Short Communication | Volume: 8, Issue: 8, August, 2018

Synthesis, Characterization of Novel PLGA Encapsulated Indole Nanoparticles and Study of its cytotoxic potential against A549 lung cancer cell line

Sudip Majumder Neha Sharma Subhra Das Namita Pandey Tapasya Srivastava Debasree Ghosha   

Open Access   

Published:  Aug 31, 2018

DOI: 10.7324/JAPS.2018.8820

Objectives: Indole and its derivatives are gaining importance because of their anti-cancer activity. Here, we have reported the synthesis and characterization of novel polymeric poly D, L-lactide-co-glycolide (PLGA) indole nanoparticles, and investigated their cytotoxic potential against A549 lung cancer cells. Materials and methods: Nanoparticles were synthesized by solvent emulsion-diffusion-evaporation method. Size determination was done by Transmission Electron Microscopy (TEM), encapsulation efficiency using UV-Vis spectra, release kinetics using dialysis, measurement of drug-polymer interaction by Fourier Transform Infra Red Spectroscopy (FTIR) and surface charge by zeta potential. Cell viability of lung cancer cells (A549) was determined by (3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyltetrazolium bromide (MTT) assay and morphological analysis. Results: Nanoparticles were spherical in shape with an average diameter of 65 nm, encapsulation efficiency was found to be about 78% and zeta potential was −15.2mV. Drug-loaded nanoparticles showed sustained release kinetics fitting well in exponential Higuchi and Zero order Model. FTIR studies showed a broadening of the peak of PLGA indole nanoparticles at 2100-3400 cm-1 indicating the formation of drug-loaded nanoparticles. These nanoparticles showed about 95% cytotoxicity against A549 lung cancer cell lines. Results were supported by visible morphological changes in cells. Conclusion: PLGA encapsulated Indole nanoparticles were stable, having sustained release and good cytotoxic potential.

Keyword:     Nanoparticles biomaterials polymerssustained releasecytotoxicity.


Majumder S, Sharma N, Das S, Pandey N, Srivastava T, Ghosh D. Synthesis, Characterization of Novel PLGA Encapsulated Indole Nanoparticles and Study of its cytotoxic potential against A549 lung cancer cell line. J App Pharm Sci, 2018; 8(08): 144- 150.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Chu W, Zere TR, Weber MM, Wood TK, Whiteley M, Romano E, Valenzuela BH, Mc Lean RJC. Microfluidic platform for rapid antibiotic susceptibility testing of polymicrobial communities. Appl and Environ Microbiol, 2011; 78:411-419.

Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm, 2010; 67:217-223.

El-Sayed ST, Omar NI, El-Sayed MES, Shousha WG. Evaluation Antioxidant and cytotoxic activities of novel chitooligosaccharides prepared from chitosan via enzymatic hydrolysis and ultrafiltration. Journal of App Pharm Sci, 2017; 7(11):050-055

Ghosh D, Choudhury ST, Ghosh S, Mandal AK, Sarkar S, Ghosh A, Saha KD, Das N. Nanocapsulated curcumin: Oral chemopreventive formulation against diethylnitrosamine induced hepatocellular carcinoma in rat. Chem Biol Interact, 2012; 195:206–214.

Ghosh, D, Ghosh S, Sarkar S, Ghosh A, Das N, Saha KD, Mandal AK. Quercetin in vesicular delivery systems: Evaluation in combating arsenic-induced acute liver toxicity associated gene expression in rat model. Chem Biol Interact, 2010; 186:61–71.

Gouda R, Vaishya H, Qing Z. Application of mathematical models in drug release kinetics of carbidopa and levodopa ER tablets. J Dev Drugs, 2007; 6(2):1-8.

Hariharan S, Bhardwaj V, Bala I, Sitterberg J, Bakowsky U, Ravi Kumar MNV. Design of Estradiol loaded PLGA Nanoparticulate formulations: a potent oral delivery system for Hormone therapy. Pharm. Res, 2006; 23(1):184–195.

Honary S and Zahir F. Effect of zeta potential on the properties of Nano-Drug Delivery Systems – A review (Part 1). Trop J Pharm Res, 2013; 12(2):255–264.

Ibrahim AY, El-Newary SA, Youness ER, Ibrahim AMM, El Kashak WA. Protective and therapeutic effect of Vitex agnus-castus against prostate cancer in rat. Journal of App Pharm Sci, 2017; 7(12):133-143.

Jain S, Hirst DG, Sullivan JMO. Gold nanoparticles as novel agents for cancer therapy. Br. J. Radiol, 2012; 85(1010):101-113.

Kim SY, Ryu JS, Li H, Park WJ, Yun HY, Baek KJ, Kwon NS, Sohn UD, Kim DS. UVB-activated indole-3-acetic acid induces apoptosis of PC-3 prostate cancer cells. Anticancer Res, 2010; 30 (11):4607-4612.

Kim YS, Milner JA. Indole-3-carbinol inhibits cell proliferation and induces apoptosis in Hep-2 laryngeal cancer cells. J Nutr Biochem, 2005; 16:65-73.

Kundu B, Ghosh D, Sinha MK, Sen PS, Balla, VK., Das N, Basu D. Doxorubicin-intercalated nano-hydroxyapatite drug-delivery system for liver cancer: An animal model. Ceramics International, 2013; 39(8):9557- 9566.

Lee J, Maeda T, Hoong SH, Wood TK. Reconfiguring the quorum-sensing regulator SdiA of Escherichia coli to control biofilm formation via indole and N-acylhomoserine lactones. Appl Environ Microbiol, 2009; 75:1703-1716.

Li G, Young KD. Indole production by the tryptphanase Tna Ain Escherischia coli is determined by the amount of exogenous tryprophan. Microbiology, 2013; 159:402-410.

Luo Y, Wang TT, Teng Z, Chen P, Sun J, Wang Q. Encapsulation of indole-3-carbinol and 3,3'-diindolylmethane in zein/carboxymethyl chitosan nanoparticles with controlled release property and improved stability. Food Chem, 2013; 201:224-230.

Mao CG, Tao ZZ, Chen Z, Chen C, Chen SM, Wan LJ. Expression of TWIST an inducer of epithelial-mesenchymal transition, in nasopharyngeal carcinoma and its clinical significance. Exp Ther Med, 2014; 8(1):207-212.

Mirza AZ, Siddiqui FA. Nanomedicine and drug delivery: a mini review. Int Nano Lett, 2014; 4(94):1-7.

Murugan K, Choonara YE, Kumar P, Bijukumar D, Toit LC, Pillay V. parameters and characteristics governing cellular internalization and trans-barrier trafficking of nanostructures. Int. J. Nanomedicine, 2015; 10:2191-2206.

Pandey N, Dhiman S, Srivastava, T, Majumder S. Transition metal oxide nanoparticles are effective in inhibiting lung cancer cell survival in the hypoxic tumor microenvironment. Chem Biol Interact, 2016; 254(4):221-230.

Patel H, Darji N, Pillai J, Patel B. Recent advance in anti-cancer activity of indole derivatives. Int. J. Drug Res. Tech, 2012; 2(3):225-230.

Patila S, Sandberg A, Heckert E, Self W, Seal S. Protein adsorption and cellular uptake of cerium oxide nanoparticles as a function of zeta potential. Biomaterials, 2007; 28(31):4600-4607.

Preetha P, Srinivasa R, Pushpalatha P, Biphasic Drug Delivery in controlled release formulations-A review. Int. J Pharmacy Technology, 2015; 6(4)3046-3060.

Sankar R., Maheswari R., Karthik S, Shivashangari KS, Ravikumar V. Anticancer activity of Ficusreligiosa engineered copper oxide nanoparticles. Mater. Sci. Eng. C, 2014; 44:234-239.

Shaikh J, Ankhola DD, Beniwal V, Singh D, Ravi Kumar MNV. Nanoparticle encapsulation improves oral bioavailability of curcumin by at least 9-fold when compared to curcumin administered with piperine as absorption enhancer. Eur. J. Pharm. Sci, 2009; 37(3-4):223–230.

Subal CB. 2006. Modelling of Drug release: The Higuchi equation and its application.

Tarnuzzer RW, Colon J, Patil S, Seal S. Vacancy engineered ceria nanostructures for protection from radiation-induced cellular damage. Nano Lett, 2005; 5:2573-2577.

Thakkar VT, Shah PA, Soni TG, Parmar MY, Gohel MC et al. Goodness-of-fit model-dependent approach for release kinetics of levofloxacin hemihydrates floating tablet. Dissolution Technologies, 2009; 16:35-39.

Wang YQ, Chen C, Chen Z, Xu Y, Wang Y, Xiao BK, Chen SM, Tao ZZ. Indole-3-carbinol inhibits cell proliferation and induces apoptosis in Hep-2 laryngeal cancer cells. Oncol. Rep, 2013; 30(1):227-233.

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