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In situ niosome forming maltodextrin proniosomes of candesartan cilexetil: In vitro and in vivo evaluations.
Int J Biol Macromol. 2016 Jan; 82:453-63.IJ

Abstract

The aim of this study is to develop novel proniosomal tablets of candesartan cilexetil. Drug loaded proniosomes were prepared as dry powder by slurry method. The critical parameters of the production process were the type of the carrier (sorbitol, maltodextrin, and lactose), addition of charge inducers, rotation speed of the rotavapor and solvent evaporation temperature. The effects of these parameters on proniosome specifications such as the recovery, drug loading, drug release were investigated and also the influence on the particle size and surface charge of the niosomes derived by the hydration of proniosomes were evaluated. The mean particle size and drug loading of niosomes formed from the hydrated proniosomes were 204 ± 2 nm and 99.09 ± 0.04% respectively, with a negative charge -43.65 ± 0.54 mV. The proniosomes demonstrated good flowability, compressibility and consolidation properties both alone and together with the tableting agents (microcrystalline cellulose and cross-linked poly vinylpyrrolidone). The niosomes derived by the hydration of proniosomal tablets preserved their initial properties. Compatibly with the increased in vitro drug dissolution rate, the relative bioavailability of drug from proniosomal tablets increased 1.86-fold and 2.75-fold and higher candesartan plasma levels were achieved within shorter time compared to the pure drug.

Authors+Show Affiliations

Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey. Electronic address: nyuksel@pharmacy.ankara.edu.tr.Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey.Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey.Department of Pharmacology, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26455402

Citation

Yuksel, Nilufer, et al. "In Situ Niosome Forming Maltodextrin Proniosomes of Candesartan Cilexetil: in Vitro and in Vivo Evaluations." International Journal of Biological Macromolecules, vol. 82, 2016, pp. 453-63.
Yuksel N, Bayindir ZS, Aksakal E, et al. In situ niosome forming maltodextrin proniosomes of candesartan cilexetil: In vitro and in vivo evaluations. Int J Biol Macromol. 2016;82:453-63.
Yuksel, N., Bayindir, Z. S., Aksakal, E., & Ozcelikay, A. T. (2016). In situ niosome forming maltodextrin proniosomes of candesartan cilexetil: In vitro and in vivo evaluations. International Journal of Biological Macromolecules, 82, 453-63. https://doi.org/10.1016/j.ijbiomac.2015.10.019
Yuksel N, et al. In Situ Niosome Forming Maltodextrin Proniosomes of Candesartan Cilexetil: in Vitro and in Vivo Evaluations. Int J Biol Macromol. 2016;82:453-63. PubMed PMID: 26455402.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In situ niosome forming maltodextrin proniosomes of candesartan cilexetil: In vitro and in vivo evaluations. AU - Yuksel,Nilufer, AU - Bayindir,Zerrin Sezgin, AU - Aksakal,Elif, AU - Ozcelikay,A Tanju, Y1 - 2015/10/09/ PY - 2015/07/11/received PY - 2015/10/05/revised PY - 2015/10/06/accepted PY - 2015/10/13/entrez PY - 2015/10/13/pubmed PY - 2016/10/14/medline KW - Bioavailability KW - Dissolution KW - Particle size KW - Pharmacokinetics KW - Proniosomes KW - Surfactants SP - 453 EP - 63 JF - International journal of biological macromolecules JO - Int J Biol Macromol VL - 82 N2 - The aim of this study is to develop novel proniosomal tablets of candesartan cilexetil. Drug loaded proniosomes were prepared as dry powder by slurry method. The critical parameters of the production process were the type of the carrier (sorbitol, maltodextrin, and lactose), addition of charge inducers, rotation speed of the rotavapor and solvent evaporation temperature. The effects of these parameters on proniosome specifications such as the recovery, drug loading, drug release were investigated and also the influence on the particle size and surface charge of the niosomes derived by the hydration of proniosomes were evaluated. The mean particle size and drug loading of niosomes formed from the hydrated proniosomes were 204 ± 2 nm and 99.09 ± 0.04% respectively, with a negative charge -43.65 ± 0.54 mV. The proniosomes demonstrated good flowability, compressibility and consolidation properties both alone and together with the tableting agents (microcrystalline cellulose and cross-linked poly vinylpyrrolidone). The niosomes derived by the hydration of proniosomal tablets preserved their initial properties. Compatibly with the increased in vitro drug dissolution rate, the relative bioavailability of drug from proniosomal tablets increased 1.86-fold and 2.75-fold and higher candesartan plasma levels were achieved within shorter time compared to the pure drug. SN - 1879-0003 UR - https://www.unboundmedicine.com/medline/citation/26455402/In_situ_niosome_forming_maltodextrin_proniosomes_of_candesartan_cilexetil:_In_vitro_and_in_vivo_evaluations_ DB - PRIME DP - Unbound Medicine ER -