Chandy T, Sharma C P
Division of Biosurface Technology, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Trivandrum, India.
Biomaterials. 1996 Jan;17(1):61-6. doi: 10.1016/0142-9612(96)80756-3.
Ferric chloride was embedded in a chitosan matrix to develop a prolonged-release form. The in vitro release profiles of ferric ions from chitosan beads were monitored in 0.1 M Tris-HCl buffer, pH 7.4, using a UV spectrophotometer. The amount of drug release was much higher initially, followed by a constant slow release profile for a prolonged period. The initial burst release was substantially modified with liposome and albumin coatings. From scanning electron microscope studies, it appears that the ferric ions diffuse out slowly to the dissolution medium through the micropores of the chitosan matrix. Further, the liposome forms a phospholipid membrane layer in the pores of chitosan beads and encapsulates the ferric ions within their vesicles and controls the release profile. The chitosan beads loaded with ferric ions substantially inhibited the polyurethane-associated calcification, in an in vitro model system. The released ferric ions, appeared to alter the protein-surface binding and improved the biocompatibility of the matrix. The results propose the possibility of modifying the polymer matrix to obtain a desired controlled release of the drug for a prolonged period.
将氯化铁包埋于壳聚糖基质中以制成缓释剂型。使用紫外分光光度计在pH 7.4的0.1 M Tris-HCl缓冲液中监测壳聚糖珠中铁离子的体外释放曲线。药物释放量最初要高得多,随后在较长时间内呈持续缓慢释放曲线。脂质体和白蛋白包衣对最初的突释进行了实质性改良。从扫描电子显微镜研究来看,铁离子似乎通过壳聚糖基质的微孔缓慢扩散到溶解介质中。此外,脂质体在壳聚糖珠的孔隙中形成磷脂膜层,并将铁离子包裹在其囊泡内,从而控制释放曲线。在体外模型系统中,负载铁离子的壳聚糖珠显著抑制了聚氨酯相关的钙化。释放出的铁离子似乎改变了蛋白质与表面的结合,并改善了基质的生物相容性。结果表明,有可能对聚合物基质进行改良,以在较长时间内实现药物的理想控释。