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
相关论文
共 50 条
  • [31] Hydrogel-Based Drug Delivery Systems for Poorly Water-Soluble Drugs
    McKenzie, Matthew
    Betts, David
    Suh, Amy
    Bui, Kathryn
    Kim, London Doyoung
    Cho, Hyunah
    [J]. MOLECULES, 2015, 20 (11) : 20397 - 20408
  • [32] Gastrointestinal lipolysis of lipid-based excipients intended for the oral drug delivery of poorly water-soluble drugs
    Fernandez, Sylvie
    Carriere, Frederic
    Jannin, Vincent
    [J]. OCL-OILSEEDS AND FATS CROPS AND LIPIDS, 2010, 17 (04) : 259 - 263
  • [33] Improved oral bioavailability of poorly water-soluble indirubin by a supersaturatable self-microemulsifying drug delivery system
    Chen, Zhi-Qiang
    Liu, Ying
    Zhao, Ji-Hui
    Wang, Lan
    Feng, Nian-Ping
    [J]. INTERNATIONAL JOURNAL OF NANOMEDICINE, 2012, 7 : 1115 - 1125
  • [34] Coaxial Electrospray Formulations for Improving Oral Absorption of a Poorly Water-Soluble Drug
    Zhang, Shaoling
    Kawakami, Kohsaku
    Yamamoto, Marina
    Masaoka, Yoshie
    Kataoka, Makoto
    Yamashita, Shinji
    Sakuma, Shinji
    [J]. MOLECULAR PHARMACEUTICS, 2011, 8 (03) : 807 - 813
  • [35] Enhancement of oral bioavailability of the poorly water-soluble drug silybin by sodium cholate/phospholipid-mixed micelles
    Yu, Jiang-nan
    Zhu, Yuan
    Wang, Li
    Peng, Min
    Tong, Shan-shan
    Cao, Xia
    Qiu, Hui
    Xu, Xi-ming
    [J]. ACTA PHARMACOLOGICA SINICA, 2010, 31 (06) : 759 - 764
  • [36] Enhancement of oral bioavailability of the poorly water-soluble drug silybin by sodium cholate/phospholipid-mixed micelles
    Jiang-nan Yu
    Yuan Zhu
    Li Wang
    Min Peng
    Shan-shan Tong
    Xia Cao
    Hui Qiu
    Xi-ming Xu
    [J]. Acta Pharmacologica Sinica, 2010, 31 : 759 - 764
  • [37] A DELIVERY DEVICE CONTAINING A POORLY WATER-SOLUBLE DRUG IN A HYDROPHOBIC MEDIUM - RUMINAL DELIVERY APPLICATION
    THOMBRE, AG
    CARDINAL, JR
    FOURNIER, LA
    [J]. JOURNAL OF CONTROLLED RELEASE, 1992, 18 (03) : 221 - 234
  • [38] Development and Characterization of a Biocompatible Soybean Oil-Based Microemulsion for the Delivery of Poorly Water-Soluble Drugs
    Aloisio, Carolina
    Longhi, Marcela R.
    De Oliveira, Anselmo Gomes
    [J]. JOURNAL OF PHARMACEUTICAL SCIENCES, 2015, 104 (10) : 3535 - 3543
  • [39] Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability
    Krstic, Marko
    Popovic, Miljana
    Dobricic, Vladimir
    Ibric, Svetlana
    [J]. MOLECULES, 2015, 20 (08) : 14684 - 14698
  • [40] Design and characterization of a surfactant-enriched tablet formulation for oral delivery of a poorly water-soluble immunosuppressive agent
    Ruddy, SB
    Matuszewska, BK
    Grim, YA
    Ostovic, D
    Storey, DE
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1999, 182 (02) : 173 - 186