关键词: drug loading and releasing inhibiting zone porous chitosan/hydroxyapatite microspheres vancomycin

来  源:   DOI:10.3390/pharmaceutics16060730   PDF(Pubmed)

Abstract:
Porous chitosan/hydroxyapatite (Chi-HAp) composite microspheres were prepared in an aqueous solution containing chitosan, calcium nitrate, and ammonium dihydrogen phosphate by using a hydrothermal method at various temperatures. The investigation indicated that temperature significantly impacted the final product\'s appearance. Hydroxyapatite (HAp) coupled with dicalcium phosphate dihydrate (DCPD) flakes were obviously found at 65 and 70 °C, while the latter gradually disappeared at higher temperatures. Conversely, synthesis at 90 °C led to smaller particle sizes due to the broken chitosan chains. The microspheres synthesized at 75 °C were selected for further analysis, revealing porous structures with specific surface areas of 36.66 m2/g, pores ranging from 3 to 100 nm, and pore volumes of 0.58 cm3/g. Vancomycin (VCM), an antibiotic, was then absorbed on and released from the microspheres derived at 75 °C, with a drug entrapment efficiency of 20% and a release duration exceeding 20 days. The bacteriostatic activity of the VCM/composite microspheres against Staphylococcus aureus increased with the VCM concentration and immersion time, revealing a stable inhibition zone diameter of approximately 4.3 mm from 24 to 96 h, and this indicated the retained stability and efficacy of the VCM during the encapsulating process.
摘要:
在含壳聚糖的水溶液中制备了多孔壳聚糖/羟基磷灰石(Chi-HAp)复合微球,硝酸钙,和磷酸二氢铵在不同温度下使用水热法。调查表明,温度显著影响最终产品的外观。在65和70°C下明显发现了羟基磷灰石(HAp)与二水合磷酸二钙(DCPD)薄片的偶联,而后者在较高温度下逐渐消失。相反,在90°C下的合成由于断裂的壳聚糖链导致更小的粒度。选择在75°C下合成的微球进行进一步分析,显示比表面积为36.66m2/g的多孔结构,孔范围从3到100纳米,孔体积为0.58cm3/g。万古霉素(VCM),抗生素,然后在75°C下从微球上吸收并释放,药物包封率为20%,释放持续时间超过20天。VCM/复合微球对金黄色葡萄球菌的抑菌活性随VCM浓度和浸泡时间的增加而增加,在24至96小时内,发现稳定的抑制区直径约为4.3毫米,并且这表明在封装过程中VCM的保留稳定性和功效。
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