Trimethyl chitosan nanoparticles enhances dissolution of the poorly water soluble drug Candesartan-Cilexetil

Aylin Gecer; Nuray Yıldız; Ayla Calımlı; Belma Turan

Macromolecular Research, Vol.18, No.10, 986-991, October, 2010

DOI10.1007/s13233-010-1004-0 Export Citation

Trimethyl chitosan nanoparticles enhances dissolution of the poorly water soluble drug Candesartan-Cilexetil

Aylin Gecer^†, Nuray Yıldız, Ayla Calımlı, and Belma Turan¹

Faculty of Engeering, Department of Chemical Engineering, Ankara University, Ankara, 06100, Turkey, Korea
¹Faculty of Medicine, Department of Biophysics, Ankara University, Ankara, 06410, Turkey

E-mail:

Candesartan-cilexetil, an angiotensin receptor blocker, exhibits low bioavailability after oral administration due to its low water solubility. Chitosan is considered one of the most promising biopolymers for drug delivery as a vehicle and trimethyl chitosan is a water soluble chitosan derivative. Trimethyl chitosan nanoparticles were prepared by the ionic crosslinking of a trimethyl chitosan solution with tripolyphosphate, at ambient temperatures during stirring. SEM and TEM (scanning and transmission electron microscopy) revealed trimethyl chitosan and trimethyl chitosan nanoparticles between 1,000-3,000 nm and 13-350 nm in size, respectively. Candesartan-cilexetil was loaded on trimethyl chitosan nanoparticles, trimethyl chitosan, gum arabic and commercial water soluble chitosan using an ultrasonic effect, and the potential of the polymers to increase the solubility of candesartan-cilexetil was investigated. Trimethyl chitosan nanoparticles are a superior vehicle for increasing the solubility of candesartan-cilexetil compared to trimethyl chitosan, gum arabic or commercial water soluble chitosan.

Keywords:candesartan-cilexetil;chitosan nanoparticle;water solubility;bioavailability

[References]

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Genta I, Pavanetto F, Conti B, Giunchedi P, Conte U, STP Pharma Sci., 5, 202 (1995)
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Avadi MR, Zohuriaan-Mehr MJ, Younessi P, Amini M, Tehrani MR, Shafiee A, J. Bioact. Compat. Polym., 18, 469 (2003)
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Ishimura Y, Chatani F, Sato S, Int. J. Toxicol., 18, 369 (1999)
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Amidi M, Romeijn SG, Borchard G, Junginger HE, Hennink WE, Jiskoot W, J. Control. Release, 111, 107 (2006)
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Rao SVS, Radhakrishnanand P, Suryanarayana MV, Himabindu V, Chromatographia, 66, 499 (2007)
Ding Y, Xia X, Zhang C, Nanotechnology, 17, 4156 (2006)
Britto D, Assis BGO, Carbohydr. Polym., 69, 305 (2007)
He W, Du YM, Dai WB, Wu Y, Zhang M, J. Appl. Polym. Sci., 99(3), 1140 (2006)
Hamman JH, Kotze AF, Drug Dev. Ind. Pharm., 27, 373 (2001)
Snyman D, Hamman JH, Kotze JS, Rollings JE, Kotze AF, Carbohydr. Polym., 50, 145 (2002)
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Babu VR, Areefulla SH, Mallikarjun V, J. Pharm. Res., 3, 141 (2010)

[Referenced By]

[1] Shiraishi S, Arahira M, Imai T, Otagiri M, Chem Pharm Bull, 38, 185 (1990)

[2] Acarturk F, Sencan A, Celebi N, STP Pharma Sci., 3, 369 (1993)

[3] Genta I, Pavanetto F, Conti B, Giunchedi P, Conte U, STP Pharma Sci., 5, 202 (1995)

[4] Kim D, Jeong Y, Choi C, Roh S, Kang S, Jang M, Nah J, Int. J. Pharm., 319, 130 (2006)

[5] Holme KR, Perlin AS, Carbohydr. Res., 302, 7 (1997)

[6] Chung YC, Kuo CL, Chen CC, Bioresour. Technol., 96(13), 1473 (2005)

[7] Sieval AB, Thanou M, Kotze AF, Verhoef JC, Brussee J, Junginger HE, Carbohydr. Polym., 36, 157 (1998)

[8] Thanou M, Verhoef JC, Marbach P, Junginger HE, J. Pharm. Sci., 89, 951 (2000)

[9] Yang T, Chou C, Li C, Food Res. Intern., 35, 707 (2002)

[10] Avadi MR, Zohuriaan-Mehr MJ, Younessi P, Amini M, Tehrani MR, Shafiee A, J. Bioact. Compat. Polym., 18, 469 (2003)

[11] Miao J, Chen GH, Gao CJ, Lin CG, Wang D, Sun MK, J. Membr. Sci., 280(1-2), 478 (2006)

[12] Li D, Liu L, Tian K, Liu J, Fan X, Carbohydr. Polym., 67, 40 (2007)

[13] Portero A, Remunan-Lopez C, Vila-Jato JL, Int. J. Pharm., 175, 75 (1998)

[14] Merisko-Liversidge E, Liversidge GG, Cooper ER, Eur. J. Pharm. Sci., 18, 113 (2003)

[15] Miyabayashi T, Okuda T, Motohashi M, Izawa K, Yashiki T, J. Chromatogr. B, 677, 123 (1996)

[16] Cagigal E, Gonzalez L, Alonso RM, Jimenez RM, J. Pharm. Biomed. Anal., 26, 477 (2001)

[17] Ishimura Y, Chatani F, Sato S, Int. J. Toxicol., 18, 369 (1999)

[18] Raasch W, Wittmershaus C, Dendorfer A, Voges I, Pahlke F, Dodt C, Dominiak P, Johren O, Endocrinology, 147, 3539 (2006).

[19] Amidi M, Romeijn SG, Borchard G, Junginger HE, Hennink WE, Jiskoot W, J. Control. Release, 111, 107 (2006)

[20] Qutab SS, Razzaq SN, Ashfaq M, Shuja ZA, Khan IU, Acta Chromatographica, 19, 119 (2007)

[21] Rao SVS, Radhakrishnanand P, Suryanarayana MV, Himabindu V, Chromatographia, 66, 499 (2007)

[22] Ding Y, Xia X, Zhang C, Nanotechnology, 17, 4156 (2006)

[23] Britto D, Assis BGO, Carbohydr. Polym., 69, 305 (2007)

[24] He W, Du YM, Dai WB, Wu Y, Zhang M, J. Appl. Polym. Sci., 99(3), 1140 (2006)

[25] Hamman JH, Kotze AF, Drug Dev. Ind. Pharm., 27, 373 (2001)

[26] Snyman D, Hamman JH, Kotze JS, Rollings JE, Kotze AF, Carbohydr. Polym., 50, 145 (2002)

[27] Chen F, Zhang Z, Huang Y, Int. J. Pharm., 336, 166 (2007)

[28] Babu VR, Areefulla SH, Mallikarjun V, J. Pharm. Res., 3, 141 (2010)