. Therefore, 25 treatments per legume–sorghum combination were created according to a central composite design. An acceptable silage quality was reached when at least half of the fresh biomass consisted of sorghum in combination with at least 15 g of additional WSC/kg fresh material. The nutritive value of mixed silages as well as pure sorghum silage in combination with dry jack beans was determined through in vitro digestibility in the rumen and small intestine. Polyethylene glycol increased the in vitro production of short-chain fatty acids, ammonia (NH3) concentrations and effective rumen dry matter and crude protein degradability for both mixed silages, indicating that tannins reduced rumen degradability. The latter action could be positive as the amount of digestible bypass protein increased when no PEG was added in the silo. Propionate and valerate proportions were increased through PEG addition to sorghum–JB and sorghum–VB silages, respectively, suggesting that the nature of the tannins differ between these legumes.

Bioactivity of Fibrous Polymer Based Nanocomposites for Application in Regenerative Medicine

2012 ◽  
Vol 714 ◽  
pp. 229-236 ◽  
Author(s):  
Ewa Stodolak-Zych ◽  
Aleksander Góra ◽  
Łukasz Zych ◽  
Magdalena Szumera
Keyword(s):  
Electron Microscopy ◽  
Thermal Analysis ◽  
Scattering Method ◽  
Dynamic Light Scattering Method ◽  
Nanocomposite Polymer ◽  
Transmission Electron ◽  
Electrospinning Method ◽  
Fibrous Polymer ◽  
Scanning Electron

Aim of the work was production of nanocomposite polymer fibres containing ceramic particles using the electrospinning method and characterisation of morphology and bioactivity of the produced materials. The first stage of investigations consisted in preparation of a series of poly-L-lactide (PLA) solutions in various solvents mixtures in order to reach viscosity which would allow formation of fibres by the electrospinning method. Ceramic nanoparticles such as tricalcium phosphate (TCP) and silica (SiO2) were used as nanofillers of the polymer matrix. Their particle size distribution in the solvent solution as well as in the polymer suspension was determined by dynamic light scattering method (DLS). Morphology of the nanoparticles was observed using transmission electron microscopy (TEM). Distribution of the nanofillers in the nanocomposite fibres as well as diameter and morphology of the fibres was assessed using scanning electron microscopy with energy dispersive spectroscopy method (SEM/EDS). Effect of the nanofillers addition and the shaping method on the structure of the PLA matrix was investigated on the basis of the thermal analysis methods (TG/DSC) on the nanocomposite foils prepared by casting. It was revealed that the nanocomposite fibres showed apatite nucleation inin vitroconditions i.e. after incubation in SBF (37°C/ 3 days).

scholarly journals Cat Heart Muscle in Vitro

1962 ◽  
Vol 46 (2) ◽  
pp. 201-213 ◽  
Author(s):  
Ernest Page
Keyword(s):  
Molecular Size ◽  
Water Soluble ◽  
Osmotic Gradient ◽  
Papillary Muscles ◽  
Total Water ◽  
Inulin Space ◽  
Soluble Molecule ◽  
Cat Heart ◽  
Molecular Radius

The "osmotic gradient" method, an intracellular microelectrode technique for determining whether an uncharged, water-soluble molecule enters cells or remains extracellular, is described. Using this method, a series of carbohydrates of graded molecular size were examined. In cat papillary muscles mannitol, molecular radius 4.0 Å, remained extracellular while arabinose, molecular radius 3.5 Å entered the cells. Measurement of the simultaneous uptake of H3-mannitol and C14-inulin showed that mannitol equilibrates with 40 per cent of total water in 1 hour, after which the mannitol space does not further increase. By contrast, inulin, molecular radius ∼15 Å, equilibrates with 24 per cent of total water in 1 hour; thereafter the inulin space continues to increase very slowly. The intracellular K concentrations are significantly higher and the intracellular Na and Cl concentrations significantly lower when mannitol rather than inulin is used to measure the extracellular space. The intracellular Cl concentration determined with Cl36 or Br82 is significantly higher than that calculated from the membrane potential assuming a passive Cl distribution. In addition, it is shown that choline enters and is probably metabolized by the cells of papillary muscle.

DEVELOPMENT OF SOLID DISPERSION TABLET OF CARVEDILOL TO IMPROVE SOLUBILITY

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 54-59
Author(s):  
S. S Shelake ◽  
◽  
R. G Gaikwad ◽  
S Patil ◽  
F. I. Mevekari ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Media ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Water Soluble Drugs ◽  
Ft Ir

Crystalline state compounds are typically dissolution rate limited and dissolution rate is directly proportional to the solubility for BCS class II or class IV compounds. Solid dispersions are one of the most promising strategies to improve the oral bioavailability poorly water soluble drugs. The purpose of this study was to increase solubility of carvedilol by solid dispersion (SDs) technique with Poloxamer (PXM) 407 in aqueous media. The carvedilol- PXM 407 solid dispersion was prepared by solvent evaporation, kneading and melting method. It was characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), Fourier transformation infra-red spectroscopy (FT-IR), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared solid dispersion were found to have higher dissolution rates as compared to intact carvedilol. During formulation of solid dispersion crystalline to amorphous transition has been observed.

scholarly journals Synthesis and anti-cancer activities of a water soluble gold(III) porphyrin

2015 ◽  
Vol 19 (01-03) ◽  
pp. 398-403 ◽  
Author(s):  
Aaron D. Lammer ◽  
Melissa E. Cook ◽  
Jonathan L. Sessler
Keyword(s):  
Anticancer Agents ◽  
Ovarian Cancer Cell ◽  
Ovarian Cancer Cell Line ◽  
Aqueous Media ◽  
Cancer Cell Line ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Physiological Conditions ◽  
Anti Cancer

Gold(III) compounds continue to be explored for their potential utility as anticancer agents. A recognized limitation is the reactivity of gold(III), which is typically reduced to the more labile gold(I) state under physiological conditions. The use of porphyrins can overcome this problem. However, to date the stabilization provided by the use a strongly chelating porphyrin is offset by the poor solubility of the resulting complex in aqueous media. In this work, we describe the synthesis and in vitro anti-cancer activity of a gold(III)porphyrin complex with relatively good aqueous solubility. As judged from standard antiproliferation assays, this complex displays an IC50 of 9 μM for the A2780 human ovarian cancer cell line. This is a higher level of potency than displayed by two related control systems.

scholarly journals IN VITRO DISSOLUTION STUDY OF GLIMEPIRIDE FROM BINARY AND TERNARY SOLID DISPERSION FORMULATION

2019 ◽  
Author(s):  
Sharmin Akhter ◽  
Md. Sajjad Hossen ◽  
Md. Salahuddin ◽  
Muazzem Ahmed Sunny ◽  
Farzana Akther Sathi ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Peer Review ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 4000 ◽  
Ternary Solid Dispersion ◽  
E Mail

Glimepiride (GMP) is poorly water soluble drug, so solubility is the main constraint for its oral bioavailability. Because, poor aqueous solubility and slow dissolution rate of the glimepiride lead to irreproducible clinical response or therapeutic failure in some cases due to sub therapeutic plasma drug levels. In this study, binary and ternary solid dispersion of glimepiride were prepared with polyethylene glycol 6000 (PEG 6000) and polyethylene glycol 4000 (PEG 4000) at different weight ratios using the solvent evaporation and melting method. It was found the drug was released 0.46% after 5 minutes and only 15.83% within 60 minutes from active glimepiride on the other hand the release pattern of glimepiride from the binary formulation containing PEG 4000 in 1:5 (Formulation coding: G5) showed the best result. It was found that the ternary different SD formulation containing(PEG4000:Glimepiride:Povidone) In ratio 1:1:0.25 (Formulation coding were : G13) showed the best result. The drug was changed to amorphous form after solid dispersion. Itwas also evident that solid dispersions improve solubility of drug particles thus enhancing dissolution characteristics of drugs they increase the oral bioavailability. Peer Review History: UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file Average Peer review marks at initial stage: 4.5/10 Average Peer review marks at publication stage: 7.5/10 Reviewer(s) detail: Name: Dr. Mohammed Abdel-Wahab Sayed Abourehab  Affiliation: Umm Al-Qura University;  Makkah Al-Mukarramah, Saudi Arabia E-mail: [email protected]   Name: Dr. Evren Alğin Yapar Affiliation: Turkish Medicines and Medical Devices Agency, Turkiye E-mail: [email protected] Comments of reviewer(s):

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