CAJ | 학술논문

目的制备万古霉素阳离子脂质体(CLV)复合的纳米羟基磷灰石/壳聚糖/魔芋葡苷聚糖(n-HA/CS/KGM)支架,探讨其在模拟体液中的释放特性. 方法采用逆向蒸发法制备CLV,将其与n-HA/CS/KGM支架复合,并在扫描电镜下观察复合支架中CLV的形态;采用中国药典推荐的方法Ⅲ溶出装置,研究CLV体外从支架释放的性质和特点,以及6种不同CLV和KGM含量对支架释药行为的影响. 结果扫描电镜观察显示:CLV复合n-HA/CS/KGM支架完整保存了CLV的结构,首先从支架中释放的主要是CLV而不是游离药物;CLV从支架中释放1h内可以观察到“爆释”现象,整个释放过程可以用基于Frutos等提出的数学模型的改良公式进行良好模拟.无论是KGM还是CLV在支架中的含量对支架的释放行为均有显著影响:当加入CLV的量未达到饱和之前,随着KGM成分的增加或CLV成分的减少,CLV的释放率和释放量都可显著减少,差异有统计学意义(P＜0.05). 结论通过调整支架中KGM和(或)CLV成分的含量,可以得到不同释放速率和释放药物比率的复合支架,可满足临床应用的不同需要.
목적 제비만고매소양리자지질체(CLV)복합적납미간기린회석/각취당/마우포감취당(n-HA/CS/KGM)지가,탐토기재모의체액중적석방특성. 방법 채용역향증발법제비CLV,장기여n-HA/CS/KGM지가복합,병재소묘전경하관찰복합지가중CLV적형태;채용중국약전추천적방법Ⅲ용출장치,연구CLV체외종지가석방적성질화특점,이급6충불동CLV화KGM함량대지가석약행위적영향. 결과 소묘전경관찰현시:CLV복합n-HA/CS/KGM지가완정보존료CLV적결구,수선종지가중석방적주요시CLV이불시유리약물;CLV종지가중석방1h내가이관찰도“폭석”현상,정개석방과정가이용기우Frutos등제출적수학모형적개량공식진행량호모의.무론시KGM환시CLV재지가중적함량대지가적석방행위균유현저영향:당가입CLV적량미체도포화지전,수착KGM성분적증가혹CLV성분적감소,CLV적석방솔화석방량도가현저감소,차이유통계학의의(P＜0.05). 결론 통과조정지가중KGM화(혹)CLV성분적함량,가이득도불동석방속솔화석방약물비솔적복합지가,가만족림상응용적불동수요.
Objective To design a novel artificial bone scaffold and investigate its release properties in simulated body fluid.Methods Cationic liposomal vancomycin (CLV) was prepared by a modified reverse phase evaporation method.Porous nano-hydroxyapatite/chitosan/konjac glucomannan (n-HA/CS/KGM) scaffolds were loaded with CLV to form a novel complex drug carrier (LLS).Scanning electron microscopy was used to determine the microstructures of LLS.A type Ⅲ Chinese Pharmacopoeia dissolution apparatus was used in the drug release studies.The kinetics of CLV release from LLS and the effects of 6 different amounts of konjac glucomannan (KGM) and CLV in LLS were examined in vitro.Results Electron microscopy indicated that the liposomes were well preserved in the scaffolds,and that CLV rather than free vancomycin was released from the scaffolds.An initial burst effect was observed at the first hour.The whole process of CLV release could be well simulated on the basis of a modified Frutos' equation.The weight percentage of KGM or CLV greatly influenced the release behavior of the scaffolds.Before saturation of the CLV added,increase of KGM or decease of CLV significantly reduced release of the CLV (P ＜ 0.05).Conclusion By adjusting the ratio of KGM/CLV,which significantly influenced the release rate of CLV,we successfully prepared customized scaffolds whose different release rates might satisfy diverse therapy requirements.