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Cyclodextrins are cyclic cone shaped oligosaccharides. A guest molecule can be incorporated into the hydrophobic inner of the cyclodextrin to form non-covalent complexes. The formation of these complexes in general, increases the solubility, stability, dissolution rate, and bioavailability of drugs with poor water solubility. Different techniques were applied to gain insights about the interaction between paclitaxel and randomly methylated-β-cyclodextrin during the formation of an inclusion complex. Results from infrared spectroscopy, differential scanning calorimetry, nuclear magnetic resonance and scanning electron microscopy were compared. The fast and economical pulsed nuclear magnetic resonance spectroscopy allows to explain that mol paclitaxel:mol RAMEβ-CD 1:20 was the best ratio to obtain inclusion complexes. In addition, the preferred aromatic ring for the inclusion is that in the position 3? of the side chain of paclitaxel molecule. Fil: Williams Velázquez, Natalia Noemi. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Ferreyra, Maria Graciela. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Mengatto, Luciano Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Santagapita, Patricio Roman. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias. Instituto de Tecnología de Alimentos y Procesos Quimicos. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Instituto de Tecnología de Alimentos y Procesos Quimicos.; Argentina Fil: Buera, Maria del Pilar. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias. Instituto de Tecnología de Alimentos y Procesos Quimicos. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Instituto de Tecnología de Alimentos y Procesos Quimicos.; Argentina Fil: Luna, Julio Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina

Progesterone (PGT) is a natural hormone that stimulates and regulates various important functions, such as the preparation of the female body for conception and pregnancy. Due to its low water solubility, it is administered in a micronized form and/or in vehicles with specific solvents requirements. In order to improve the drug solubility, inclusion complexes of PGT and β-cyclodextrins were obtained by the freeze-drying method. Two β-cyclodextrins (native and methylated) in two solvents (water and water:ethanol) and different molar ratio of the reagents were the variables tested for the selection of the best condition for the preparation of the complexes. The PGT/randomly methylated-β-cyclodextrin complexes were incorporated into chitosan thermosensitive hydrogels, as an alternative formulation for the vaginal administration of PGT. Neither the micro and macroscopic characteristics of the gels nor the transition time from solution to gel were modified after the complexes incorporation. In addition, chitosan gels with complexes resisted better the degradation in simulated vaginal fluid in comparison to commercial gel (Crinone®). The chitosan gel with inclusion complexes and Crinone® were tested in vitro in a diffusion assay to evaluate the delivery of the hormone and its diffusion through porcine epithelial mucosa obtained from vaginal tissue. Chitosan gel presented sustained diffusion similar to the exhibited by commercial gel. The use of chitosan gels with inclusion complexes based on cyclodextrins would be a viable alternative for vaginal administration of PGT. Fil: Velazquez, Natalia Soledad. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Turino, Ludmila Noelia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Luna, Julio Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Mengatto, Luciano Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina

Chitosan - β-glycerophosphate hydrogels have been widely studied for biomedical applications in recent years. In the current study a Chitosan - β-glycerophosphate hydrogel was evaluated as a platform for sodium fluoride release in the gastrointestinal tract. For this purpose, microscopy observation, infrared spectroscopy, stability, rheology studies and in vitro release assays were carried out. The hydrogel was stable for at least 48 h when exposed to an aqueous media in a pH range from 4 to 7 and the release of sodium fluoride was controlled for more than 6 h. In vivo studies were carried out in order to evaluate the oral administration of sodium fluoride using the hydrogel in comparison to a water solution. Fluoride pharmacokinetic was similar when the drug was administered with both formulations. Nevertheless, fluoride absorption was greater when the drug was given with the hydrogel, and further, drug-related side effects were absents. These results suggest that Chitosan - β-glycerophosphate hydrogel could be a good candidate for sustained release of fluoride in oral formulation. Fil: Fookes, Federico Adrian. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Mengatto, Luciano Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Rigalli, Alfredo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Médicas. Laboratorio de Biología Ósea; Argentina Fil: Luna, Julio Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Médicas. Laboratorio de Biología Ósea; Argentina

Objectives: To evaluate the combination of more than one release system in the same formulation as a useful strategy to achieve paclitaxel delivery in a more sustained and controlled manner. Methods: The present study deals with the preparation of poly(lactide-co-glycolide) microparticles loaded with paclitaxel and included in a chitosan thermo-sensitive gelling solution. The microparticles were characterized by their size, shape and drug loading. The formulation was characterized by scanning electron microscopy, in vitro release experiments and was evaluated in mice bearing mammary adenocarcinoma. Key findings: The formation of paclitaxel crystals in a pharmaceutical formulation reduces its efficacy. In this work, the use of microparticles avoided this phenomenon. Combining more than one delivery system allowed delivering paclitaxel in a more sustained and controlled manner leading to a long-term effect in the site of action. The formulation showed an inhibition in tumour volume of 63.0% in comparison with the control group. Conclusions: One intratumour injection of gelling solution containing the microparticles was at least as efficacious as four intraperitoneal injections of a commercial formulation. In addition, the delivery system was nontoxic, and the treated mice presented the highest percentage of tumour regression and median survival time. Fil: Pesoa, Juan Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Rico, Maria Jose. Universidad Nacional de Rosario. Facultad de Ciencias Médicas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Rozados, Viviana Rosa. Universidad Nacional de Rosario. Facultad de Ciencias Médicas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Scharovsky, Olga Graciela. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Médicas; Argentina Fil: Luna, Julio Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Mengatto, Luciano Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina

In this work, a new recyclable ethylene-vinyl acetate (EVA)-based strip impregnated with amitraz (AMZ) was prepared, characterized, and evaluated for the treatment of Apis mellifera against Varroa destructor. Bees are important for natural pollination, honey, and related goods production. Varroa destructor is currently considered one of the major pests and important efforts around the world are focused on methods for varroasis treatment. The procedure of strips preparation presented in this work consisted of two steps: impregnation and molding of impregnated pellets. Differential scanning calorimetry and gas chromatography?mass spectrometry analyses confirmed that AMZ molecule resisted the impregnation and molding conditions. The strips were sufficiently strong to resist destruction by the bees. The final infestation was lower in the hives treated with AMZ/EVA strips than in those treated with commercial strips. In order to check the possibility of recycling, strips were cut into little pieces and were subjected to total AMZ extraction. Finally, the fragments were exposed to re-impregnation and molding. The strips prepared after the recycling process presented the same shape and AMZ load than fresh strips. Fil: Karp, Federico. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Luna, Julio Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Mengatto, Luciano Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina

Chitosan membranes with different cross-linking density were prepared by modifying cross-linking time. Sodium tripolyphosphate was the cross-linking agent. A pulsed nuclear magnetic resonance study was performed on uncross-linked and cross-linked membranes. Different fraction of water molecules were identified in different zones within the membranes. The ratio of water molecules per chitosan repeating unit were calculated. A maximum of twelve water molecules were tightly coordinated to the chitosan repeating unit. Also, a very small water molecule fraction was identified but it was mobile enough as not to contribute to the dipolar interactions. The cross-linking reaction could lead to the formation of hydrophilic and hydrophobic interactions. These two types of interactions could result in the coexistence of a network formed by hydrophilic and hydrophobic micropores. This knowledge could be useful for the interpretation of results of hydrophobic drugs permeation across hydrophilic membranes. For example, the increment of estradiol fluxes across chitosan membranes with an increase in cross-linking density. © 2013 Elsevier B.V. All rights reserved. Fil: Mengatto, Luciano Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Santa Fe. Instituto de Desarrollo Tecnológico Para la Industria Química (i); Argentina. Universidad Nacional del Litoral; Argentina Fil: Ferreyra, Maria Graciela. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Santa Fe. Instituto de Desarrollo Tecnológico Para la Industria Química (i); Argentina. Universidad Nacional del Litoral; Argentina Fil: Rubiolo, Amelia Catalina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Santa Fe. Instituto de Desarrollo Tecnológico Para la Industria Química (i); Argentina. Universidad Nacional del Litoral; Argentina Fil: Rintoul, Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Santa Fe. Instituto de Desarrollo Tecnológico Para la Industria Química (i); Argentina. Universidad Nacional del Litoral; Argentina Fil: Luna, Julio Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Santa Fe. Instituto de Desarrollo Tecnológico Para la Industria Química (i); Argentina. Universidad Nacional del Litoral; Argentina

The parameters affecting the sol/gel transition of chitosan-based thermogelling systems, their final proper-ties and structure have been reported. Nevertheless, equa-tions that define this relationship specific for a particular case have not been developed. The aim of this study was to develop these equations for a general formulation without drugs, so they could be used in the preparation of different drug delivery systems. First, a factorial design was built to evaluate the main factors affecting the pH of a gel-forming solution, gelling time at ambient temperature and 37.5 °C and residual mass after exposure to a buffer solution. The analyzed independent factors were: chitosan concentration, β-glycerophosphate concentration, mixing temperature and mixing time. Mixing time was the only factor whose effect on the responses was not significant; the other three factors were considered for the optimization study. Then, a central composite design based on response surface methodology was carried out to develop statistical models which describe the relationship between active independent factors and the studied responses. The optimized gel was prepared and characterized. FTIR experiments showed that hydrogen bonds and electrostatic attraction were the main types of interactions following sol-to-gel transition. The most important finding of this investigation was that the resulting equations could be used to prepare gel-forming solutions with the desired pH, gelling time and residualmass. The significance of these equations was considered in their potential use to design hydrogels intended for con-trolled drug delivery. Fil: Mengatto, Luciano Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Pesoa, Juan Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Velazquez, Natalia Soledad. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Luna, Julio Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina

The present work deals with the study of estradiol permeation in chitosan membranes. A fractional factorial design was built for the determination of the main factors affecting estradiol permeation. The independent factors analysed were: concentration of chitosan, concentration of cross-linking agent, cross-linking time and thermal treatment. It was found that concentration of chitosan and cross-linking time significantly affected the response. The effects of thermal treatment and concentration of cross-linking agent were not significant. An optimization process based on response surface methodology was carried out in order to develop a statistical model which describes the relationship between active independent variables and estradiol flux. This model can be used to find out a combination of factor levels during response optimization. Possible options for response optimization are to maximize, minimize or move towards a target value. Fil: Mengatto, Luciano Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Cabrera, Maria Ines. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico Para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico Para la Industria Química; Argentina Fil: Luna, Julio Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico Para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico Para la Industria Química; Argentina

Chitosan is a versatile carrier for biologically active agent from a small molecule such as an antibiotic to macromolecules such as proteins and nucleic acids. In addition, drug delivery devices based on chitosan can be available in a variety of morphologies including films, fibers, nanoparticles and microspheres. Otherwise the inherent advantages of this polymer such as biocompatibility, tissue adhesions and hydrophilic nature, chitosan can be modified to accomplish a specific purpose, for example improves release kinetics. In this review, recent patents of chitosan-based film systems for drug delivery are presented and discussed. This review include matrix type systems, membrane coated systems and film forming solution. For each one of these systems, several examples of manufacture processes, bioactive agents to be delivered and specifics applications are considered. This work highlights the use of chitosan in the film technology for drug delivery, presenting examples of chitosan used in an unmodified state and examples of modifications of the polymer backbone.

Polymeric membranes with skin-mimetic permeability properties appear as attractive models for use in the development of transdermal drug delivery systems. These membranes can be placed in contact with the transdermal system and simulate the skin barrier. In the current work, statistical experimental design was implemented for preparation of the optimized chitosan membrane to mimic human epidermis. For this purpose, an optimization process based on response surface methodology was carried out in order to determine the best combination of independent factors for membrane preparation. The independent factors analyzed were concentration of chitosan, concentration of cross-linking agent, and cross-linking time. The optimized membrane successfully simulated the cumulative amount of estradiol released per unit time for human epidermis. In addition, the optimized membrane was evaluated for the development of an estradiol delivery system. This in vitro technology may offer an alternative methodology for the development of transdermal delivery systems.

One possibility to obtain a higher dose of drug in a lower formulation volume can be by using of saturated quantity of drug in one of the phases of an emulsion. These formulations are called suspoemulsions (S/O/W). When a hydrophobic polymer is added to the organic phase of suspoemulsions, these formulations can be used to entrap the drug inside microspheres after in situ precipitation of the polymer-drug-excipients mix. In this work, performance and stability of progesterone suspensions in triacetin as organic phase of suspoemulsions were evaluated. These formulations were compared with O/W emulsions. Mathematical models were used to study in vitro release profiles. The results confirmed that S/O/W systems could be an attractive alternative to O/W formulations for the entrapment of progesterone inside poly(d,l-lactide-co-glycolide) microspheres. Diffusive-based models fit the in vitro release of progesterone from in situ-formed microspheres. For longer release periods, a time-dependent diffusion coefficient was successfully estimated.

Chitosan membranes were obtained by a casting/solvent evaporation method and cross-linking with sodium tripolyphosphate. The effect of cross-linking time was studied and the cross-linked membranes were characterized with respect to equilibrium water content, sodium content, IR spectroscopy and permeability to a model drug (Estradiol). Sodium content increased with increasing cross-linking time. Equilibrium water content was higher in the membrane with the lowest cross-linking time. This membrane also showed a higher flux of Estradiol compared with the other which exhibited an increment in equilibrium water content and flux of Estradiol with the increase in cross-linking duration. These dissimilar results could be explained by a significant correlation between the hydrophilicity of the membrane and the hydrophobicity of Estradiol. Fil: Mengatto, Luciano Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Luna, Julio Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina Fil: Cabrera, Maria Ines. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina