Association efficiency of three ionic forms of oxytetracycline to cationic and anionic oil-in-water nanoemulsions analyzed by diafiltration.

Abstract:

:The association efficiency of oxytetracycline (OTC) to pharmaceutical available, ionic oil-in-water nanoemulsions is studied. Theoretical mathematical developments allowed us to differentiate by diafiltration (DF) between thermodynamically and kinetically controlled binding of the drug to the nanoemulsions, and relate these important magnitudes to the association efficiency. The nanoemulsions have been prepared by the solvent displacement technique in the presence of cationic and anionic surfactants. The resulting nanoemulsions were stable at 4°C and 25°C for 60 days, have a size of ∼ 200 nm, showing polydispersity indexes ranging between 0.11 and 0.23, and present zeta potentials ranging between -90 and +60 mV, depending on the charge of the surfactants used. The zeta potential of the nanoemulsions influenced the interaction with OTC, having three ionic forms at different pH, namely, cationic, zwitterionic, and anionic. DF proved to be a powerful tool for the quantification of the drug association efficiency, achieving values up to 84%. Furthermore, this technique allowed obtaining different values of the drug fractions reversibly bound (11%-57%) and irreversibly bound (10%-40%) to the nanoemulsions depending on the surfactants used and pH. These findings may be useful for the development of new drug delivery systems, and as routine assays in academia and pharmaceutical industries.

journal_name

J Pharm Sci

authors

Orellana SL,Torres-Gallegos C,Araya-Hermosilla R,Oyarzun-Ampuero F,Moreno-Villoslada I

doi

10.1002/jps.24255

subject

Has Abstract

pub_date

2015-03-01 00:00:00

pages

1141-52

issue

3

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(16)30036-3

journal_volume

104

pub_type

杂志文章
  • Establishment of a Drug-Induced, Bile Acid-Dependent Hepatotoxicity Model Using HepaRG Cells.

    abstract::Bile acid (BA) retention within hepatocytes is an underlying mechanism of cholestatic drug-induced liver injury (DILI). We previously developed an assay using sandwich-cultured human hepatocytes (SCHHs) to evaluate drug-induced hepatocyte toxicity accompanying intracellular BA accumulation. However, due to shortcoming...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.01.013

    authors: Susukida T,Sekine S,Nozaki M,Tokizono M,Oizumi K,Horie T,Ito K

    更新日期:2016-04-01 00:00:00

  • In vivo and in vitro evaluation of a microencapsulated narcotic antagonist.

    abstract::Injectable microcapsules containing 75% (w/w) cyclazocine, a narcotic antagonist, were prepared with dl-poly(lactic acid) as the coating material. Capsule fractions falling between 105 and 295 mum released about 90% of their cyclazocine in 8 days of rotating-bottle extraction at 37 degrees in pH 7.4 phosphate buffer. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650612

    authors: Mason N,Thies C,Cicero TJ

    更新日期:1976-06-01 00:00:00

  • Kinetics of chlorambucil hydrolysis using high-pressure liquid chromatography.

    abstract::A stability-specific high-pressure liquid chromatographic (HPLC) method was developed to assay intact chlorambucil (I) in the presence of its hydrolytic decomposition products. The HPLC method was used to follow the degradation kinetics of I over pH 1.0-10.0 in the presence of various buffers with and without added ch...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710113

    authors: Chatterji DC,Yeager RL,Gallelli JF

    更新日期:1982-01-01 00:00:00

  • Transport in quantitative structure-activity relationships. VI: Relationship between transport rate constants and partition coefficients.

    abstract::The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700930

    authors: van de Waterbeemd H,van Bakel P,Jansen A

    更新日期:1981-09-01 00:00:00

  • High-performance liquid chromatographic determination of (Z)- and (E)-doxepin hydrochloride isomers.

    abstract::A high-performance liquid chromatographic method for the determination of (Z)- and (E)-doxepin hydrochloride isomers was developed. The analysis employs a column packed with spherical silica microparticles (5-6 mum), and a mobile phase of acetonitrile-chloroform-diethylamine (750:250:0.2) permits baseline resolution a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600681133

    authors: Whall TJ,Dokladalova J

    更新日期:1979-11-01 00:00:00

  • Drying rates of tablet granulations II: effect of particle size and granular densities.

    abstract::The effects of the granule size and density on the drying rate kinetics of tablet granulations were studied using lactose and sulfathiazole granules prepared with acacia mucilage and providone solution. The drying rate kinetics consisted of three distinct phases of drying when the drying rate was platted against remai...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600640631

    authors: Opankunle WO,Bhutani BR,Bhatia VN

    更新日期:1975-06-01 00:00:00

  • Fetal and maternal placental and nonplacental clearances of metoclopramide in chronically instrumented pregnant sheep.

    abstract::The placental and nonplacental clearances of metoclopramide were studied in nine chronically instrumented, near-term pregnant sheep using a two-compartment open model. Metoclopramide was administered to the ewe and fetus on separate occasions as an initial iv bolus loading dose followed by a constant-rate infusion, wi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600791204

    authors: Riggs KW,Rurak DW,Taylor SM,McErlane BA,McMorland GH,Axelson JE

    更新日期:1990-12-01 00:00:00

  • Sustained release of isomazole from matrix tablets administered to dogs.

    abstract::Isomazole matrix tablet formulations, with various concentrations of hydroxypropyl methylcellulose (HPMC) hydrogel, were prepared and tested for sustained-release activity. Sustained-release activity was determined by administering isomazole test formulations orally to conscious dogs, instrumented with an indwelling l...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600780715

    authors: Wilson HC,Cuff GW

    更新日期:1989-07-01 00:00:00

  • Species difference in GI motor response to somatostatin.

    abstract::Acute experiments were performed on overnight fasted chloralose-urethan anesthetized dogs, cats, rabbits, and rats. Under these conditions, somatostatin practically abolished gastric contractions and decreased GI tonus in all species examined. The canine duodenum, jejunum, and ileum exhibited only a contractile respon...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680913

    authors: Tansy MF,Martin JS,Landin WE,Kendall FM

    更新日期:1979-09-01 00:00:00

  • Bioavailability of generic ritonavir and lopinavir/ritonavir tablet products in a dog model.

    abstract::In this study, we explored the bioavailability in dogs and chemical potency of generic ritonavir and lopinavir/ritonavir tablet products manufactured by various pharmaceutical companies. Chemical potency of the products was examined by HPLC quantitation of ritonavir and lopinavir. Using a dog model, we determined poin...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21712

    authors: Garren KW,Rahim S,Marsh K,Morris JB

    更新日期:2010-02-01 00:00:00

  • Drug delivery trends in clinical trials and translational medicine: Updated analysis of ClinicalTrials.gov database.

    abstract::While the number of clinical trials has continued to grow by about 20% in the past six months, no corresponding growth in product approval by the food and drug administration is seen or anticipated in the near future. Late-stage clinical failures due to lack of efficacy or toxicity continues to be a challenge. The opt...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21649

    authors: Ho RJ,Chien JY

    更新日期:2009-06-01 00:00:00

  • A novel multivariate approach for estimating the degree of similarity in bioavailability between two pharmaceutical products.

    abstract::Statistical assessment of bioavailability and bioequivalence of drug products is generally carried out with a univariate analysis by independently comparing each relevant parameter [such as, area under the drug concentration curve (AUC) and peak drug concentration (Cmax)] of the test and reference products. The assump...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600840620

    authors: Hsu HC,Lu HL,Chan KK

    更新日期:1995-06-01 00:00:00

  • Determination of propylene carbonate in pharmaceutical formulations using liquid chromatography.

    abstract::A stability-indicating reversed-phase high-performance liquid chromatographic method using a refractive index detector is described for the determination of propylene carbonate in pharmaceutical formulations. Good precision and accuracy of the method was demonstrated using an aqueous formulation. This method is also a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740626

    authors: Cheng H,Gadde RR

    更新日期:1985-06-01 00:00:00

  • Do multidrug resistance-associated protein-1 and -2 play any role in the elimination of estradiol-17 beta-glucuronide and 2,4-dinitrophenyl-S-glutathione across the blood-cerebrospinal fluid barrier?

    abstract::The purpose of this study was to examine the role of multidrug resistance-associated protein-1 and -2 (Mrp1 and Mrp2) in the efflux transport of organic anions across the blood-cerebrospinal fluid (CSF) barrier. The CSF concentration of estradiol-17beta-glucuronide (E(2)17betaG) and 2,4-dinitrophenyl-S-glutathione (DN...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10521

    authors: Lee YJ,Kusuhara H,Sugiyama Y

    更新日期:2004-01-01 00:00:00

  • Structural characterization and aging of glassy pharmaceuticals made using acoustic levitation.

    abstract::Here, we report the structural characterization of several amorphous drugs made using the method of quenching molten droplets suspended in an acoustic levitator. (13) C NMR, X-ray, and neutron diffraction results are discussed for glassy cinnarizine, carbamazepine, miconazole nitrate, probucol, and clotrimazole. The (...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23464

    authors: Benmore CJ,Weber JK,Tailor AN,Cherry BR,Yarger JL,Mou Q,Weber W,Neuefeind J,Byrn SR

    更新日期:2013-04-01 00:00:00

  • Crystal structures of azathioprine dihydrate and 6-methylmercaptopurine trihydrate.

    abstract::The crystal and molecular structures of 6-methylmercaptopurine trihydrate and of azathioprine dihydrate were determined by the use of three-dimensional, X-ray, diffractometer data and were refined by least squares. Both molecules crystallize in the N(9)-H tautomer form, in contrast to the N(7)-H tautomer form found in...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600640206

    authors: Cook WJ,Bugg CE

    更新日期:1975-02-01 00:00:00

  • Limits on optimizing ocular drug delivery.

    abstract::The problem of optimizing ocular bioavailability of topically applied ophthalmic drugs is discussed. A formula for drug concentration in the tear film is derived using well-known pharmacokinetic relationships and a first-order drug decay model for the tear film. The time integral of the tear film concentration is then...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600800113

    authors: Keister JC,Cooper ER,Missel PJ,Lang JC,Hager DF

    更新日期:1991-01-01 00:00:00

  • Isomerization of ceftibuten in aqueous solution.

    abstract::The isomerization reactions of ceftibuten and ceftibuten-related compounds in aqueous solution were investigated to estimate the substitution effect on the isomerization reaction and identify the three proximal dissociation constants of ceftibuten kinetically from the pH-rate profiles. The isomerization reaction of ce...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js980048z

    authors: Hashimoto N,Hirano K

    更新日期:1998-09-01 00:00:00

  • The physical stability of the recombinant tuberculosis fusion antigens h1 and h56.

    abstract::The recombinant fusion proteins hybrid 1 [H1 (Ag85B-ESAT-6)] and hybrid 56 [H56 (Ag85B-ESAT-6-Rv2660c)] derived from Mycobacterium tuberculosis are promising antigens for subunit vaccines against tuberculosis. Both antigens are early batches of antigens to be enrolled in human clinical trials and it is therefore impor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23669

    authors: Hamborg M,Kramer R,Schanté CE,Agger EM,Christensen D,Jorgensen L,Foged C,Middaugh CR

    更新日期:2013-10-01 00:00:00

  • Liquid chromatographic determination of 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one in human plasma with fluorescence detection.

    abstract::A simple and sensitive assay for quantitating 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one (1; BMY 26517) in human plasma was developed using high-performance liquid chromatography with fluorescence detection. The method involves precipitation of protein and reversed-phase chromatography. The method i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600761216

    authors: Cheng H,Pittman KA,Dandekar KA

    更新日期:1987-12-01 00:00:00

  • Amino acid analogs IV:4-fluoroisoleucine.

    abstract::4-Fluoroisoleucine was produced by ammonolysis of 2-bromo-4-fluoro-3-methylpentanoic acid, which resulted from the bromofluorination of 4-methyl-2-pentenoic acid. It did not inhibit Plasmodium berghei in mice at 640 mg/kg and was not toxic to the animals. The fluoroamino acid inhibited Aspergillus niger, Trichoderma v...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670542

    authors: Gershon H,Shanks L,Clarke DD

    更新日期:1978-05-01 00:00:00

  • Indolizines II: search for potential oral hypoglycemic agents.

    abstract::A few 1,2-bis(N-alkylaminomethyl)indolizines, simple indolizinecarboxylic acids, and several 6-alkoxyindolizine-2-carboxylic acids were synthesized and screened as possible oral hypoglycemic agents. The absence of any significant hypoglycemic activity excludes these compounds from the predicted structural lead provide...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:

    authors: De AU,Saha BP

    更新日期:1975-02-01 00:00:00

  • Cholesterol-mediated activation of P-glycoprotein: distinct effects on basal and drug-induced ATPase activities.

    abstract::Cholesterol promotes basal and verapamil-induced ATPase activity of P-glycoprotein (P-gp). We investigated whether these effects are related to each other and to the impact of the sterol on bilayer fluidity and verapamil membrane affinity. P-gp was reconstituted in egg-phosphatidylcholine (PhC) liposomes with or witho...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21558

    authors: Belli S,Elsener PM,Wunderli-Allenspach H,Krämer SD

    更新日期:2009-05-01 00:00:00

  • Secondary antithyroid action of drugs in relation to structure.

    abstract::Molecular interactions between iodine and disulfiram, clomethiazole, and tolnaftate were investigated by electron spectroscopy. Iodine forms charge transfer complexes with these molecules, with 1:1 stoichiometry and of the n-sigma type. The formation constants were compared with those obtained with antithyroid molecul...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600731205

    authors: Buxeraud J,Absil AC,Raby C

    更新日期:1984-12-01 00:00:00

  • Autoxidation of tetrazepam in tablets: prediction of degradation impurities from the oxidative behavior in solution.

    abstract::The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are 7-chloro-5-(1,2-epoxy...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810216

    authors: Boccardi G,Deleuze C,Gachon M,Palmisano G,Vergnaud JP

    更新日期:1992-02-01 00:00:00

  • Application of a Best Practice Approach Using Resonant Mass Measurement for Biotherapeutic Product Characterization.

    abstract::Characterizing and quantifying subvisible particles in protein drug products is critical to ensuring product quality. A variety of analytical methods are used to detect and make meaningful measurements of subvisible particles. Resonant mass measurement (RMM) is a novel technology that characterizes the subvisible part...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.12.017

    authors: Krueger AB,Hadley J,Cheney PP,Markova N,Carpenter JF,Fradkin AH

    更新日期:2019-05-01 00:00:00

  • Incidence of experimental fascioliasis on hepatic disposition of [3H]tetracycline and [14C]rafoxanide in rats.

    abstract::[7-3H]Tetracycline and [carbonyl-14C]rafoxanide were injected intravenously into anesthetized controls and rats in which experimental fascioliasis had been induced by 20 Fasciola hepatica metacercariae. The biliary excretion (1 and 3 h, respectively) of the radioactivity consisted of approximately 4% of the administer...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740921

    authors: Galtier P,Larrieu G,Franc M

    更新日期:1985-09-01 00:00:00

  • Indolizine derivatives with biological activity IV: 3-(2-Aminoethyl)-2-methylindolizine, 3-(2-aminoethyl)-2-methyl-5,6,7,8-tetrahydroindolizine, and their N-alkyl derivatives.

    abstract::In a continuing search for new biologically active agents derived from indolizine, 3-(2-aminoethyl)-2-methylindolizine, 3-(2-aminoethyl)-2-methyl-5,6,7,8-tetrahydroindolizine, and some mono- and di-N-substituted derivatives were prepared. Initial pharmacological screening showed that these compounds possess anti-5-hyd...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680317

    authors: Antonini I,Claudi F,Gulini U,Micossi L,Venturi F

    更新日期:1979-03-01 00:00:00

  • Brain delivery of proteins by the intranasal route of administration: a comparison of cationic liposomes versus aqueous solution formulations.

    abstract::The goal of this research was to evaluate the effectiveness of cationic liposomes for intranasal administration of proteins to the brain. Cationic liposomes were loaded with a model protein, ovalbumin (OVAL), and a 50 microg dose was administered intranasally to rats. In qualitative studies, liposomes were loaded with...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21939

    authors: Migliore MM,Vyas TK,Campbell RB,Amiji MM,Waszczak BL

    更新日期:2010-04-01 00:00:00

  • Sensitive electron-capture GLC determination of metoclopramide in biological fluids.

    abstract::A highly sensitive and specific electron-capture GLC assay capable of detecting picogram quantities of metoclopramide, a procaine derivative, in biological fluids was developed. This assay consisted of extracting metoclopramide from an alkalinized aqueous layer into benzene. A portion of the organic phase was derivati...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670813

    authors: Tam YK,Axelson JE

    更新日期:1978-08-01 00:00:00