Optimization of cRGDfK ligand concentration on polymeric nanoparticles to maximize cancer targeting

Hoon Hyun; Youngbum Yoo; So Yeon Kim; Hyun Sun Ko; Heung Jae Chun; Dae Hyeok Yang

Journal of Industrial and Engineering Chemistry, Vol.81, 178-184, January, 2020

DOI10.1016/j.jiec.2019.09.006 Export Citation

Optimization of cRGDfK ligand concentration on polymeric nanoparticles to maximize cancer targeting

Hoon Hyun¹, Youngbum Yoo², So Yeon Kim³, Hyun Sun Ko⁴, Heung Jae Chun^{5, 6}, and Dae Hyeok Yang^{6, †}

¹Department of Biomedical Sciences, Chonnam National University Medical School, Gwangju 61469, Republic of Korea
²Department of Surgery, School of Medicine, The Konkuk University, Seoul 05030, Republic of Korea
³Department of Dental Hygiene, College of Health Sciences, Cheongju University, Cheongju 28503, Republic of Korea
⁴Department of Obstetrics & Gynecology, College of Medicine, The Catholic University of Korea, Seoul 06591, Republic of Korea
⁵Department of Medical Life Sciences, College of Medicine, The Catholic University of Korea, Seoul 06591, Republic of Korea
⁶Institute of Cell and Tissue Engineering, College of Medicine, The Catholic University of Korea, Seoul 06591, Republic of Korea

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Optimization of ligand density on polymeric nanoparticles (PNPs) is critical for targeting solid tumors. Here, we prepared fluorescent cyanine 5.5 dye and cyclo(arginine.glycine.aspartic acid.phenylalanine. lysine) ligand-modified polyethylene glycol-poly(lactic-co-glycolic acid) (Cy 5.5-cRGDfK-PEG-PLGA) NPs with different ligand concentrations and investigated their cancer-targeting abilities in vitro and in vivo. The PNPs self-assembled in an aqueous solution as round particles and showed an increase in their average size as a function of cRGDfK concentration. In vitro results revealed a gradual increase in the uptake of NPs in MDA-MB-435 breast cancer cells in a time- and ligand concentration-dependent manner. In vivo, NPs with 6 w/w% cRGDfK concentration showed prolonged uptake by the cancer tissue during the 7-day test period. These results suggest that Cy 5.5-cRGDfK6-PEG-PLGA NPs could serve as valuable drug carriers and diagnostic agents for the clinical treatment and targeting of solid cancers.

Keywords:Ligand presentation;cRGDfK;PEG-PLGA nanoparticle;Cancer targeting

[References]

Esabahy M, Heo GS, Lim SM, Sun GR, Wooley KL, Chem. Rev., 115(19), 10967 (2015)
Tang HY, Zhang HW, Ye HF, Zheng YG, J. Phys. Chem. B, 122(1), 171 (2018)
Rezvantalab S, Drude NI, Moraveji MK, Guvener N, Koons EK, Shi Y, Lammers T, Kiessling F, Front. Pharmacol., 9, 1260 (2018)
Calzoni E, Cesaretti A, Polchi A, Michele AD, Tancini B, Emiliani C, J. Funct. Biomater., 10, 4 (2019)
Yameen B, Choi WI, Vilos C, Swami A, Shi J, OC, J. Control. Release, 190, 485 (2014)
Siegel RL, Miller KD, Jemal A, CA Cancer J. Clin., 66, 7 (2016)
Danhier F, Breton AL, Preat V, Mol. Pharm., 9, 2961 (2012)
Dechantsreiter MA, Planker E, Matha B, Lohof E, Holzemann G, Jonczyk A, Goodman SL, Kessler H, J. Med. Chem., 42, 3033 (1999)
Yildiz T, Gu R, Zauscher S, Betancourt T, Int. J. Nanomed., 13, 6961 (2018)
Zhong YA, Meng FH, Deng C, Zhong ZY, Biomacromolecules, 15(6), 1955 (2014)
Kampen KR, J. Membr. Biol., 242, 69 (2011)
Lorger M, Krueger JS, O’Neal M, Staflin K, Felding-Habermann B, Pro. Natl. Acad. Sci., 106, 10666 (2009)
Ganguly KK, Pal S, Moulik S, Chatterjee A, Cell Adh. Migr., 7, 251 (2013)
Das M, Mohanty C, Sahoo SK, Expert Opin. Drug Deliv., 6, 285 (2009)
Park J, Singha K, Son S, Kim J, Namgung R, Yun CO, Kim WJ, Cancer Gene Ther., 19, 741 (2012)
Danhier F, Le Breton A, Preat V, Mol. Pharm., 9, 2961 (2012)
Arap W, Pasqualini R, Ruoslahti E, Curr. Opin. Oncol., 10, 560 (1998)
Haggag YA, Matchett KB, Falconer RA, Isreb M, Jones J, Faheem A, McCarron P, El-Tanani M, Cancers, 11, 222 (2019)
Chi C, Wu JB, Pan D, J. Biomed. Opt., 21, 050901 (2016)
Frangioni JV, Curr. Opin. Chem. Biol., 7, 626 (2003)
Xiaomin Y, Yan F, Wang F, Qin W, Wu G, Xiaojian Y, Shao C, Chung LWK, Yuan J, Med. Sci. Monit., 21, 511 (2015)
Caswell PT, Norman JC, Traffic, 7, 14 (2006)
Caswell P, Norman J, Trends Cell Biol., 18, 257 (2008)
Bridges K, Haford J, Ashwell G, Klausner RD, Proc. Natl. Acad. Sci. U. S. A., 79, 350 (1982)
Cui Y, Song X, Li S, He B, Yang L, Dai W, Zhang H, Wang X, Yang B, Zhang Q, Oncotarget, 8, 38618 (2017)
Weissleder R, Kelly K, Sun EY, Shtatland T, Josephson L, Nat. Biotechnol., 23, 1418 (2005)
Josan JS, Handl HL, Sankaranarayanan R, Xu L, Lynch RM, Vagner J, Mash EA, Hruby VJ, Gillies RJ, Bioconjugate Chem., 22, 1270 (2011)
Lundquist JJ, Toone EJ, Chem. Rev., 102(2), 555 (2002)
Ashley CE, Carnes EC, Phillips GK, Padilla D, Durfee PN, Brown PA, Hanna TN, Liu JW, Phillips B, Carter MB, Carroll NJ, Jiang XM, Dunphy DR, Willman CL, Petsev DN, Evans DG, Parikh AN, Chackerian B, Wharton W, Peabody DS, Brinker CJ, Nat. Mater., 10(5), 389 (2011)
Bartlett DW, Su H, Hldebrandt IJ, Weber WA, Davis ME, Proc. Natl. Acad. Sci. U. S. A., 104, 15549 (2007)
Toy R, Peiris PM, Ghaghada KB, Karathanasis E, Nanomedicine, 9, 121 (2014)
Zhang Z, Lai Y, Yu L, Ding J, Biomaterials, 31, 7873 (2010)

[Referenced By]

[1] Esabahy M, Heo GS, Lim SM, Sun GR, Wooley KL, Chem. Rev., 115(19), 10967 (2015)

[2] Tang HY, Zhang HW, Ye HF, Zheng YG, J. Phys. Chem. B, 122(1), 171 (2018)

[3] Rezvantalab S, Drude NI, Moraveji MK, Guvener N, Koons EK, Shi Y, Lammers T, Kiessling F, Front. Pharmacol., 9, 1260 (2018)

[4] Calzoni E, Cesaretti A, Polchi A, Michele AD, Tancini B, Emiliani C, J. Funct. Biomater., 10, 4 (2019)

[5] Yameen B, Choi WI, Vilos C, Swami A, Shi J, OC, J. Control. Release, 190, 485 (2014)

[6] Siegel RL, Miller KD, Jemal A, CA Cancer J. Clin., 66, 7 (2016)

[7] Danhier F, Breton AL, Preat V, Mol. Pharm., 9, 2961 (2012)

[8] Dechantsreiter MA, Planker E, Matha B, Lohof E, Holzemann G, Jonczyk A, Goodman SL, Kessler H, J. Med. Chem., 42, 3033 (1999)

[9] Yildiz T, Gu R, Zauscher S, Betancourt T, Int. J. Nanomed., 13, 6961 (2018)

[10] Zhong YA, Meng FH, Deng C, Zhong ZY, Biomacromolecules, 15(6), 1955 (2014)

[11] Kampen KR, J. Membr. Biol., 242, 69 (2011)

[12] Lorger M, Krueger JS, O’Neal M, Staflin K, Felding-Habermann B, Pro. Natl. Acad. Sci., 106, 10666 (2009)

[13] Ganguly KK, Pal S, Moulik S, Chatterjee A, Cell Adh. Migr., 7, 251 (2013)

[14] Das M, Mohanty C, Sahoo SK, Expert Opin. Drug Deliv., 6, 285 (2009)

[15] Park J, Singha K, Son S, Kim J, Namgung R, Yun CO, Kim WJ, Cancer Gene Ther., 19, 741 (2012)

[16] Danhier F, Le Breton A, Preat V, Mol. Pharm., 9, 2961 (2012)

[17] Arap W, Pasqualini R, Ruoslahti E, Curr. Opin. Oncol., 10, 560 (1998)

[18] Haggag YA, Matchett KB, Falconer RA, Isreb M, Jones J, Faheem A, McCarron P, El-Tanani M, Cancers, 11, 222 (2019)

[19] Chi C, Wu JB, Pan D, J. Biomed. Opt., 21, 050901 (2016)

[20] Frangioni JV, Curr. Opin. Chem. Biol., 7, 626 (2003)

[21] Xiaomin Y, Yan F, Wang F, Qin W, Wu G, Xiaojian Y, Shao C, Chung LWK, Yuan J, Med. Sci. Monit., 21, 511 (2015)

[22] Caswell PT, Norman JC, Traffic, 7, 14 (2006)

[23] Caswell P, Norman J, Trends Cell Biol., 18, 257 (2008)

[24] Bridges K, Haford J, Ashwell G, Klausner RD, Proc. Natl. Acad. Sci. U. S. A., 79, 350 (1982)

[25] Cui Y, Song X, Li S, He B, Yang L, Dai W, Zhang H, Wang X, Yang B, Zhang Q, Oncotarget, 8, 38618 (2017)

[26] Weissleder R, Kelly K, Sun EY, Shtatland T, Josephson L, Nat. Biotechnol., 23, 1418 (2005)

[27] Josan JS, Handl HL, Sankaranarayanan R, Xu L, Lynch RM, Vagner J, Mash EA, Hruby VJ, Gillies RJ, Bioconjugate Chem., 22, 1270 (2011)

[28] Lundquist JJ, Toone EJ, Chem. Rev., 102(2), 555 (2002)

[29] Ashley CE, Carnes EC, Phillips GK, Padilla D, Durfee PN, Brown PA, Hanna TN, Liu JW, Phillips B, Carter MB, Carroll NJ, Jiang XM, Dunphy DR, Willman CL, Petsev DN, Evans DG, Parikh AN, Chackerian B, Wharton W, Peabody DS, Brinker CJ, Nat. Mater., 10(5), 389 (2011)

[30] Bartlett DW, Su H, Hldebrandt IJ, Weber WA, Davis ME, Proc. Natl. Acad. Sci. U. S. A., 104, 15549 (2007)

[31] Toy R, Peiris PM, Ghaghada KB, Karathanasis E, Nanomedicine, 9, 121 (2014)

[32] Zhang Z, Lai Y, Yu L, Ding J, Biomaterials, 31, 7873 (2010)