title: Development and characterization of mixed niosomes for oral delivery using candesartan cilexetil as a model poorly water-soluble drug.
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.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, 06100, Tandogan, Ankara, Turkey, zsezgin@pharmacy.ankara.edu.tr.
authors.forename: Zerrin
authors.initials: Z
authors.lastname: Sezgin-Bayindir
authors.forename: Mustafa Naim
authors.initials: MN
authors.lastname: Antep
authors.forename: Nilufer
authors.initials: N
authors.lastname: Yuksel
mesh_terms: D000284:Administration, Oral; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000737:chemistry; D001562:Benzimidazoles / Q000008:administration & dosage* / Q000737:chemistry*; D001713:Biphenyl Compounds / Q000008:administration & dosage* / Q000737:chemistry*; D004058:Diffusion; D004339:Drug Compounding / Q000379:methods; D004355:Drug Stability; D057927:Hydrophobic and Hydrophilic Interactions; D008081:Liposomes / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry*; D013777:Tetrazoles / Q000008:administration & dosage* / Q000737:chemistry*; D014867:Water / Q000737:chemistry*
chemical_list: D000959:Antihypertensive Agents; D001562:Benzimidazoles; D001713:Biphenyl Compounds; D008081:Liposomes; D013501:Surface-Active Agents; D013777:Tetrazoles; D014867:Water; C077793:candesartan cilexetil