In vitro controlled release of tuberculosis drugs by amphiphilic branched copolymer nanoparticles

Mani Gajendiran; Heejung Jo; Kyobum Kim; Sengottuvelan Balasubramanian

Journal of Industrial and Engineering Chemistry, Vol.77, 181-188, September, 2019

DOI10.1016/j.jiec.2019.04.033 Export Citation

In vitro controlled release of tuberculosis drugs by amphiphilic branched copolymer nanoparticles

Mani Gajendiran^{1, 2}, Heejung Jo², Kyobum Kim^{2, †}, and Sengottuvelan Balasubramanian^{1, †}

¹Department of Inorganic Chemistry, University of Madras, Guindy Campus, Chennai, 600025, India
²Division of Bioengineering, School of Life Sciences and Bioengineering, Incheon National University, Incheon, 22012, Republic of Korea

E-mail:,

Poly(lactic-co-glycolic acid) (PLGA)-poly ethylene glycol (PEG) based amphiphilic branched copolymer nanoparticles (NPs) have been developed for controlled release of tuberculosis (TB) drugs which include rifampicin (RIF), isoniazid (INH) and pyrazinamide (PYZ). The drug loading efficiency and the percentage drug content of polymer NPs increase by increasing the amount of PEG content in polymer NPs. The branched PLGA-PEG based copolymer NPs exhibit initial burst release followed by sustained release of RIF for 840 h, INH for 72 h, and PYZ for 720 h. The branched citrate-PEG-PLGA copolymer NPs can act as potential drug carriers when compared to their linear analogues.

Keywords:Citrate-PEG-PLGA branched copolymer;Polymer nanoparticles;In vitro drug release;Rifampicin;Isoniazid;Pyrazinamide

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[2] Pontali E, Sotgiu G, Tiberi S, Tadolini M, Visca D, D’Ambrosio L, Centis R, Spanevello A, Migliori GB, Eur. Respir. J., 52, 180093 (2018)

[3] Shaji J, Shaikh M, Int. J. Pharmacy Pharm. Sci., 8, 1 (2016)

[4] Shivangi, Meena LS, Appl. Biochem. Biotechnol., 185(3), 815 (2018)

[5] Thomas D, Latha MS, Thomas KK, J. Drug Deliv. Sci. Technol, 46, 392 (2018)

[6] Praphakar RA, Munusamy MA, Rajan M, Int. J. Pharm., 524, 168 (2017)

[7] Sarmah M, Hussain A, Ramteke A, Maji TK, J. Chem. Sci., 128, 1291 (2016)

[8] Huang J, Chen Z, Li Y, Li L, Zhang G, Drug Des. Dev. Ther., 11, 585 (2017)

[9] Huang D, Li D, Wang T, Shen H, Zhao P, Liu B, You Y, Ma Y, Yang F, Wu D, Wang S, Biomaterials, 52, 417 (2015)

[10] Gajendiran M, Gopi V, Elangovan V, Murali RV, Balasubramanian S, Colloids Surf. B: Biointerfaces, 104, 107 (2013)

[11] Gajendiran M, Divakar S, Raaman N, Balasubramanian S, Curr. Drug Deliv., 10, 722 (2013)

[12] Gajendiran M, Yousuf SMJ, Elangovan V, Balasubramanian S, J. Mater. Chem. B, 2, 418 (2014)

[13] De Faria TJ, Roman M, De Souza NM, De Vecchi R, De Assis JV, Dos Santos ALD, Bechtold IH, Winter N, Soares MJ, Silva LP, De Almeida MJ, Bafica A, Antimicrob. Agents Chemother., 56, 2259 (2012)

[14] Gajendiran M, Balasubramanian S, Adv. Mater. Res., 584, 460 (2012)

[15] Raj CA, Kumar PS, Kumar KS, Int. J. Pharm. Pharm. Sci., 4, 398 (2012)

[16] Gajendiran M, Balashanmugam P, Kalaichelvan PT, Balasubramanian S, Mater. Res. Exp., 3, 065401 (2016)

[17] Duro-Castano A, Movellan J, Vicent MJ, Biomater. Sci., 3, 1321 (2015)

[18] Jie Fu, Peter A. Campochiaro, Hanes JS, US Patent Appl. 0272994 A1 (2013).

[19] Minesso A, Cavalieri R, Chinellato R, US patent 9873817B2 (2018).

[20] Wang ZY, Zhao YM, Wang F, Wang J, J. Appl. Polym. Sci., 99, 244 (2005)

[21] Naeini AT, Adeli M, Vossoughi M, Nanomedicine, 6, 556 (2010)

[22] Pandey R, Sharma A, Zahoor A, Sharma S, Khuller GK, Prasad B, J. Antimicrob. Chemother., 52, 981 (2003)

[23] Santos RHT, Santos NG, Alves JPH, Garcia CAB, Romao LCP, Arguelho MLPM, Bioelectrochemistry, 72, 122 (2008)

[24] Hiremath PS, Saha RN, AAPS PharmSciTech, 9, 1171 (2008)

[25] Doll KM, Shogren RL, Willett JL, Swift G, J. Polym. Sci. A: Polym. Chem., 44(14), 4259 (2006)

[26] Yang J, Webb AR, Pickerill SJ, Hageman G, Ameer GA, Biomaterials, 27, 1889 (2006)

[27] Li YP, Pei YY, Zhang XY, Gu ZH, Zhou ZH, Yuan WF, Zhou JJ, Zhu JH, Gao XJ, J. Control. Release, 71, 203 (2001)

[28] Yao F, Bai Y, Chen W, An X, Yao K, Sun P, Lin H, Eur. Polym. J., 40, 1895 (2004)

[29] Han S, Kim C, Kwon D, Polymer, 38(2), 317 (1997)

[30] Wang ZY, Zhao YM, Wang F, J. Appl. Polym. Sci., 102(1), 577 (2006)

[31] Diab R, Brillault J, Bardy A, Gontijo AVL, Olivier JC, Int. J. Pharm., 436, 833 (2012)

[32] Doan TVP, Olivier JC, Int. J. Pharm., 382, 61 (2009)

[33] Ito F, Fujimori H, Honnami H, Kawakami H, Kanamura K, Makino K, Colloids Surf. B: Biointerfaces, 66, 65 (2008)

[34] Chaubey P, Mishra B, Carbohydr. Polym., 101, 1101 (2014)

[35] Patel BK, Parikh RH, Aboti PS, J. Drug Deliv., 2013, 10 (2013)

[36] Chimote G, Banerjee R, J. Biomed. Mater. Res. A, 89A, 281 (2008)

[37] Sarfaraz MD, Hiremath D, Chowdary KPR, Indian J. Pharm. Sci., 72, 101 (2010)

[38] Chenna GP, Shetty SK, Pai JB, Gopinath B, Ahmed M, Int. J. ChemTech Res., 3, 5 (2011)

[39] Mehta SK, Kaur G, Verma A, Colloids Surf. A: Physicochem. Eng. Asp., 375, 219 (2011)

[40] Qurratul A, Sharma S, Khuller GK, Garg SK, J. Antimicrob. Chemother., 51, 931 (2003)

[41] Jain GK, Pathan SA, Akhter S, Ahmad N, Jain N, Talegaonkar S, Khar RK, Ahmad FJ, Polym. Degrad. Stabil., 95, 2360 (2010)

[42] Milacic V, Schwendeman SP, Pharm. Res., 31, 436 (2014)

[43] Romero JA, Kuczler FJ, Am. Fam. Physician, 57, 749 (1998)