Preparation of Biodegradable PLGA Nanospheres Employing a Fast Solvent Evaporation Method

Jung Yoon Jang; Byung Soo Kwon; Hea Eun Lee; Dong Hwan Kim; Ho Kyung Kang; Jae Seon Kang; Sangkil Lee; Guang Jin Choi

Journal of Industrial and Engineering Chemistry, Vol.13, No.6, 1043-1046, November, 2007

Jung Yoon Jang, Byung Soo Kwon, Hea Eun Lee, Dong Hwan Kim, Ho Kyung Kang¹, Jae Seon Kang, Sangkil Lee^†, and Guang Jin Choi^†

Department of Pharmaceutical Engineering, College of Engineering, In Je University (Gimhae Campus), Gyeongnam621-749, Korea
¹Cell Medicine, R&D Department, Gyeongnam 621-749, Korea

E-mail:,

The traditional W1/O/W2 emulsion method has a limit on the control of particle size to a nano-scale with high drug encapsulation efficiency (EE%). In the present study, we modified the solvent removal time and rate to develop an oral peptide drug delivery system using sCT as a model drug. We monitored the effect of the type of poly (vinyl alcohol) (PVA) within the W2 phase on the EE%. SEM images and particle size measurements revealed that the outer surfaces of representative nanosphere samples were very fine and even; the particle size was 383.2 ± 8.7 nm with a narrow size distribution (polydispersity index = 0.25 ± 0.004). The EE% increased depending on the solvent removal time and rate from 11.4 ± 1.3 to 28.8 ± 3.0 and 52.5 ± 6.5, compared to control nanospheres, respectively. The EE% of sCT was also enhanced by controlling the molecular weight of PVA within the W2 phase.

Keywords:PLGA;nanosphere;W1/O/W2;rotary evaporation;salmon calcitonin

[References]

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McClean S, Prosser E, Meehan E, O’Malley D, Clarke N, Ramtoola Z, Brayden D, Eur. J. Pharm. Sci., 6, 153 (1998)
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Nefzger M, Kreuter J, Voges R, Liehl E, Czok R, J. Pharm. Sci., 73, 1309 (1984)
Lee CM, Lee HC, Lee KY, J. Biosci. Bioeng., 100(3), 255 (2005)
Li H, Song JH, Park JS, Han K, Int. J. Pharm., 258, 11 (2003)
Lyons KC, Charman WN, Miller R, Christopher JH, Int. J. Pharm., 199, 17 (2000)
Kea WT, Lin SY, Hoa HO, Sheua MT, J. Control. Release, 102, 489 (2005)
Gao ZG, Choi HG, Shin HJ, Park KM, Lim SJ, Hwang KJ, Kim CK, Int. J. Pharm., 161, 75 (1998)
Kim SK, Lee EH, Vaishalia B, Lee S, Lee YK, Kim CY, Moon HT, Byuna Y, J. Control. Release, 105, 32 (2005)
Gaucher G, Dufresne MH, Sant VP, Maysinger NKD, Leroux JC, J. Control. Release, 109, 169 (2005)
Mathot F, van Beijsterveldt L, Preat V, Brewster M, Arien A, J. Control. Release, 111, 47 (2006)
Fernandez-Carballido A, Herrero-Vanrell R, Molina-Martinez IT, Pastorizai P, Int. J. Pharm., 279, 33 (2004)
You ES, Jang HS, Ahn WS, Kang MI, Jun MG, Kim YC, Chun HJ, J. Ind. Eng. Chem., 13(2), 219 (2007)
Luan X, Skupin M, Siepmann J, Bodmeier R, Int. J. Pharm., 324, 168 (2006)
Win KY, Feng SS, Biomaterials, 26, 2713 (2005)
Frazza EJ, Schmitt EE, J. Biomed. Mater. Res., 5, 43 (1971)
Brady JM, Cutright DE, Miller RA, Battestone GC, J. Biomed. Mater. Res., 7, 155 (1973)
Camilleri P, Okafo GN, Southan C, Brown R, Anal. Biochem., 198, 36 (1991)
Schneyer CR, J. Md. Med., 40, 469 (1991)
Huwyler R, Born W, Ohanhaus EE, Fischer JA, Am. J. Physiol., 236, E15 (1979)
Prego C, Garcia M, Torres D, Alonso MJ, J. Control. Release, 101, 151 (2005)
Song KH, Chung SJ, Shim CK, J. Control. Release, 84, 27 (2002)
Rathbone MJ, Drummond BK, Tucker IG, Adv. Drug Deliv. Rev., 13, 1 (1994)
Freytag T, Dashevsky A, Tillman L, Hardee GE, Bodmeiera R, J. Control. Release, 69, 197 (2000)
Kim HK, Park TG, Int. J. Pharm., 229, 107 (2001)
Bilati U, Allemann E, Doelker E, AAPS. Pharm. Sci. Tech., 6, 74 (2005)
Yang YY, Chung TS, Ng NP, Biomaterials, 22, 231 (2001)
Carrio A, Schwach G, Coudane J, Vert M, J. Control. Release, 37, 113 (1995)

[Referenced By]

[1] van der Lubben M, Verhoef JC, van Aelst AC, Borchard G, Junginger HE, Biomaterials, 22, 687 (2001)

[2] McClean S, Prosser E, Meehan E, O’Malley D, Clarke N, Ramtoola Z, Brayden D, Eur. J. Pharm. Sci., 6, 153 (1998)

[3] Pappo J, Ermak TH, Clin. Exp. Immunol., 76, 144 (1989)

[4] Nefzger M, Kreuter J, Voges R, Liehl E, Czok R, J. Pharm. Sci., 73, 1309 (1984)

[5] Lee CM, Lee HC, Lee KY, J. Biosci. Bioeng., 100(3), 255 (2005)

[6] Li H, Song JH, Park JS, Han K, Int. J. Pharm., 258, 11 (2003)

[7] Lyons KC, Charman WN, Miller R, Christopher JH, Int. J. Pharm., 199, 17 (2000)

[8] Kea WT, Lin SY, Hoa HO, Sheua MT, J. Control. Release, 102, 489 (2005)

[9] Gao ZG, Choi HG, Shin HJ, Park KM, Lim SJ, Hwang KJ, Kim CK, Int. J. Pharm., 161, 75 (1998)

[10] Kim SK, Lee EH, Vaishalia B, Lee S, Lee YK, Kim CY, Moon HT, Byuna Y, J. Control. Release, 105, 32 (2005)

[11] Gaucher G, Dufresne MH, Sant VP, Maysinger NKD, Leroux JC, J. Control. Release, 109, 169 (2005)

[12] Mathot F, van Beijsterveldt L, Preat V, Brewster M, Arien A, J. Control. Release, 111, 47 (2006)

[13] Fernandez-Carballido A, Herrero-Vanrell R, Molina-Martinez IT, Pastorizai P, Int. J. Pharm., 279, 33 (2004)

[14] You ES, Jang HS, Ahn WS, Kang MI, Jun MG, Kim YC, Chun HJ, J. Ind. Eng. Chem., 13(2), 219 (2007)

[15] Luan X, Skupin M, Siepmann J, Bodmeier R, Int. J. Pharm., 324, 168 (2006)

[16] Win KY, Feng SS, Biomaterials, 26, 2713 (2005)

[17] Frazza EJ, Schmitt EE, J. Biomed. Mater. Res., 5, 43 (1971)

[18] Brady JM, Cutright DE, Miller RA, Battestone GC, J. Biomed. Mater. Res., 7, 155 (1973)

[19] Camilleri P, Okafo GN, Southan C, Brown R, Anal. Biochem., 198, 36 (1991)

[20] Schneyer CR, J. Md. Med., 40, 469 (1991)

[21] Huwyler R, Born W, Ohanhaus EE, Fischer JA, Am. J. Physiol., 236, E15 (1979)

[22] Prego C, Garcia M, Torres D, Alonso MJ, J. Control. Release, 101, 151 (2005)

[23] Song KH, Chung SJ, Shim CK, J. Control. Release, 84, 27 (2002)

[24] Rathbone MJ, Drummond BK, Tucker IG, Adv. Drug Deliv. Rev., 13, 1 (1994)

[25] Freytag T, Dashevsky A, Tillman L, Hardee GE, Bodmeiera R, J. Control. Release, 69, 197 (2000)

[26] Kim HK, Park TG, Int. J. Pharm., 229, 107 (2001)

[27] Bilati U, Allemann E, Doelker E, AAPS. Pharm. Sci. Tech., 6, 74 (2005)

[28] Yang YY, Chung TS, Ng NP, Biomaterials, 22, 231 (2001)

[29] Carrio A, Schwach G, Coudane J, Vert M, J. Control. Release, 37, 113 (1995)