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钟家浩,姚文栋,谢先泽,徐恒武.不同部位载药可溶性微针载药量比较及体外评价[J].浙江中西医结合杂志,2023,33(6):
不同部位载药可溶性微针载药量比较及体外评价
Drug loading comparison and in vitro evaluation of different position drug-loaded dissolving microneedles
投稿时间:2022-09-23  修订日期:2022-12-20
DOI:
中文关键词:  可溶性微针  载药部位  载药量  体外评价
英文关键词:dissolving microneedle  drug loading capacity  drug-loading position  in vitro evaluation
基金项目:浙江省药学会医院药学专项科研资助项目(石药专项)(2019ZYY23),
作者单位E-mail
钟家浩 浙江中医药大学附属第一医院(浙江省中医院) 496713635@qq.com 
姚文栋 浙江中医药大学附属第一医院(浙江省中医院)  
谢先泽 浙江中医药大学附属第一医院(浙江省中医院)  
徐恒武* 浙江中医药大学附属第一医院(浙江省中医院) xuhengwu@126.com 
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中文摘要:
      目的 制备不同部位载药可溶性微针(DMN),探究其载药量并对其进行体外评价。 方法 通过两步离心法制备不同部位载药的DMN。显微镜观察DMN形态特征。然后,通过HF-50数显推拉力计测定不同部位载药DMN机械强度;HPLC测定不同部位载药的DMN载药量;Franz透皮扩散池考察不同部位载药的DMN体外透皮性能及释放趋势。 结果 所制备的三种不同部位载药DMN均为金字塔形。不同部位载药的三种DMN机械强度无显著性差异。相较于针体载药的DMN(DMN-A),背衬层载药的DMN(DMN-B)、针体与背衬层均载药的DMN(DMN-C)载药量均显著增加,分别为DMN-A的5.75、6.83倍。DMN-A透皮释放速率最快,在4 h基本释放完全;DMN-B释放速率在三者中最慢;而DMN-C释放速度介于两者之间,释放速率接近DMN-B。 结论 本研究通过对三种不同部位载药的微针评价,增加载药空间明显提高了载药量;后续设计可以改进靠近微针的前部背衬层用于载药,增加载药空间的同时避免药物的浪费。
英文摘要:
      Objective Preparing different positions drug-loaded dissolving microneedles (DMN) to explore their drug loading capacity and evaluate in vitro. Methods Different position drug-loaded dissolving microneedles were prepared by two-step centrifugation. The morphology of DMN were observed by microscope. Then, the mechanical strength of DMN were measured by HF-50 digital push-pull meter; the drug loading capacity of different positions drug-loaded DMN were determined by HPLC; the in vitro transdermal performance and release of drug-loaded DMN were investigated by Franz transdermal diffusion cell. Results The three types DMN were all pyramid-shaped. There was no significant difference in the mechanical strength of the three DMN. Compared with the drug-loaded DMN in the needle body (DMN-A), the drug-loaded DMN in the backing layer (DMN-B)、the DMN in both the needle body and the backing layer (DMN-C) were significantly increased in drug loading capacity, which were 5.75 and 6.83 times that of DMN-A, respectively. The transdermal release of DMN-A was the fastest, and the release rate was basically complete in 4 h; the release rate of DMN-B was the slowest among the three DMN; the release rate of DMN-C was between the DMN-A and DMN-B, and the release rate was close to that of DMN-B. Conclusion In this study, through the evaluation of the DMN loaded with drugs in three different positions, the drug loading capacity was improved significantly by increasing the drug loading space; Subsequent designs could add the front backing layer near the needle bodies for drug loading, increasing the drug loading space and avoiding drug waste.
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