Purpose: Evaluation of the rheological, biological and therapeutic properties of a new topical formulation consisting of chitosan gel containing 1% silver sulfadiazine, as an alternative for the treatment of burn wounds. Methods: An experimental study was done with 21 Wistar rats divided into three groups. Group I was treated with chitosan gel without the antimicrobial, group II was treated with chitosan gel with 1% silver sulfadiazine and group III was treated with commercially available 1% silver sulfadiazine cream. Results: Due to its pseudoplastic characteristic and good bioadhesiveness, the chitosan gels showed a satisfactory retention time over the wounds. No statistical difference was found in the amount of drug released from the chitosan gel and commercially available cream, as well as in the healing time among the groups. Wounds treated with chitosan gel with silver sulfadiazine showed a higher fibroblast production and a better angiogenesis than in the other groups, which are important parameters on the evolution of the healing process. Conclusion: The topical use of chitosan gel in association with silver sulfadiazine ameliorated the neovascularization and inflammatory reaction in burn wounds. This new formulation showed advantageous rheological properties and efficient release of the drug. Key words: Chitosan. Silver Sulfadiazine. Gel. Wound Healing. Rats. RESUMOObjetivo: Avaliar as propriedades reológicas, biológicas e terapêuticas de uma nova formulação de uso tópico, a partir de um gel de quitosana, contendo sulfadiazina de prata a 1%, no tratamento de queimaduras. Métodos: Foi realizado estudo experimental com 21 ratos Wistar distribuídos em três grupos de sete animais. As queimaduras dos animais do grupo I foram tratadas com gel de quitosana sem antimicrobiano, o grupo II foi tratado com gel de quitosana contendo sulfadiazina de prata 1% e o grupo III foi tratado com creme de sulfadiazina de prata 1%, comumente utilizado no tratamento de queimados. Resultados: Devido às características pseudoplásticas e à boa bioadesividade, os géis de quitosana apresentaram um tempo de retenção satisfatório sobre as feridas. A liberação da sulfadiazina de prata, bem como o tempo de cicatrização, não foram estatisticamente diferentes. Feridas tratadas com o gel de quitosana contendo sulfadiazina de prata apresentaram uma maior produção de fibroblastos e uma melhor angiogênese, comparando-se com os outros grupos, fatores que indicaram uma maior evolução no processo de cicatrização. Conclusão: O uso tópico do gel de quitosana com sulfadiazina de prata a 1% melhorou a neovascularização e a reação inflamatória em queimaduras e essa nova formulação mostrou boas propriedades reológicas associadas a eficiente liberação do fármaco. Descritores: Quitosana. Sulfadiazina de prata. Cicatrização de Feridas. Ratos.

Cationic polymeric nanoparticles (NPs) have the ability to overcome biological membranes, leading to improved efficacy of anticancer drugs. The modulation of the particle-cell interaction is desired to control this effect and avoid toxicity to normal cells. In this study, we explored the surface functionalization of cationic polymethylmethacrylate (PMMA) NPs with two natural compounds, sialic acid (SA) and cholesterol (Chol). The performance of benznidazole (BNZ) was assessed in vitro in the normal renal cell line (HEK-293) and three human cancer cell lines, as follows: human colorectal cancer (HT-29), human cervical carcinoma (HeLa), and human hepatocyte carcinoma (HepG2). The structural properties and feasibility of NPs were evaluated and the changes induced by SA and Chol were determined by using multiple analytical approaches. Small (<200 nm) spherical NPs, with a narrow size distribution and high drug-loading efficiency were prepared by using a simple and reproducible emulsification solvent evaporation method. The drug interactions in the different self-assembled NPs were assessed by using Fourier transform-infrared spectroscopy. All formulations exhibited a slow drug-release profile and physical stability for more than 6 weeks. Both SA and Chol changed the kinetic properties of NPs and the anticancer efficacy. The feasibility and potential of SA/Chol-functionalized NPs has been demonstrated in vitro in the HEK-293, HepG2, HeLa, and HT-29 cell lines as a promising system for the delivery of BNZ.

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Chitosan is a natural copolymer generally available in pharmaceutical and food powders associated with drugs, vitamins, and nutraceuticals. This study focused on monitoring the effect of the morphology and structural features of the chitosan particles for controlling the release profile of the active pharmaceutical ingredient (API) propranolol hydrochloride. Chitosan with distinct molecular mass (low and medium) were used in the formulations as crystalline and irregular particles from commercial raw material, or as spherical, uniform, and amorphous spray-dried particles. The API–copolymer interactions were assessed when adding the drug before (drug-loaded particles) or after the spray drying (only mixed with blank particles). The formulations were further compared with physical mixtures of the API with chitin and microcrystalline cellulose. The scanning electron microscopy (SEM) images, surface area, particle size measurements, X-ray diffraction (XRD) analysis and drug loading have supported the drug release behavior. The statistical analysis of experimental data demonstrated that it was possible to control the drug release behavior (immediate or slow drug release) from chitosan powders using different types of particles.

Federal do Rio Grande do Norte -CP 1662 -59078-970 -Natal -RN Recebido em 1/9/98; aceito em 28/4/99 THE STUDY OF INFLUENCE OF CROSSLINKING AND ORGANIC ADDITIVES ON THE BEHAVIOR OF CHITOSAN GELS. The physical-chemical process of swelling in water-based gel of natural polymers is investigated with the purpose of applying these systems to biomedical materials for controlled release of drugs. In this work we develop a study about the sol-gel transition of solutions of chitosan in the presence of formaldehyde and glutaraldehyde like crosslinking agents and we have determined the effect of many aditives in the time of gelification from the elaborated sistems. The phisical-chemistry process of swelling of the formed gels was evaluated in function of the degree of crosslinking of the incorporated aditives and the pH. Gelling times of chitosan solutions were obtained using viscosimetric measurement, in the pre-gel state, as well as condutivity ones.The results obtained suggest that component concentration modifies the kinetic profile of the transition and the swelling behavior. Regarding H+ content, the gels were highly susceptible to swelling in acidic conditions, which characterize this system as pH -sensitive.