Preparation and characterization of valsartan-loaded polyoxalate microspheres: In vitro release profiles

Jung Keun Lee; Seok Cheol Yoo; A. Ram Kim; Dongwon Lee; Peter M. Kang; Soon Hong Yuk; Paul M. Vanhoutte; Gilson Khang

Macromolecular Research, Vol.21, No.5, 550-555, May, 2013

DOI10.1007/s13233-013-1054-1 Export Citation

Preparation and characterization of valsartan-loaded polyoxalate microspheres: In vitro release profiles

Jung Keun Lee, Seok Cheol Yoo, A. Ram Kim, Dongwon Lee , Peter M. Kang, Soon Hong Yuk¹, Paul M. Vanhoutte, and Gilson Khang^†

Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, Chonbuk National University, Jeonbuk, 561-756, Korea
¹College of Pharmacy, Korea University, Chungnam, 339-700, Korea

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Valsartan, a selective angiotensin II type 1 receptor (AT1R) antagonist, has a high bioavailability. Hydrophobic polyoxalate has been suggested for use in biodegradable medical devices such as absorbable sutures and controlled release applications. In this study, we developed valsartan-loaded polyoxalate microspheres by varying the polyoxalate molecular weight, surfactant content, and initial drug loading rate. The morphology of the valsartanloaded polyoxalate microspheres was evaluated by scanning electron microscopy and the hydrolysis kinetics of polyoxalate were investigated. The influences regarding the preparation parameters were evaluated with respect to the release of valsartan. The results demonstrated that the release behavior can be effectively controlled by the preparation conditions.

Keywords:valsartan;polyoxalate;microspheres;controlled release

[References]

Markham A, Goa KL, Drugs, 54, 299 (1997)
Hermida RC, Calvo C, Auala DE, Fernandez JR, Covelo M, Mojon A, Lopez JE, J. Hypertens., 23, 1913 (2005)
Cudina O, Brboric J, Jankovic I, Karljikovic-Rajic K, Vladimirov S, Colloids Surf. B: Biointerfaces, 65, 80 (2008)
Gonzalez O, Iriarte G, Ferreiros N, Maguregui MI, Alonso RM, Jimenez RM, J. Pharm. Biomed., 50, 630 (2009)
Eom S, Yoo SC, Kim YK, Lee YH, Lee EY, Yu H, Lee D, Khang G, Polym.(Korea), 34(4), 333 (2010)
Bodmer D, Kissel T, Traechslin E, J. Control. Release, 2, 129 (1992)
Jalil R, Nixon JR, J. Microencapsul., 7, 45 (1990)
Khang G, Cho JC, Lee JW, Rhee JM, Lee HB, Bio-Med. Mater. Eng., 9, 49 (1999)
Freiberg S, Zhu X, Int. J. Pharm., 282, 1 (2004)
Lee E, Kim S, Seong K, Park H, Seo H, Khang G, Lee D, J. Biomater. Sci.-Polym. Ed., 22, 83 (2011)
Kim S, Seong K, Kim O, Kim S, Seo H, Lee M, Khang G, Lee D, Biomacromolecules, 11(3), 555 (2010)
Lee D, Khaja S, Velasquez-Castano JC, Dasari M, Sun C, Petros J, Taylor WR, Murthy N, Nat. Mater., 6(10), 765 (2007)
Rawat A, Burgess DJ, Int. J. Pharm., 394, 99 (2010)
Nii T, Ishiis F, Int. J. Pharm., 298, 198 (2001)
Thomasin C, Merkle HP, Gander B, J. Pharm. Sci., 87, 269 (1998)
Sturesson C, Carlfores J, Edman K, Andersson M, Int. J. Pharm., 89, 235 (1993)
Guyot M, Fawaz F, Int. J. Pharm., 175, 61 (1998)
Mao S, Xu J, Cai C, Germershaus O, Schaper A, Kissel T, Int. J. Pharm., 334, 137 (2007)
Jeyanthi R, Mehta RC, Thanoo BC, DeLuca PP, J. Microencapsul., 14(2), 163 (1997)
Li WI, Anderson KW, Mehta RC, DeLuca PP, J. Control. Release, 37, 199 (1995)
Wischkel C, Schwendeman SP, Int. J. Pharm., 364, 298 (2008)
Yang Y, Chia H, Chung T, J. Control. Release, 69, 81 (2000)
Kim BS, Oh JM, Kim KS, Seo KS, Cho JS, Khang G, Lee HB, Park K, Kim MS, Biomaterials, 30, 902 (2009)
Li M, Rouaud O, Poncelet D, Int. J. Pharm., 363, 26 (2008)

[Related Articles]

[1] Markham A, Goa KL, Drugs, 54, 299 (1997)

[2] Hermida RC, Calvo C, Auala DE, Fernandez JR, Covelo M, Mojon A, Lopez JE, J. Hypertens., 23, 1913 (2005)

[3] Cudina O, Brboric J, Jankovic I, Karljikovic-Rajic K, Vladimirov S, Colloids Surf. B: Biointerfaces, 65, 80 (2008)

[4] Gonzalez O, Iriarte G, Ferreiros N, Maguregui MI, Alonso RM, Jimenez RM, J. Pharm. Biomed., 50, 630 (2009)

[5] Eom S, Yoo SC, Kim YK, Lee YH, Lee EY, Yu H, Lee D, Khang G, Polym.(Korea), 34(4), 333 (2010)

[6] Bodmer D, Kissel T, Traechslin E, J. Control. Release, 2, 129 (1992)

[7] Jalil R, Nixon JR, J. Microencapsul., 7, 45 (1990)

[8] Khang G, Cho JC, Lee JW, Rhee JM, Lee HB, Bio-Med. Mater. Eng., 9, 49 (1999)

[9] Freiberg S, Zhu X, Int. J. Pharm., 282, 1 (2004)

[10] Lee E, Kim S, Seong K, Park H, Seo H, Khang G, Lee D, J. Biomater. Sci.-Polym. Ed., 22, 83 (2011)

[11] Kim S, Seong K, Kim O, Kim S, Seo H, Lee M, Khang G, Lee D, Biomacromolecules, 11(3), 555 (2010)

[12] Lee D, Khaja S, Velasquez-Castano JC, Dasari M, Sun C, Petros J, Taylor WR, Murthy N, Nat. Mater., 6(10), 765 (2007)

[13] Rawat A, Burgess DJ, Int. J. Pharm., 394, 99 (2010)

[14] Nii T, Ishiis F, Int. J. Pharm., 298, 198 (2001)

[15] Thomasin C, Merkle HP, Gander B, J. Pharm. Sci., 87, 269 (1998)

[16] Sturesson C, Carlfores J, Edman K, Andersson M, Int. J. Pharm., 89, 235 (1993)

[17] Guyot M, Fawaz F, Int. J. Pharm., 175, 61 (1998)

[18] Mao S, Xu J, Cai C, Germershaus O, Schaper A, Kissel T, Int. J. Pharm., 334, 137 (2007)

[19] Jeyanthi R, Mehta RC, Thanoo BC, DeLuca PP, J. Microencapsul., 14(2), 163 (1997)

[20] Li WI, Anderson KW, Mehta RC, DeLuca PP, J. Control. Release, 37, 199 (1995)

[21] Wischkel C, Schwendeman SP, Int. J. Pharm., 364, 298 (2008)

[22] Yang Y, Chia H, Chung T, J. Control. Release, 69, 81 (2000)

[23] Kim BS, Oh JM, Kim KS, Seo KS, Cho JS, Khang G, Lee HB, Park K, Kim MS, Biomaterials, 30, 902 (2009)

[24] Li M, Rouaud O, Poncelet D, Int. J. Pharm., 363, 26 (2008)