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阿米卡星负载红细胞的包封及体外评价

Encapsulation and in vitro evaluation of amikacin-loaded erythrocytes.

作者信息

Millán Carmen Gutiérrez, Castañeda Aránzazu Zarzuelo, López Francisco González, Marinero María Luisa Sayalero, Lanao José M, Arévalo Miguel

机构信息

Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Salamanca, Salamanca, Spain.

出版信息

Drug Deliv. 2005 Nov-Dec;12(6):409-16. doi: 10.1080/10717540590968909.

Abstract

The aim of our present work was to establish the effect of the osmolality of the hypotonic buffer on the encapsulated amount and the in vitro properties of Amikacin-loaded erythrocytes. Amikacin was encapsulated in rat erythrocytes using a hypotonic dialysis method with hypotonic buffers of different osmolalities with mean values around 90 and 150 mOsm/kg. Morphological examination of the ghost erythrocytes was accomplished using scanning electron microscopy (SEM). The osmotic fragility of normal and loaded erythrocytes was tested using hypotonic solutions. Evaluation of the hematological parameters of the control and loaded erythrocytes was carried out using a hematology system analyzer. Amikacin release from loaded erythrocytes was tested in autologous plasma at 37 degrees C over a 24-h period. The quantification of Amikacin in loaded erythrocytes and in autologous plasma was performed using an HPLC technique. A higher osmotic fragility of loaded erythrocytes was observed using a low osmolality buffer. Some hematological parameters showed statistically significant differences between the loaded erythrocytes obtained using two buffers of different osmolalities with respect to untreated erythrocytes. According to our results, Amikacin carrier erythrocytes obtained by hypotonic dialysis using a low osmolality buffer (90 mOsm/kg) should afford a good encapsulation yield, appropriate morphological properties, and sustained release in vitro.

摘要

我们目前工作的目的是确定低渗缓冲液的渗透压对载阿米卡星红细胞的包封量及体外性质的影响。采用低渗透析法,使用平均值约为90和150 mOsm/kg的不同渗透压的低渗缓冲液,将阿米卡星包封于大鼠红细胞中。利用扫描电子显微镜(SEM)对空壳红细胞进行形态学检查。使用低渗溶液测试正常红细胞和载药红细胞的渗透脆性。使用血液学系统分析仪评估对照红细胞和载药红细胞的血液学参数。在37℃下于自体血浆中对载药红细胞的阿米卡星释放进行24小时测试。使用HPLC技术对载药红细胞和自体血浆中的阿米卡星进行定量。使用低渗缓冲液时,观察到载药红细胞具有较高的渗透脆性。在使用两种不同渗透压缓冲液获得的载药红细胞与未处理红细胞之间,一些血液学参数显示出统计学上的显著差异。根据我们的结果,通过使用低渗缓冲液(90 mOsm/kg)进行低渗透析获得的载阿米卡星红细胞应具有良好的包封率、合适的形态学性质及体外缓释性能。

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