Decalepis hamiltonii (Wight & Arn.) Fortified Jaggery: Its Physico-chemical Characterization and Studies on its In vitro Biological Activities

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.

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

Pharmaceutics ◽

10.3390/pharmaceutics11060263 ◽

2019 ◽

Vol 11 (6) ◽

pp. 263 ◽

Cited By ~ 4

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.

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Nanomedicines for active targeting: Physico-chemical characterization of paclitaxel-loaded anti-HER2 immunonanoparticles and in vitro functional studies on target cells

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2009.07.006 ◽

2009 ◽

Vol 38 (3) ◽

pp. 230-237 ◽

Cited By ~ 42

Author(s):

A. Cirstoiu-Hapca ◽

F. Buchegger ◽

L. Bossy ◽

M. Kosinski ◽

R. Gurny ◽

...

Keyword(s):

Chemical Characterization ◽

Active Targeting ◽

Target Cells ◽

Functional Studies ◽

Physico Chemical

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

Journal of Controlled Release ◽

10.1016/j.jconrel.2012.07.015 ◽

2012 ◽

Vol 162 (3) ◽

pp. 545-552 ◽

Cited By ~ 63

Author(s):

Amélie Dufaÿ Wojcicki ◽

Hervé Hillaireau ◽

Thais Leite Nascimento ◽

Silvia Arpicco ◽

Myriam Taverna ◽

...

Keyword(s):

Hyaluronic Acid ◽

Chemical Characterization ◽

Cd44 Receptor ◽

Physico Chemical

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

Molecules ◽

10.3390/molecules26165107 ◽

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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Chiral Forms of 4-(2',4'-Difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic Acid (Flobufen) and Its Metabolite.Synthesis and Basic Biological Properties

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19970498 ◽

1997 ◽

Vol 62 (3) ◽

pp. 498-509 ◽

Cited By ~ 5

Author(s):

Miroslav Kuchař ◽

Marie Poppová ◽

Antonín Jandera ◽

Vladimíra Panajotovová ◽

Hana Zůnová ◽

...

Keyword(s):

Rheumatoid Arthritis ◽

Biological Activities ◽

Biological Properties ◽

Optical Isomers ◽

Clinical Testing ◽

Chemical Parameters ◽

Physico Chemical ◽

Oxobutanoic Acid

4-(2',4'-Difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid (1, flobufen) is subjected to clinical testing in the treatment of rheumatoid arthritis. Owing to the occurrence of a centre of chirality, the compound exists in two enantiomers, and its major human metabolite, viz. 4-(2',4'-difluorobiphenyl-4-yl)-4-hydroxy-2-methylbutanoic acid isolated in the lactone form (2), possesses two chiral centres, making possible the existence of four stereoisomers. All of the optical isomers of the substances 1 and 2 were prepared. For flobufen (1), the racemate was separated into the stereoisomers by using the salts 3 with R-(+)- or S-(-)-1-phenylethylamine. The pairs of stereoisomers of 2, obtained by reduction of R-(+)-flobufen or the S-(-)-enantiomer, were separated by column chromatography. The physico-chemical parameters of the optical isomers were determined and some biological activities were evaluated in both in vitro and in vivo models.

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Identification of a Proanthocyanidin from Litchi Chinensis Sonn. Root with Anti-Tyrosinase and Antioxidant Activity

Biomolecules ◽

10.3390/biom10091347 ◽

2020 ◽

Vol 10 (9) ◽

pp. 1347

Author(s):

Matthew Saive ◽

Manon Genva ◽

Thibaut Istasse ◽

Michel Frederich ◽

Chloé Maes ◽

...

Keyword(s):

Antioxidant Activities ◽

Biological Activities ◽

Chemical Characterization ◽

2D Nmr ◽

Ethnobotanical Study ◽

Traditional Use ◽

Litchi Chinensis ◽

Isolated Compound ◽

First Time

This work follows an ethnobotanical study that took place in the island of Mayotte (France), which pointed out the potential properties of Litchi chinensis Sonn. roots when used to enhance skin health and appearance. Through in vitro testing of a crude methanolic extract, high anti-tyrosinase (skin whitening effect) and antioxidant activities (skin soothing effect) could be measured. HPLC successive bio-guided fractionation steps allowed the purification of one of the compounds responsible for the biological activities. The isolated compound was characterized by UV, IR, MS and 2D-NMR, revealing, for the first time in Litchi chinensis Sonn. roots, an A-type proanthocyanidin and thus revealing a consensus among the traditional use shown by the ethnobotanical study, in vitro biological activities and chemical characterization.

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Design, physico-chemical characterization and in vitro biological activity of organogold(III) glycoconjugates

Dalton Transactions ◽

10.1039/d1dt01100f ◽

2021 ◽

Author(s):

Andrea Pettenuzzo ◽

Keti Vezzù ◽

Maria Luisa Di Paolo ◽

Eirini Fotopoulou ◽

Luciano Marchiò ◽

...

Keyword(s):

Biological Activity ◽

Anticancer Agents ◽

Chemical Characterization ◽

Physico Chemical

In order to develop new metal-based glycoconjugates as potential anticancer agents, four organometallic gold(III)-dithiocarbamato glycoconjugates of the type [AuIII(2-Bnpy)(SSC-Inp-GlcN)](PF6) (2-Bnpy: 2-benzylpyridine; Inp: isonipecotic moiety; GlcN: amino-glucose scaffold; Au3-Au6) and the...

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