Development and Characterization of Mixed Niosomes for Oral Delivery Using Candesartan Cilexetil as a Model Poorly Water-Soluble Drug

被引:74
|
作者
Sezgin-Bayindir, Zerrin [1 ]
Antep, Mustafa Naim [1 ]
Yuksel, Nilufer [1 ]
机构
[1] Ankara Univ, Dept Pharmaceut Technol, Fac Pharm, TR-06100 Ankara, Turkey
来源
AAPS PHARMSCITECH | 2015年 / 16卷 / 01期
关键词
in vitro drug release; niosomes; oral drug delivery; stability; surfactants; IN-VITRO; POLYMERIC NANOPARTICLES; STABILITY; VESICLES; LIPOSOMES; PH; FORMULATION; PACLITAXEL; SYSTEMS;
D O I
10.1208/s12249-014-0213-9
中图分类号
R9 [药学];
学科分类号
1007 ;
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.
引用
收藏
页码:108 / 117
页数:10
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