Dataset Information

Production and Characterization of Glutathione-Chitosan Conjugate Films as Systems for Localized Release of Methotrexate.

ABSTRACT: Cancer is one of the most serious public health problems that affect humanity. Diverse delivery systems of anticancer drugs have been developed to enhance the treatment effectiveness and patient compliance. Thus, drug delivery systems from polymeric films could be an interesting and promising alternative, especially for skin chemotherapeutics. In this work, polymeric films based on glutathione-chitosan conjugates with degrees of thiolation of 4.4%, 5.1% and 7.0% were synthetized by casting-evaporation method and subsequent loading with methotrexate. The surface properties of these films were evaluated by contact angle and spreading rate measurements. The sessile drop methods along with the thermodynamic parameter of work of adhesion were determined using the Young-Dupré semi-empirical model. The in vitro methotrexate release was assessed at a pH of 4.5 and 7.4 simulating physiological conditions. Data from the resulting profiles were fitted to the order one, Higuchi, Peppas-Sahlin and Korsmeyer-Peppas kinetic models. The results suggest a strong relationship between the thiolation degree and hydrophilic surface properties such as contact angle and water spreading rate, whereas the work of adhesion was not significantly affected. Further, these polymer films could control the methotrexate release through diverse mechanisms such as diffusion and relaxation depending on the thiolation degree and the aqueous medium employed. In fact, as thiolation degree increased, the release mechanism shifted from a primary diffusional type towards a predominant relaxation-driven mechanism. These polymer films could be used as modified systems for anticancer local delivery.

SUBMITTER: Ciro Y

PROVIDER: S-EPMC6960860 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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Production and Characterization of Glutathione-Chitosan Conjugate Films as Systems for Localized Release of Methotrexate.

Ciro Yhors Y Rojas John J Yarce Cristian J CJ Salamanca Constain H CH

Polymers 20191207 12

Cancer is one of the most serious public health problems that affect humanity. Diverse delivery systems of anticancer drugs have been developed to enhance the treatment effectiveness and patient compliance. Thus, drug delivery systems from polymeric films could be an interesting and promising alternative, especially for skin chemotherapeutics. In this work, polymeric films based on glutathione-chitosan conjugates with degrees of thiolation of 4.4%, 5.1% and 7.0% were synthetized by casting-evapo ...[more]

PMID: 31817917

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Project description:The development of new biocompatible materials for application in the replacement of deteriorated tissues (due to accidents and diseases) has gained a lot of attention due to the high demand around the world. Tissue engineering offers multiple options from biocompatible materials with easy resorption. Chitosan (CS) is a biopolymer derived from chitin, the second most abundant polysaccharide in nature, which has been highly used for cell regeneration applications. In this work, CS films and Ruta graveolens essential oil (RGEO) were incorporated to obtain porous and resorbable materials, which did not generate allergic reactions. An oil-free formulation (F1: CS) and three different formulations containing R. graveolens essential oil were prepared (F2: CS-RGEO 0.5%; F3: CS+RGEO 1.0%; and F4: CS+RGEO 1.5%) to evaluate the effect of the RGEO incorporation in the mechanical and thermal stability of the films. Infrared spectroscopy (FTIR) analyses demonstrated the presence of RGEO. In contrast, X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analysis showed that the crystalline structure and percentage of CS were slightly affected by the RGEO incorporation. Interesting saturation phenomena were observed for mechanical and water permeability tests when RGEO was incorporated at higher than 0.5% (v/v). The results of subdermal implantation after 30 days in Wistar rats showed that increasing the amount of RGEO resulted in greater resorption of the material, but also more significant inflammation of the tissue surrounding the materials. On the other hand, the thermal analysis showed that the RGEO incorporation almost did not affect thermal degradation. However, mechanical properties demonstrated an understandable loss of tensile strength and Young's modulus for F3 and F4. However, given the volatility of the RGEO, it was possible to generate a slightly porous structure, as can be seen in the microstructure analysis of the surface and the cross-section of the films. The cytotoxicity analysis of the CS+RGEO compositions by the hemolysis technique agreed with in vivo results of the low toxicity observed. All these results demonstrate that films including crude essential oil have great application potential in the biomedical field.

Dataset Information

Production and Characterization of Glutathione-Chitosan Conjugate Films as Systems for Localized Release of Methotrexate.

Publications

Production and Characterization of Glutathione-Chitosan Conjugate Films as Systems for Localized Release of Methotrexate.

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