前往化源商城

AAPS PharmSciTech 2015-02-01

Development and characterization of mixed niosomes for oral delivery using candesartan cilexetil as a model poorly water-soluble drug.

Zerrin Sezgin-Bayindir, Mustafa Naim Antep, Nilufer Yuksel

文献索引:AAPS PharmSciTech 16(1) , 108-17, (2015)

全文:HTML全文

摘要

The aim of this study was to prepare candesartan cilexetil-loaded niosomes and mixed niosomes to enhance the aqueous solubility of the drug, thus improving its oral bioavailability. The formulations were prepared using various types and combinations of surfactants, copolymers, and charge-inducing agents. The candesartan cilexetil entrapment efficiency, particle size, and zeta potential of these niosomes varied within the range of 99.06 ± 1.74 to 36.26 ± 2.78, 157.3 ± 3.3 to 658.3 ± 12.7 nm, and -14.7 ± 2.8 to -44.5 ± 1.5 mV, respectively. The in vitro drug release from niosomes was improved after niosomal entrapment compared to pure candesartan cilexetil. The sedimentation behavior study and formulation stability tests against bile salt revealed that mixed niosomes prepared by combining Span 60 and Pluronic P85 demonstrated better stability. The differential scanning calorimetry analysis showed the conversion of crystal structure of candesartan cilexetil to the soluble amorphous form after niosomal encapsulation which induced the drug release. Consequently, oral drug delivery by Span 60/Pluronic P85-mixed niosomes seems feasible due to enhanced drug release and stability.

相关化合物

结构式 名称/CAS号 全部文献
异丙醇 结构式 异丙醇
CAS:67-63-0
氯化钠 结构式 氯化钠
CAS:7647-14-5
十八胺 结构式 十八胺
CAS:124-30-1
甲醇 结构式 甲醇
CAS:67-56-1
胆固醇 结构式 胆固醇
CAS:57-88-5
磷酸二氢钾 结构式 磷酸二氢钾
CAS:7778-77-0
去氧胆酸钠 结构式 去氧胆酸钠
CAS:302-95-4
氯化钠-35cl 结构式 氯化钠-35cl
CAS:20510-55-8
坎地沙坦酯 结构式 坎地沙坦酯
CAS:145040-37-5
双十六烷基磷酸 结构式 双十六烷基磷酸
CAS:2197-63-9