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1.
Pharmaceutics ; 15(12)2023 Nov 21.
Artigo em Inglês | MEDLINE | ID: mdl-38139991

RESUMO

Papain (an enzyme from the latex of Carica papaya) is an interesting natural bioactive macromolecule used as therapeutic alternative for wound healing due to debridement action in devitalized or necrotic tissues. However, its use in high doses can induce potential skin irritation and side effects. In this study, experiments explored the ability of chitosan membrane to immobilize papain, consequently improving enzymatic activity and controlling enzyme release. Papain-loading capacity was tested via experiments of force microscopy (AFM), scanning electron microscopy (SEM-FEG), and X-ray diffraction analyses. Fourier transform infrared spectroscopy and thermal analyses assessed the enzyme interactions with the copolymer. The investigation of the feasibility of membranes included pH on the surface, elasticity, and breaking strength measurements. The surface wettability and swelling capacity of different formulations revealed the best formulation for in vitro papain release experiments. The membranes had a transparent, rough, crystalline characteristic, which was homogeneous with the membrane within the neutrality. The immobilization of papain in the chitosan membrane resulted in a decrease in the vibration band characteristic of pure papain, suggesting a displacement in the vibration bands in the FTIR spectrum. The presence of papain decreased hydrophobicity on the surface of the membrane and disturbed the membrane's ability to swell. Chitosan membranes containing papain 2.5% (0.04 g) and 5.0% (0.08 g) preserved feasible properties and improved the enzymatic activity compared (0.87 ± 0.12 AU/mg and 1.59 ± 0.10 AU/mg) with a free papain sample (0.0042 ± 0.001 AU/mg). Concentrations of over 10% (0.16 g) led to phase separation into membranes. Chitosan membranes exhibited a slow papain release behavior adjusted via the Higushi model. The experimental achievements suggest a novel and promising method for the enhancement of papain. The results indicate the potential for prolonged bioactivity for use on wounds.

2.
Mater Sci Eng C Mater Biol Appl ; 78: 978-987, 2017 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-28576075

RESUMO

Several polymers have been investigated for producing cationic nanocarriers due to their ability to cross biological barriers. Polycations such as copolymers of polymethylmethacrylate are highlighted due to their biocompatibility and low toxicity. The purpose of this study was to produce small and narrow-sized cationic nanoparticles able to overcome cell membranes and improve the biological activity of benznidazole (BNZ) in normal and cancer cells. The effect of composition and procedure parameters of the used emulsification-solvent evaporation method were controlled for this purpose. The experimental approach included particle size, polydispersity index, zeta potential, atomic force microscopy (AFM), attenuated total reflectance Fourier transforms infrared spectroscopy (ATR- FTIR), drug loading efficiency, and physical stability assays. Spherical and stable (over six weeks) sub 150nm cationic nanoparticles were optimized, with the encapsulation efficiency >80%. The used drug/copolymer ratio modulated the slow drug release, which was adjusted by the parabolic diffusion mathematical model. In addition, the ability of the cationic nanoparticles improve the BNZ uptake in the normal kidney cells (HEK 293) and the human colorectal cancer cells (HT 29) demonstrate that this novel BNZ-loaded cationic has great potential as a chemotherapeutic application of benznidazole.


Assuntos
Nanopartículas , Portadores de Fármacos , Liberação Controlada de Fármacos , Células HEK293 , Humanos , Nitroimidazóis , Tamanho da Partícula
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