Back to Journals » International Journal of Nanomedicine » Volume 7

Enhancement of the dissolution rate and bioavailability of fenofibrate by a melt-adsorption method using supercritical carbon dioxide

Authors Cha KH, Cho KJ, Kim MS, Kim JS, Park HJ, Park J, Cho W, Park JS, Hwang SJ

Received 12 August 2012

Accepted for publication 14 September 2012

Published 25 October 2012 Volume 2012:7 Pages 5565—5575

DOI https://doi.org/10.2147/IJN.S36939

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 2

Kwang-Ho Cha,1,3 Kyung-Jin Cho,3 Min-Soo Kim,4 Jeong-Soo Kim,3 Hee Jun Park,1,3 Junsung Park,1,3 Wonkyung Cho,1,3 Jeong-Sook Park,3 Sung-Joo Hwang1,2

1
Yonsei Institute of Pharmaceutical Sciences, 2College of Pharmacy, Yonsei University, Incheon, Republic of Korea; 3College of Pharmacy, Chungnam National University, Daejeon, Republic of Korea; 4Department of Pharmaceutical Engineering, Inje University, Gimhae, Republic of Korea

Background: The aim of this study was to enhance the bioavailability of fenofibrate, a poorly water-soluble drug, using a melt-adsorption method with supercritical CO2.
Methods: Fenofibrate was loaded onto Neusilin® UFL2 at different weight ratios of fenofibrate to Neusilin UFL2 by melt-adsorption using supercritical CO2. For comparison, fenofibrate-loaded Neusilin UFL2 was prepared by solvent evaporation and hot melt-adsorption methods. The fenofibrate formulations prepared were characterized by differential scanning calorimetry, powder x-ray diffractometry, specific surface area, pore size distribution, scanning electron microscopy, and energy-dispersive x-ray spectrometry. In vitro dissolution and in vivo bioavailability were also investigated.
Results: Fenofibrate was distributed into the pores of Neusilin UFL2 and showed reduced crystal formation following adsorption. Supercritical CO2 facilitated the introduction of fenofibrate into the pores of Neusilin UFL2. Compared with raw fenofibrate, fenofibrate from the prepared powders showed a significantly increased dissolution rate and better bioavailability. In particular, the area under the drug concentration-time curve and maximal serum concentration of the powders prepared using supercritical CO2 were 4.62-fold and 4.52-fold greater than the corresponding values for raw fenofibrate.
Conclusion: The results of this study highlight the usefulness of the melt-adsorption method using supercritical CO2 for improving the bioavailability of fenofibrate.

Keywords: fenofibrate, melt adsorption, supercritical CO2, bioavailability

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]

 

Other articles by this author:

Cyclosporine A micellar delivery system for dry eyes

Kang H, Cha KH, Cho W, Park J, Park HJ, Sun BK, Hyun SM, Hwang SJ

International Journal of Nanomedicine 2016, 11:2921-2933

Published Date: 21 June 2016

Biodistribution of newly synthesized PHEA-based polymer-coated SPION in Sprague Dawley rats as magnetic resonance contrast agent [Corrigendum]

Park J, Cho W, Park HJ, Cha KH, Ha DC, Choi YW, Lee HY, Cho SH, Hwang SJ

International Journal of Nanomedicine 2014, 9:559-560

Published Date: 20 January 2014

Biodistribution of newly synthesized PHEA-based polymer-coated SPION in Sprague Dawley rats as magnetic resonance contrast agent

Park J, Cho W, Park HJ, Cha KH, Ha DC, Choi YW, Lee HY, Cho SH, Hwang SJ

International Journal of Nanomedicine 2013, 8:4077-4089

Published Date: 31 October 2013

Optimized formulation of solid self-microemulsifying sirolimus delivery systems

Cho W, Kim MS, Kim JS, Park J, Park HJ, Cha KH, Park JS, Hwang SJ

International Journal of Nanomedicine 2013, 8:1673-1682

Published Date: 26 April 2013

Enhanced bioavailability of sirolimus via preparation of solid dispersion nanoparticles using a supercritical antisolvent process

Kim MS, Kim JS, Park HJ, Cho WK, Cha KH, Hwang SJ

International Journal of Nanomedicine 2011, 6:2997-3009

Published Date: 24 November 2011

Readers of this article also read:

Antimicrobial activity of metal oxide nanoparticles against Gram-positive and Gram-negative bacteria: a comparative study

Azam A, Ahmed AS, Oves M, Khan MS, Habib SS, Memic A

International Journal of Nanomedicine 2012, 7:6003-6009

Published Date: 5 December 2012

Encapsulation of cisplatin in long-circulating and pH-sensitive liposomes improves its antitumor effect and reduces acute toxicity

Leite EA, Souza CM, Carvalho-Júnior AD, Coelho LG, Lana AM, Cassali GD, Oliveira MC

International Journal of Nanomedicine 2012, 7:5259-5269

Published Date: 9 October 2012

Supramolecular nanoparticles generated by the self-assembly of polyrotaxanes for antitumor drug delivery

Liu R, Lai YS, He B, Li Y, Wang G, Chang S, Gu Z

International Journal of Nanomedicine 2012, 7:5249-5258

Published Date: 5 October 2012

Novel micelle formulation of curcumin for enhancing antitumor activity and inhibiting colorectal cancer stem cells

Wang K, Zhang T, Liu L, Wang XL, Wu P, Chen ZG, Ni C, Zhang JS, Hu FQ, Huang J

International Journal of Nanomedicine 2012, 7:4487-4497

Published Date: 13 August 2012

Fabrication and characterization of a rapid prototyped tissue engineering scaffold with embedded multicomponent matrix for controlled drug release

Chen M, Le DQ, Hein S, Li P, Nygaard JV, Kassem M, Kjems J, Besenbacher F, Bünger C

International Journal of Nanomedicine 2012, 7:4285-4297

Published Date: 3 August 2012

Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study

Song X, Jiang Y, Ren CJ, Sun X, Zhang Q, Gong T, Zhang ZR

International Journal of Nanomedicine 2012, 7:3689-3699

Published Date: 13 July 2012

Evaluation of the genotoxicity of cellulose nanofibers

de Lima R, Feitosa LO, Maruyama CR, Barga MA, Yamawaki PC, Vieira IJ, Teixeira EM, Corrêa AC, Mattoso LH, Fraceto LF

International Journal of Nanomedicine 2012, 7:3555-3565

Published Date: 11 July 2012

Electrostatic self-assembly of multilayer copolymeric membranes on the surface of porous tantalum implants for sustained release of doxorubicin

Guo X, Chen M, Feng W, Liang J, Zhao H, Tian L, Chao H, Zou X

International Journal of Nanomedicine 2011, 6:3057-3064

Published Date: 28 November 2011