Removal Efficiency of Insoluble β-Cyclodextrin Polymer from Water-Soluble Carcinogenic Direct Azo Dyes.

A batch system was applied to study the adsorption of three dyes (methyl violet, eriochrom black T and helianthin) from aqueous solution onto β-cyclodextrin polymer, synthesized by using citric acid as a cross linking agent. This polymer lets to adsorb only methyl violet for this effect, several operator variables was checked only with this kind of dye, the removal efficiently increases with increase in adsorbent amount; elevation of temperature lets also to improve the dye adsorption; ionic strength has not effect on dye adsorption process, for the pH we have remarked a slight decrease in removal efficiently with increasing of pH values. Equilibrium study was investigated by applying three models (Langumir, Frendlich and Temkin), results show that Langumir isotherm is the appropriate model.

Effect of Autoclaving on the Physicochemical Properties and Biological Activity of Aluminum Oxyhydroxide Used as an Adjuvant in Vaccines.

The long-term biodistribution of non-biodegradable microstructures or nanostructures used in vaccinations is widely unknown. This is the case for aluminum oxyhydroxide, the most widely used vaccine adjuvant, which is a nanocrystalline compound that spontaneously forms nanoprecipitates. Although generally well-tolerated, aluminum oxyhydroxide is detected in macrophages a long time after vaccination in individuals predisposed to the development of systemic and neurological aspects of the autoimmune (inflammatory) syndrome induced by modified adjuvant.

Development and validation of HPLC method for simultaneous quantification of alpha-tocopherol (free or encapsulated) and cholesterol in semen cryopreservation media.

The HPLC method was developed and validated for assaying alpha-tocopherol and cholesterol in cryopreservation media. Chromatographic separation was performed on an isocratic system, using a C-18 column. The mobile phase was composed of a mixture of methanol:acetonitrile:water 68:28:4 (v/v/v), using a flow rate of 1.

New Formulation and Evaluation of Camptothecin Encapsulated and/or Dispersed Suppository.

Background: Camptothecin is known for its potent anticancer activity. However, its optimal activity is reduced due to its low solubility and stability in biological media.

Objective: The aim of the present study is to design and characterize a Camptothecin (CPT) suppository formulation.

Syndromic Surveillance of Acute Gastroenteritis Using the French Health Insurance Database: Discriminatory Algorithm and Drug Prescription Practices Evaluations.

The French national public health agency (Santé publique France) has used data from the national health insurance reimbursement system (SNDS) to identify medicalised acute gastroenteritis (mAGE) for more than 10 years. This paper presents the method developed to evaluate this system: performance and characteristics of the discriminatory algorithm, portability in mainland and overseas French departments, and verification of the mAGE database updating process. Pharmacy surveys with certified mAGE from 2012 to 2015 were used to characterise mAGE and to estimate the sensitivity and predictive positive value (PPV) of the algorithm.

New Polymer Inclusion Membrane Containing β-Cyclodextrin Polymer: Application for Pharmaceutical Pollutant Removal from Waste Water.

We present herein the preparation of novel polymer inclusion membranes (PIMs) containing insoluble β-CD polymer as a carrier, polyvinyl chloride as a base polymer, and dibuthylphtalate (DBP) as a plasticizer in varying proportions. The prepared PIMs can be obtained by a simple, fast, and high-yield preparation process. Physicochemical characterizations of such membranes occurred in a homogeneous structure.

Enhanced Dissolution and Oral Bioavailability of Cyclosporine A: Microspheres Based on αβ-Cyclodextrins Polymers.

Cyclosporine (CsA) has a selective property of suppressing various T-lymphocyte functions. This is of utmost importance in preventing allograft rejection by several organ transplantations, as well as in the treatment of systemic and local autoimmune disorders. However, the poor water solubility of CsA can be a major hurdle for its absorption into the blood stream, which leads to low bioavailability and thus less efficacy.

Preparation and Characterization of Spherical Amorphous Solid Dispersion with Amphotericin B.

In the present study, new polymer microspheres of amphotericin B (AmB) were prepared by a spray drying technique using cyclodextrin polymers (Poly-CD) to improve the solubility and dissolution of AmB, to prevent in vivo toxic AmB aggregations. Formulations were characterized through scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), thermal analysis, Raman spectroscopy, particle size, drug purity test and in vitro release studies. The analysis indicated that the chemical structure of AmB remained unchanged in the amorphous solid dispersion, but the structure was changed from crystalline to amorphous.

Solid Dispersions for Oral Administration: An Overview of the Methods for their Preparation.

Oral drug delivery remains the most physiological and therefore the most preferred, simplest and easiest administration route. Nevertheless, a multitude of potentially clinically important drugs will not reach the market or achieve their full potential unless their oral bioavailability is improved by formulation. The aim of this review is to present an overview of properties, formulation, excipients and characterization of solid dispersions corresponding to one of the different formulation strategies for design and development of poorly soluble drugs.

Amorphous solid dispersion studies of camptothecin-cyclodextrin inclusion complexes in PEG 6000.

Abstract: The present work focused on the solubility enhancement of the poorly water-soluble anti-cancer agent camptothecin which, in its natural state, presents poor solubility inducing lack of activity with a marked toxicity. A new approach is adopted by using a ternary system including camptothecin (CPT) and cyclodextrins (CDs) dispersed in polyethylene glycol (PEG) 6000. Camptothecin solubility variations in the presence of α-CD, β-CD, γ-CD, hydroxypropyl-α-CD (HPα-CD), hydroxypropyl-β-CD (HPβ-CD), permethyl-β-CD (PMβ-CD) and sulfobutyl ether-β-CD (SBEβ-CD), were evaluated by Higuchi solubility experiments.

Interaction Study of an Amorphous Solid Dispersion of Cyclosporin A in Poly-Alpha-Cyclodextrin with Model Membranes by (1)H-, (2)H-, (31)P-NMR and Electron Spin Resonance.

The properties of an amorphous solid dispersion of cyclosporine A (ASD) prepared with the copolymer alpha cyclodextrin (POLYA) and cyclosporine A (CYSP) were investigated by (1)H-NMR in solution and its membrane interactions were studied by (1)H-NMR in small unilamellar vesicles and by (31)P (2)H NMR in phospholipidic dispersions of DMPC (dimyristoylphosphatidylcholine) in comparison with those of POLYA and CYSP alone. (1)H-NMR chemical shift variations showed that CYSP really interacts with POLYA, with possible adduct formation, dispersion in the solid matrix of the POLYA, and also complex formation. A coarse approach to the latter mechanism was tested using the continuous variations method, indicating an apparent 1 : 1 stoichiometry.

Identification of tiagabine degradation products using liquid chromatography with electrospray ionization multistage mass spectrometry and ultra-performance liquid chromatography/high-resolution mass spectrometry.

Rationale: Tiagabine hydrochloride monohydrate drug substance (TGB) is an antiepileptic agent effective in the treatment of seizure disorders. The stability of TGB was studied and its degradation products were identified for the first time.

Methods: TGB was heated in the presence of H(2)O(2).

Sinefungin-PLGA nanoparticles: drug loading, characterization, in vitro drug release and in vivo studies.

Cryptosporidiosis, the leading cause of endemic and epidemic diarrhoeal disease worldwide is due to Cryptosporidium parvum, a spore-forming protozoan. Anticryptosporidial pharmacological and/or immunological agents were initially tested in immunodeficient models of cryptosporidiosis, and sinefungin exhibited a significant dose dependent curative and preventive activity. Shedding relapses observed after discontinuation of sinefungin therapy lead to identify the bile ducts as a protected reservoir that may sustain chronic infection.

Cyclodextrin polymers as efficient solubilizers of albendazole: complexation and physico-chemical characterization.

The inclusion behavior of natural cyclodextrins (CDs) and polymers based on natural cyclodextrins (CD-polymer), in solution and in solid-state, was studied towards a poorly water-soluble anti-helminthic drug, albendazole (ABZ), chemically methyl[5-(propylthio)-1-H-benzimidazol-2yl]carbamate. Drug-cyclodextrin solid systems were prepared by freeze-drying. Phase solubility study was used to evaluate the interaction in solution, between ABZ/(CDs) and ABZ/CD-polymers.

Ethical observations on the choice of parenteral solvents. Choice of parenteral solvent...

The parenteral administration of insoluble drugs leads to the use of biologically active solvents inducing effects associated with ethical cause of concern including pain and pharmacological interactions. Selected vehicles currently used were ethically and scientifically reviewed. Our investigations allowed reinforcing the formulation decision tree with an ethical point of view.

Effect of iontophoresis and penetration enhancers on transdermal absorption of metopimazine.

Background: Metopimazine is an antiemetic drug already used by oral and rectal administration. It would be interesting to develop a new formulation for a transdermal administration.

Objective: The objective of this study was to determine the influence of iontophoresis on the metopimazine transdermal absorption and the possible synergistic enhancement with chemical enhancers.

Percutaneous absorption of metopimazine and effect of cyclodextrins.

Metopimazine (MPZ) is used to prevent emesis during chemotherapies. A transdermal delivery system of MPZ may present a great advantage in patients to improve compliance. Hydroxypropyl beta cyclodextrin (HPbetaCD) and partially methylated beta cyclodextrin (PMbetaCD) were tested to enhance the percutaneous absorption of MPZ through pig skin using Franz's cells.

Solubility and dissolution rate of progesterone-cyclodextrin-polymer systems.

This contribution focused on the solubility improvement of the poorly water-soluble steroid hormone progesterone which, in its natural state, presents a reduced oral bioavailability. In the first part of this study, two simple, reproducible methods that were candidates for use in the preparation of inclusion complexes with cyclodextrins were investigated. Solubility capacities of the progesterone complex with hydroxypropyl-beta-CD (HPbeta-CD), hydoxypropyl-gamma-CD (HPgamma-CD), permethyl-beta-CD (PMbeta-CD), and sulfobutylether-beta-CD (SBEbeta-CD), prepared by the freeze-drying and precipitation methods, were evaluated by Higuchi phase solubility studies.

Optimization of entrapment of metronidazole in amphiphilic beta-cyclodextrin nanospheres.

Several aspects of the manufacture of nanospheres containing metronidazole were studied. Nanospheres made of amphiphilic beta-cyclodextrin containing metronidazole were prepared by adding an acetone solution of amphiphilic cyclodextrin to an aqueous solution of metronidazole with or without Pluronic PE/F68 as the surfactant. An optimized formulation with high encapsulation efficiencies and with an appropriate particle size for intravenous administration, was developed.