Perphenazine–fumaric acid salts with improved solubility: preparation, physico-chemical characterization and in vitro dissolution

CrystEngComm ◽  
2012 ◽  
Vol 14 (18) ◽  
pp. 6035 ◽  
Author(s):  
Giovanna Bruni ◽  
Mariarosa Maietta ◽  
Lauretta Maggi ◽  
Marcella Bini ◽  
Doretta Capsoni ◽  
...  
Keyword(s):  
Fumaric Acid ◽  
Chemical Characterization ◽  
In Vitro Dissolution ◽  
Physico Chemical ◽  
Acid Salts

Complexation with Hydroxypropyl-gama-Cyclodextrin of Birch Tree Extract Physico-chemical Characterisation of their Binary Products

2008 ◽  
Vol 59 (6) ◽  
Author(s):  
Codruta Soica ◽  
Cristina A. Dehelean ◽  
Valentin Ordodi ◽  
Diana Antal ◽  
Vicentiu Vlaia
Keyword(s):  
Inclusion Complexes ◽  
Water Solubility ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Bark Extract ◽  
Birch Bark ◽  
Preparation Methods ◽  
Birch Tree ◽  
Physico Chemical

Birch bark contains important pentacyclic triterpens that determine an anticancer, anti-inflammatory and antiviral activity. The compounds can be extracted by simple procedures with organic solvents. The major problem of this type of triterpens is their low water solubility which can be increased by physical procedures like cyclodextrin complexation. The aim of present study was to analyse the products between birch bark extract and hydroxypropyl-g -cyclodextrin. Hydroxypropyl-g -cyclodextrin (HPGCD) was used as a host to improve its solubility in water, via inclusion complex formation. In order to obtain the inclusion complexes, 1:2 molar ratio and two preparation methods (physical mixing, kneading) were used. The inclusion complexes were analyzed by in vitro dissolution tests, thermal analysis and X-ray diffraction.

Antibody targeting of lipid nanocapsules for directed drug delivery: physico-chemical characterization and in vitro study

2010 ◽  
Vol 15 (23-24) ◽  
pp. 1105-1105
Author(s):  
P. Sánchez-Moreno ◽  
H. Boulaiz ◽  
J.A. Marchal ◽  
J.L. Ortega-Vinuesa ◽  
J.M. Peula García ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Chemical Characterization ◽  
In Vitro Study ◽  
Vitro Study ◽  
Lipid Nanocapsules ◽  
Physico Chemical ◽  
Antibody Targeting

scholarly journals In Vitro Physico-Chemical Characterization and Standardized In Vivo Evaluation of Biocompatibility of a New Synthetic Membrane for Guided Bone Regeneration

Materials ◽  
2019 ◽  
Vol 12 (7) ◽  
pp. 1186
Author(s):  
Lívia da Costa Pereira ◽  
Carlos Fernando de Almeida Barros Mourão ◽  
Adriana Terezinha Neves Novellino Alves ◽  
Rodrigo Figueiredo de Brito Resende ◽  
Marcelo José Pinheiro Guedes de Uzeda ◽  
...  
Keyword(s):  
Bone Regeneration ◽  
Chemical Properties ◽  
Chemical Characterization ◽  
Guided Bone Regeneration ◽  
Tissue Reaction ◽  
In Vivo Evaluation ◽  
Physico Chemical ◽  
Tissue Reactions

This study’s aim was to evaluate the biocompatibility and bioabsorption of a new membrane for guided bone regeneration (polylactic-co-glycolic acid associated with hydroxyapatite and β-tricalcium phosphate) with three thicknesses (200, 500, and 700 µm) implanted in mice subcutaneously. Scanning electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy, and the quantification of carbon, hydrogen and nitrogen were used to characterize the physico-chemical properties. One hundred Balb-C mice were divided into 5 experimental groups: Group 1—Sham (without implantation); Group 2—200 μm; Group 3—500 μm; Group 4—700 μm; and Group 5—Pratix®. Each group was subdivided into four experimental periods (7, 30, 60 and 90 days). Samples were collected and processed for histological and histomorphometrical evaluation. The membranes showed no moderate or severe tissue reactions during the experimental periods studied. The 500-μm membrane showed no tissue reaction during any experimental period. The 200-μm membrane began to exhibit fragmentation after 30 days, while the 500-μm and 700-µm membranes began fragmentation at 90 days. All membranes studied were biocompatible and the 500 µm membrane showed the best results for absorption and tissue reaction, indicating its potential for clinical guided bone regeneration.

scholarly journals Optimization of Innovative Three-Dimensionally-Structured Hybrid Vesicles to Improve the Cutaneous Delivery of Clotrimazole for the Treatment of Topical Candidiasis

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 263 ◽  
Author(s):  
Maria Letizia Manca ◽  
Iris Usach ◽  
José Esteban Peris ◽  
Antonella Ibba ◽  
Germano Orrù ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Transmission Electron Microscopy ◽  
Chemical Properties ◽  
Chemical Characterization ◽  
Yeast Cells ◽  
Unilamellar Vesicles ◽  
Transmission Electron ◽  
Physico Chemical

New three-dimensionally-structured hybrid phospholipid vesicles, able to load clotrimazole in a high amount (10 mg/mL), were obtained for the first time in this work by significantly reducing the amount of water (≤10%), which was replaced with a mixture of glycerol and ethanol (≈90%). A pre-formulation study was carried out to evaluate the effect of both the composition of the hydrating medium and the concentration of the phospholipid on the physico-chemical properties of hybrid vesicles. Four different three-dimensionally-structured hybrid vesicles were selected as ideal systems for the topical application of clotrimazole. An extensive physico-chemical characterization performed using transmission electron microscopy (TEM), cryogenic transmission electron microscopy (cryo-TEM), 31P-NMR, and small-angle X-ray scattering (SAXS) displayed the formation of small, multi-, and unilamellar vesicles very close to each other, and was capable of forming a three-dimensional network, which stabilized the dispersion. Additionally, the dilution of the dispersion with water reduced the interactions between vesicles, leading to the formation of single unilamellar vesicles. The evaluation of the in vitro percutaneous delivery of clotrimazole showed an improved drug deposition in the skin strata provided by the three-dimensionally-structured vesicles with respect to the commercial cream (Canesten®) used as a reference. Hybrid vesicles were highly biocompatible and showed a significant antifungal activity in vitro, greater than the commercial cream Canesten®. The antimycotic efficacy of formulations was confirmed by the reduced proliferation of the yeast cells at the site of infection in vivo. In light of these results, clotrimazole-loaded, three-dimensionally-structured hybrid vesicles appear to be one of the most innovative and promising formulations for the treatment of candidiasis infections.

scholarly journals Hyaluronic acid-bearing lipoplexes: Physico-chemical characterization and in vitro targeting of the CD44 receptor

2012 ◽  
Vol 162 (3) ◽  
pp. 545-552 ◽  
Author(s):  
Amélie Dufaÿ Wojcicki ◽  
Hervé Hillaireau ◽  
Thais Leite Nascimento ◽  
Silvia Arpicco ◽  
Myriam Taverna ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
Chemical Characterization ◽  
Cd44 Receptor ◽  
Physico Chemical

scholarly journals Synthesis, In Silico and In Vitro Evaluation of Antimicrobial and Toxicity Features of New 4-[(4-Chlorophenyl)sulfonyl]benzoic Acid Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 5107
Author(s):  
Theodora-Venera Apostol ◽  
Mariana Carmen Chifiriuc ◽  
Constantin Draghici ◽  
Laura-Ileana Socea ◽  
Luminita Gabriela Marutescu ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
In Silico ◽  
Chemical Characterization ◽  
Phenyl Group ◽  
Bacterial Strains ◽  
Benzoic Acid Derivatives ◽  
Physico Chemical ◽  
In Silico Studies ◽  
New Compounds

The multi-step synthesis, physico-chemical characterization, and biological activity of novel valine-derived compounds, i.e., N-acyl-α-amino acids, 1,3-oxazol-5(4H)-ones, N-acyl-α-amino ketones, and 1,3-oxazoles derivatives, bearing a 4-[(4-chlorophenyl)sulfonyl]phenyl moiety are reported here. The structures of the newly synthesized compounds were confirmed by spectral (UV-Vis, FT-IR, MS, 1H- and 13C-NMR) data and elemental analysis results, and their purity was determined by RP-HPLC. The new compounds were assessed for their antimicrobial activity and toxicity to aquatic crustacean Daphnia magna. Also, in silico studies regarding their potential mechanism of action and toxicity were performed. The antimicrobial evaluation revealed that the 2-{4-[(4-chlorophenyl)sulfonyl]benzamido}-3-methylbutanoic acid and the corresponding 1,3-oxazol-5(4H)-one exhibited antimicrobial activity against Gram-positive bacterial strains and the new 1,3-oxazole containing a phenyl group at 5-position against the C. albicans strain.

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