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载有放射性碘化阿西美辛的非离子表面活性剂囊泡作为一种双重抗癌疗法。

Radioiodinated acemetacin loaded niosomes as a dual anticancer therapy.

作者信息

Shewaiter Mona A, Selim Adli A, Moustafa Yasser M, Gad Shadeed, Rashed Hassan M

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Sinai University, Kantara, Egypt.

Labeled Compounds Department, Hot Laboratories Center, Egyptian Atomic Energy Authority, Cairo, Egypt.

出版信息

Int J Pharm. 2022 Nov 25;628:122345. doi: 10.1016/j.ijpharm.2022.122345. Epub 2022 Oct 28.

Abstract

A niosomal formula of acemetacin was developed to improve its tumor targeting and radio-kinetic evaluation was performed using I. Niosomes were prepared by ether injection method and characterized for particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE%) and in vitro drug release. Factors affecting radiolabeling with I were studied and optimized. Radio-kinetic evaluation was done for I-ACM optimum niosomal formula by intravenous (I.V) administration to solid tumor bearing mice and compared to I.V I-ACM solution as a control. The average droplet size, zeta potential and in vitro release after 24 h for the optimum formula were 315.23 ± 5.37 nm, -9.16 ± 2.91 and 76 %, respectively. The greatest labeling yield of I-ACM was 93.1 ± 1.1 %. Radio-kinetic evaluation showed a maximum tumor uptake of 5.431 %ID/g for I-ACM niosomal formula and 2.601 %ID/g for I-ACM solution at 60 min post I.V. injection. As a conclusion, niosomal formula increased tumor uptake of ACM by passive targeting of the nanosized niosomes. In addition, chemotherapeutic effect of ACM and radiotherapeutic effect of I were successfully combined in one treatment regimen using I-ACM niosomes which could be used as a hopeful dual anticancer therapy.

摘要

开发了醋氯芬酸的非离子表面活性剂囊泡配方以提高其肿瘤靶向性,并使用碘进行了放射动力学评估。通过乙醚注入法制备了非离子表面活性剂囊泡,并对其粒径(PS)、多分散指数(PDI)、ζ电位(ZP)、包封率(EE%)和体外药物释放进行了表征。研究并优化了影响用碘进行放射性标记的因素。通过静脉注射(I.V)给荷实体瘤小鼠注射碘标记的醋氯芬酸最佳非离子表面活性剂囊泡配方进行放射动力学评估,并与I.V碘标记的醋氯芬酸溶液作为对照进行比较。最佳配方的平均液滴大小、ζ电位和24小时后的体外释放率分别为315.23±5.37nm、-9.16±2.91和76%。碘标记的醋氯芬酸的最大标记产率为93.1±1.1%。放射动力学评估显示,静脉注射后60分钟,碘标记的醋氯芬酸非离子表面活性剂囊泡配方的最大肿瘤摄取量为5.431%ID/g,碘标记的醋氯芬酸溶液为2.601%ID/g。结论是,非离子表面活性剂囊泡配方通过纳米级非离子表面活性剂囊泡的被动靶向增加了醋氯芬酸的肿瘤摄取。此外,使用碘标记的醋氯芬酸非离子表面活性剂囊泡成功地将醋氯芬酸的化疗作用和碘的放疗作用结合在一种治疗方案中,这有望成为一种双重抗癌疗法。

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