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Development and characterization of mixed niosomes for oral delivery using candesartan cilexetil as a model poorly water-soluble drug.
AAPS PharmSciTech. 2015 Feb; 16(1):108-17.AP

Abstract

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.

Authors+Show Affiliations

Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, 06100, Tandogan, Ankara, Turkey, zsezgin@pharmacy.ankara.edu.tr.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

25204859

Citation

Sezgin-Bayindir, Zerrin, et al. "Development and Characterization of Mixed Niosomes for Oral Delivery Using Candesartan Cilexetil as a Model Poorly Water-soluble Drug." AAPS PharmSciTech, vol. 16, no. 1, 2015, pp. 108-17.
Sezgin-Bayindir Z, Antep MN, Yuksel N. Development and characterization of mixed niosomes for oral delivery using candesartan cilexetil as a model poorly water-soluble drug. AAPS PharmSciTech. 2015;16(1):108-17.
Sezgin-Bayindir, Z., Antep, M. N., & Yuksel, N. (2015). Development and characterization of mixed niosomes for oral delivery using candesartan cilexetil as a model poorly water-soluble drug. AAPS PharmSciTech, 16(1), 108-17. https://doi.org/10.1208/s12249-014-0213-9
Sezgin-Bayindir Z, Antep MN, Yuksel N. Development and Characterization of Mixed Niosomes for Oral Delivery Using Candesartan Cilexetil as a Model Poorly Water-soluble Drug. AAPS PharmSciTech. 2015;16(1):108-17. PubMed PMID: 25204859.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development and characterization of mixed niosomes for oral delivery using candesartan cilexetil as a model poorly water-soluble drug. AU - Sezgin-Bayindir,Zerrin, AU - Antep,Mustafa Naim, AU - Yuksel,Nilufer, Y1 - 2014/09/10/ PY - 2014/06/05/received PY - 2014/08/26/accepted PY - 2014/9/11/entrez PY - 2014/9/11/pubmed PY - 2015/10/22/medline SP - 108 EP - 17 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 16 IS - 1 N2 - 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. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/25204859/Development_and_characterization_of_mixed_niosomes_for_oral_delivery_using_candesartan_cilexetil_as_a_model_poorly_water_soluble_drug_ L2 - https://dx.doi.org/10.1208/s12249-014-0213-9 DB - PRIME DP - Unbound Medicine ER -