Papers by Claudio Salomon
Journal of Molecular Liquids
International Journal of Pharmaceutics, Jun 1, 2023
Journal of the Chemical Society, 1996
Journal of Food Science, Mar 20, 2023
Probiotics are live microorganisms that confer beneficial effects on the health of the host if ad... more Probiotics are live microorganisms that confer beneficial effects on the health of the host if administered in adequate amounts (106 CFU viable microorganisms/g of food). As the most frequent route of administration of these microorganisms is oral, the number of them that remains viable through the gastrointestinal tract decreases substantially. Thus, in this research work, we developed a series of alginate‐based microparticles using different adjuvants such as methylcellulose, carboxymethylcellulose, chitosan, carbopol, β‐cyclodextrin, starch, carrageenan, and Eudragit® RS 100 as carriers for improving the survival of Lactococcus lactis. The alginate‐based formulations exhibited very good drug encapsulation efficiency, up to 90%. Release studies from selected microparticles revealed that almost 100% of bacteria were in solution at 30 min. By scanning electron microscopy, irregular nonporous particles with a size between 200 and 500 µm were seen. In particular, microparticles formulated with alginate–carboxymethylcellulose and alginate–methylcellulose exhibited the best protection for the bacterial cells against both simulated gastric juice and simulated intestinal juice. In addition, those microparticulate systems were able to maintain the viability of the encapsulated bacteria in large numbers for at least 24 weeks. Thus, the present study confirmed that these alginate‐based microparticles are a valuable approach for keeping the viability and storage stability of L. lactis.
Canadian Journal of Chemistry, Mar 1, 1991
A stereospecific synthesis of 6,6-dibromo-3α-cyano-2,2-dimethylpenam-(1R)-S-oxide (2) is describe... more A stereospecific synthesis of 6,6-dibromo-3α-cyano-2,2-dimethylpenam-(1R)-S-oxide (2) is described. The X-ray single crystal investigation of this compound shows that it crystallizes in the monoclinic system, space group P21, with cell parameters a = 6.194(1), b = 9.363(1), c = 9.869(1) Å, β = 96.55(2)°, V = 568(1) Å3, and two molecules per unit cell. Thestructure was solved, from low temperature data, by direct methods, and refined, by least-squares procedures, to a final R = 3.17%, Rw = 3.38%, for 1221 observed independent reflections. The sulfoxide configuration is R. The thiazolidine presents an envelope shape with the C(3) atom 0.56 Å above the other four members of the ring mean plane. Therefore, it exhibits the conformation with α-CH3 pseudoequatorial and β-CH3 and α-CN both pseudoaxial. This conformation is different from the one reported for other penicillin sulfoxide derivatives. The geometry of the β-lactam ring is typical of the fused bicyclic penam nucleus. The ring is non-planar. The N(4) atom displays a pyramidial arrangement. The examination of crystal packing shows that molecules along a are connected by a short C—H … O contactReported single crystal studies showed two dominant conformations for the thiazolidine ring in the fused bicyclic penam nucleus: the C(3) or 2β-3α substituents both pseudoaxial, as found in 2, and the S(1) or 2β-3α substituents both pseudoequatorial, adopted by most sulfoxides. Neither of these conformations can explain the nuclear Overhauser effect data. A conformation with the substituents C2-β-methyl-C3-α-H and C2-α-methyl-C3-α-CN fully eclipsed is in accordance with the experimental results in the solution. The 1H nuclear magnetic resonance data reflect the influence of the magnetic anisotropy of the CN triple bond on the gem-dimethyl groups, particularly in relation with the geometrical features of the molecule. Comparison of 13C nuclear magnetic resonance chemical shifts for 2 and its parent penicillin sulfide (1) indicates configurationally dependent substituent effects, the magnitude of which can be used for the stereochemical assignment of sulfoxide groups in this series. Key words: penicillin sulfoxide derivatives, di-halogen penicillanates, stereospecific synthesis, NMR studies, absolute configuration determination.
ChemInform, Aug 22, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Journal of Molecular Liquids, Jul 1, 2023
International Journal of Pharmaceutics, 2018
Pharmaceutical Development and Technology, Mar 10, 2010
AAPS Introductions in the Pharmaceutical Sciences, 2023
Journal of Antimicrobial Chemotherapy, 2020
Background Benznidazole and nifurtimox are effective drugs used to treat Chagas’ disease; however... more Background Benznidazole and nifurtimox are effective drugs used to treat Chagas’ disease; however, their administration in patients in the chronic phase of the disease is still limited, mainly due to their limited efficacy in the later chronic stage of the disease and to the adverse effects related to these drugs. Objectives To evaluate the effect of low doses of nanoformulated benznidazole using a chronic model of Trypanosoma cruzi Nicaragua infection in C57BL/6J mice. Methods Nanoformulations were administered in two different schemes: one daily dose for 30 days or one dose every 7 days, 13 times. Results Both treatment schemes showed promising outcomes, such as the elimination of parasitaemia, a reduction in the levels of T. cruzi-specific antibodies and a reduction in T. cruzi-specific IFN-γ-producing cells, as well as an improvement in electrocardiographic alterations and a reduction in inflammation and fibrosis in the heart compared with untreated T. cruzi-infected animals. Th...
Materials Science and Engineering: C, 2017
Pharmaceutics
To date, the treatment for cysticercosis and neurocysticercosis consists of a single oral intake ... more To date, the treatment for cysticercosis and neurocysticercosis consists of a single oral intake of praziquantel (5–10 mg/kg), which since it is only available as tablets, hinders its administration to pediatric patients. Praziquantel is a poorly water-soluble drug which represents a challenge for its formulation in solution, particularly for the pediatric population. Thus, this study aimed to develop a palatable solution for praziquantel using pharmaceutical-accepted co-solvent systems. A design of experiments approach was applied to identify the optimal conditions for achieving a suitable amount of praziquantel in solution using co-solvent mixtures. Thus, praziquantel solubility increased from 0.38 up to 43.50 mg/mL in the optimized system. A taste masking assay in healthy human volunteers confirmed a successful reduction of drug bitterness after the addition of selected flavors and a sweetener. Stability studies were also conducted at different temperatures (4, 25, and 40 °C) for...
Pharmaceutics
To date, the treatment for cysticercosis and neurocysticercosis consists of a single oral intake ... more To date, the treatment for cysticercosis and neurocysticercosis consists of a single oral intake of praziquantel (5–10 mg/kg), which since it is only available as tablets, hinders its administration to pediatric patients. Praziquantel is a poorly water-soluble drug which represents a challenge for its formulation in solution, particularly for the pediatric population. Thus, this study aimed to develop a palatable solution for praziquantel using pharmaceutical-accepted co-solvent systems. A design of experiments approach was applied to identify the optimal conditions for achieving a suitable amount of praziquantel in solution using co-solvent mixtures. Thus, praziquantel solubility increased from 0.38 up to 43.50 mg/mL in the optimized system. A taste masking assay in healthy human volunteers confirmed a successful reduction of drug bitterness after the addition of selected flavors and a sweetener. Stability studies were also conducted at different temperatures (4, 25, and 40 °C) for...
International journal of biological macromolecules, Jan 18, 2015
In this study a novel receptor-targeted micelle delivery system based on tocopherol succinate-chi... more In this study a novel receptor-targeted micelle delivery system based on tocopherol succinate-chitosan-polyethylene glycol-folic acid (TS-CS-PEG-FA) was synthesized and loaded with paclitaxel (PTX). Physicochemical properties of the micelles such as critical micelle concentration, micelle size, entrapment efficiency, stability, release properties, cellular uptake and in vitro cytotoxicity were investigated in detail. Furthermore, the pharmacokinetics and tissue distributions of PTX-loaded micelles were evaluated in Balb/c mice and compared with Anzatax(®) (PTX in Cremophor EL(®)). Particle sizes and zeta potentials of the micelles were in the range of 162.3-277.1nm and 18.5-28.3mV, respectively. The drug entrapment efficiencies of the micelles were within 53.6-82.5% (w/w). Cytotoxicity assay demonstrated increased cytotoxic activity of PTX-loaded TS-CS-PEG-FA micelles compared to free PTX. The Vd and t1/2β of PTX-loaded TS-CS-PEG-FA were increased by 2.76- and 2.05-fold, respectivel...
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Papers by Claudio Salomon