CLX (celecoxib) is a highly hydrophobic non-steroidal anti-inflammatory drug with high plasma protein binding. We describe here the encapsulation of CLX in MLVs (multilamellar vesicles) composed of DSPC (1,2-distearoyl-sn-glycero-3-phosphocholine) and variable amounts of cholesterol. The effects of cholesterol content on liposome size, percentage drug loading and in vitro drug release profiles were investigated. Differential scanning calorimetry and FTIR (Fourier-transform infrared) spectroscopy were used to determine molecular interactions between CLX, cholesterol and DSPC. The phase transition temperature (Tm) of vesicles was reduced in a synergistic manner in the presence of both CLX and cholesterol. Encapsulation efficiency, loading and release of CLX decreased with increasing cholesterol content. FTIR results indicated that this decrease was due to a competition between CLX and cholesterol for the co-operativity region of the phospholipids. In the presence of cholesterol, CLX was pushed further into the hydrophobic core of the bilayer. However, MLVs prepared with DSPC only (without cholesterol) exhibited the lowest ability for drug retention after 72 h. Our results indicated that CLX, without the requirement of modifications to enhance solubilization, can be encapsulated and released from liposomal formulations. This method of drug delivery may be used to circumvent the low bioavailability and systemic side effects of oral CLX formulations.
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Research Article|
June 03 2010
Celecoxib-loaded liposomes: effect of cholesterol on encapsulation and in vitro release characteristics
Asli Deniz;
Asli Deniz
1
*Department of Biotechnology, Middle East Technical University, Ankara 06531, Turkey
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Asli Sade;
Asli Sade
1
†Department of Biological Sciences, Middle East Technical University, Ankara 06531, Turkey
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Feride Severcan;
Feride Severcan
*Department of Biotechnology, Middle East Technical University, Ankara 06531, Turkey
†Department of Biological Sciences, Middle East Technical University, Ankara 06531, Turkey
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Dilek Keskin;
Dilek Keskin
*Department of Biotechnology, Middle East Technical University, Ankara 06531, Turkey
‡Department of Engineering Sciences, Middle East Technical University, Ankara 06531, Turkey
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Aysen Tezcaner;
Aysen Tezcaner
*Department of Biotechnology, Middle East Technical University, Ankara 06531, Turkey
‡Department of Engineering Sciences, Middle East Technical University, Ankara 06531, Turkey
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Sreeparna Banerjee
Sreeparna Banerjee
2
*Department of Biotechnology, Middle East Technical University, Ankara 06531, Turkey
†Department of Biological Sciences, Middle East Technical University, Ankara 06531, Turkey
2To whom any correspondence should be addressed (email banerjee@metu.edu.tr).
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Publisher: Portland Press Ltd
Received:
July 31 2009
Revision Received:
October 21 2009
Accepted:
November 10 2009
Accepted Manuscript online:
November 10 2009
Online ISSN: 1573-4935
Print ISSN: 0144-8463
© The Authors Journal compilation © 2010 Biochemical Society
2010
Biosci Rep (2010) 30 (5): 365–373.
Article history
Received:
July 31 2009
Revision Received:
October 21 2009
Accepted:
November 10 2009
Accepted Manuscript online:
November 10 2009
Citation
Asli Deniz, Asli Sade, Feride Severcan, Dilek Keskin, Aysen Tezcaner, Sreeparna Banerjee; Celecoxib-loaded liposomes: effect of cholesterol on encapsulation and in vitro release characteristics. Biosci Rep 1 October 2010; 30 (5): 365–373. doi: https://doi.org/10.1042/BSR20090104
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