RESUMO
Azo polymeric hydrogels were developed for colon specific targeting. Methacryloyloxy azobenzene was synthesized and hydrogels were prepared by copolymerizing with hydroxyethyl methacrylate. These hydrogels were characterized by various spectral techniques such as Fourier transform infrared spectroscopy, thermogravimetric analysis and scanning electron microscopy. Equilibrium swelling measurements of the hydrogels were carried out in distilled water and also in simulated gastric and intestinal fluids. The in vitro release studies of the incorporated 5-flurouracil were carried out in simulated gastric and intestinal fluids. The in vitro release profiles of the drug were also obtained in the presence of azoreductase in the culture of intestinal flora. The release was faster and almost followed a zero order pattern. This can be attributed to the cleavage of the azo crosslinks in the hydrogel by the azoreductase and the release of the entrapped drug at the site of targeting i.e., colon.
Assuntos
Compostos Azo/química , Colo/metabolismo , Sistemas de Liberação de Medicamentos , Metacrilatos/química , Polímeros/síntese química , Bactérias Anaeróbias/metabolismo , Materiais Biocompatíveis/normas , Colo/efeitos dos fármacos , Fezes/química , Fluoruracila/metabolismo , Géis/normas , Humanos , Técnicas In Vitro , Microscopia Eletrônica de Varredura , Polímeros/química , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
A simple method of converting the calcium carbonate skeleton of the corals available in the Indian coast into hydroxyapatite granules has been developed. By heating the coral to 900 degrees C, the organic materials were eliminated. Powder X-ray diffraction analysis (XRD), Fourier transform infrared spectroscopy (FTIR) and thermogravimetric analysis (TGA) were employed to characterize the coral and to optimize the processing parameters as well as to confirm the hydroxyapatite formation. The coral used exhibits the presence of both aragonite and calcite phases (dimorphism). At a temperature of 900 degrees C the coral was found to decompose all the carbonate phases. The pre-heated coral is converted into hydroxyapatite by a chemical exchange reaction with di-ammonium phosphate under hydrothermal conditions. The hydroxyapatite obtained was in powder form and does not contain any impurities. The in vitro solubility test of the apatite granules performed in Gomoris, Michalelis, Sorensens, Ringer's and phosphate buffer of pH 7.2 and de-ionized water indicated the stability of the coralline hydroxyapatite.
Assuntos
Cnidários/química , Hidroxiapatitas/síntese química , Animais , Carbonato de Cálcio/química , Análise de Fourier , Concentração de Íons de Hidrogênio , Hidroxiapatitas/química , Hidroxiapatitas/metabolismo , Técnicas In Vitro , Índia , Solubilidade , Temperatura , Difração de Raios XRESUMO
Biocompatible and biodegradable pH-responsive hydrogels based on N-vinyl pyrrolidone (NVP), polyethylene glycol diacrylate (PAC) and chitosan were prepared for controlled drug delivery. These interpolymeric hydrogels were synthesized by a free radical polymerization technique using azobisisobutyronitrile (AIBN) as initiator and N,N'-methylenebisacrylamide (BIS) as crosslinker. These hydrogels were subjected to equilibrium swelling studies in enzyme-free simulated gastric and intestinal fluids (SGF and SIF). These swelling studies clearly indicated that these hydrogels were swollen more in SGF when compared to SIF. Theophylline and 5-fluorouracil (5-FU) were entrapped into these hydrogels and equilibrium-swelling studies were carried out for the drug-entrapped gels in enzyme-free SGF and SIF. The in-vitro release profiles of the drugs were established in enzyme-free SGF. More than 50% of the entrapped drugs were released in the first 2 h at gastric pH and the rest of the drug release was slower.