Triptorelin Acetate-Loaded Poly(lactide-co-glycolide) (PLGA) Microspheres for Controlled Drug Delivery

Kyonghee Park; Goo Young Jung; Myong-Ki Kim; Mork Soon Park; Yong Kook Shin; Jae-Kwan Hwang; Soon Hong Yuk

Macromolecular Research, Vol.20, No.8, 847-851, August, 2012

DOI10.1007/s13233-012-0123-1 Export Citation

Triptorelin Acetate-Loaded Poly(lactide-co-glycolide) (PLGA) Microspheres for Controlled Drug Delivery

Kyonghee Park^{1, 2}, Goo Young Jung³, Myong-Ki Kim^{1, 4}, Mork Soon Park³, Yong Kook Shin^{1, 4}, Jae-Kwan Hwang^{2, 5, †}, and Soon Hong Yuk^{6, †}

¹Chungbuk Technopark, Chungbuk, 363-883, Korea
²Department of Biomaterials Science and Engineering, Yonsei University, Seoul, 120-749, Korea
³Dongkook Pharmaceutical Company, Chungbuk, 365-830, Korea
⁴, Korea
⁵Department of Biotechnology, College of Life Science and Biotechnology, Yonsei University, Seoul, 120-749, Korea
⁶College of Pharmacy, Korea University, Chungnam, 339-700, Korea

E-mail:,

Triptorelin acetate-loaded poly(lactide-co-glycolide) (PLGA) microspheres have been prepared in binary solvent mixtures composed of dichloromethane (DCM) and acetone (AC). The surface morphology of PLGA microspheres was examined by scanning electron microscopy with varying solvent composition, and the size distribution of PLGA microspheres was measured using a particle size analyzer. Triptorelin acetate is a luteinizing hormonereleasing hormone analog that is used as a model peptide drug. With the increase of AC content in the binary solvent mixture, PLGA microspheres with smooth surface were obtained and this led to an increased loading efficiency with the decreased particle size. For the application of PLGA microspheres as a controlled drug delivery system, the release pattern of triptorelin acetate was observed and the stability of triptorelin acetate-loaded PLGA microspheres was observed with or without mannitol. The sustained release pattern was observed after the initial burst effect and the improved stability of PLGA microspheres was observed with mannitol.

Keywords:triptorelin acetate;PLGA microspheres;controlled release;peptide drug;stability;mannitol.

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[2] Deasy PB, Microencapsulation and Related Drug Processes, Dekker M, New York (1984)

[3] Jain RA, Biomaterials., 21, 2475 (2000)

[4] Kond A, Microcapsule Processing and Technology, Marcel Dekker, New York (1979)

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

[6] Woo HJ, Kim JS, KiM J, Nurunnabi M, Huh KM, Cho KJ, Lee YK, Polym.(Korea), 34(6), 527 (2010)

[7] Thomasin C, Johansen P, Alder R, Bemsel R, Hottinger G, Altorfer H, Wright AD, Wehrli G, Merkle HP, Gander B, Eur. J. Pharm. Biopharm., 42, 16 (1996)

[8] Del Mastro L, Boni L, Michelotti A, Gamucci T, Olmeo N, Gori S, Giordano M, Garrone O, Pronzato P, Bighin C, Levaggi A, Giraudi S, Cresti N, Magnolfi E, Scotto T, Vecchio C, Venturini M, JAMA., 306, 269 (2011)

[9] Whelan P, Expert Opin. Pharmacother., 11, 2929 (2010)

[10] Cirkel U, Ochs H, Schneider HP, Eur. J. Obstet.Gynecol. Reprod. Biol., 59, 61 (1995)

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[13] Schoenhammer K, Petersen H, Guethlein F, Goepferich A, Int. J. Pharm., 371, 33 (2009)

[14] Diwan M, Park TG, J. Control. Release., 73, 233 (2001)

[15] Schaefer MJ, Singh J, Drug Dev. Ind. Pharm., 27, 345 (2001)

[16] Bodmeier R, McGinity JW, Int. J. Pharm., 43, 179 (1988)

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

[18] Park TG, Lee HY, Nam YS, J. Control. Release., 55, 181 (1998)

[19] Escobedo J, Mansoori GA, AIChE J., 44(10), 2324 (1998)

[20] Astete CE, Sabliov CM, J. Biomater. Sci. Polym. Ed., 17, 247 (2006)

[21] Pourshahab PS, Gilani K, Moazeni E, Eslahi H, Fazeli MR, Jamalifar H, J. Microencapsul., 28(7), 605 (2011)

[22] Ashurst I, Malton A, Prime D, Sumby B, Pharm. Sci.Technol. Today., 3, 246 (2000)