Evaluation of the clearance characteristics of bioadhesive systems in humans
Evaluation of the clearance characteristics of bioadhesive systems in humans
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DOI：
10.1016/s0378-5173(98)00367-6
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发表时间：
1999-02-01
影响因子：
5.8
通讯作者：
Illum, L
中科院分区：
文献类型：
--
作者：
Soane, RJ;Frier, M;Illum, L
本文介绍了三种生物黏附鼻腔给药系统的特性、放射性标记和清除特性；淀粉微球、壳聚糖微球及壳聚糖溶液。人类志愿者经鼻给药后，用伽马闪烁成像技术评估50%的这些生物粘合剂材料和对照材料从鼻腔中清除所需的时间。数据显示，对照物被迅速清除，半衰期为21分钟，而生物粘合剂输送系统的半衰期要长得多。壳聚糖溶液的半衰期几乎翻了一番，达到41分钟，而淀粉微球的半衰期增加了两倍多，达到68分钟，壳聚糖微球的半衰期增加了四倍，达到84分钟。从本研究报告的结果可以确定壳聚糖体系和淀粉微球都具有良好的生物粘附特性。这些结果支持了壳聚糖递送系统可以降低鼻腔清除率的假设，从而增加了递送系统与鼻黏膜的接触时间，为增加纳入这些系统的药物的生物利用度提供了潜力。(C) 1999 Elsevier Science B.V.版权所有
This paper describes the characterisation, radiolabelling and clearance characteristics of three bioadhesive nasal delivery systems; starch microspheres, chitosan microspheres and chitosan solution. The time taken for 50% of these bioadhesive materials and a control to be cleared from the nasal cavity, after nasal administration to human volunteers, was evaluated using gamma scintigraphy. The data show that the control was cleared rapidly, with a half life of 21 min, whereas the bioadhesive delivery systems had much longer half lives. The clearance of the chitosan solution almost doubled to 41 min, whilst the half life of clearance for the starch microspheres more than tripled to 68 min and for the chitosan microspheres the half life of clearance quadrupled to 84 min. From the results reported in this study it is possible to determine that both chitosan systems and the starch microspheres have good bioadhesive characteristics. The results have supported the hypothesis that chitosan delivery systems can reduce the rate of clearance from the nasal cavity, thereby increasing the contact time of the delivery system with the nasal mucosa, providing the potential for increasing the bioavailability of drugs incorporated into these systems. (C) 1999 Elsevier Science B.V. All rights reserved.