Noorma Rosita, Yuyun Nailufa, Dewi Melani Hariyadi
Noorma Rosita, Yuyun Nailufa, Dewi Melani Hariyadi
Pharmaceutics Department, Faculty Pharmacy, Universitas Airlangga, Surabaya, Indonesia.
Volume - 13,
Issue - 5,
Year - 2020
Epigallocatechin gallate (EGCG) is a natural product compound which has known to have anticancer activity. However, its bioavailability was low of 0.1% limited by poor stability. This study was aimed to produce microspheres as drug delivery system to improve the stability of drug. EGCG-Chitosan microspheres were formed by ionotropic gelation-aerosolization technique and were produced from chitosan and sodium tripolyphosphate. This study evaluated effect of 1, 2 and 3% of chitosan concentration on physical characteristics, stability and activity of EGCG-Chitosan microspheres. Physical characteristics were evaluated in terms of particle size, morphology, moisture content, entrapment efficiency, drug loading, yield, swelling index, physical stability and activity. Stability was evaluated by measuring size, entrapment efficiency and drug loading at 25°C and 50°C temperature for storage period of 7, 14, 21 and 30 days. Activity test was evaluated with MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay using HeLa cells. Particle sizes of formula were 2.29, 2.68, and 3.11 µm respectively with entrapment efficiency of 33.94, 52.27, 62.14% and drug loading of 23.25, 29.36, and 32.24 % correspondingly. Morphology was spherical with smooth surface. Yields were 78.25, 79.36, and 79.77% respectively. No significant differences between all formulas indicated that microspheres were stable during storage. Activity results showed that formula with chitosan 3% was the most active as anti-cervical cancer showing by IC50 was 83.58 µg/mL. EGCG-chitosan microspheres demonstrated potential as drug delivery system and as anti-cervical cancer.
Cite this article:
Noorma Rosita, Yuyun Nailufa, Dewi Melani Hariyadi. Characteristics, Stability and Activity of Epigallocatechin Gallate (EGCG)-Chitosan Microspheres: Effect of Polymer Concentration. Research J. Pharm. and Tech 2020; 13(5): 2303-2309. doi: 10.5958/0974-360X.2020.00415.1
Noorma Rosita, Yuyun Nailufa, Dewi Melani Hariyadi. Characteristics, Stability and Activity of Epigallocatechin Gallate (EGCG)-Chitosan Microspheres: Effect of Polymer Concentration. Research J. Pharm. and Tech 2020; 13(5): 2303-2309. doi: 10.5958/0974-360X.2020.00415.1 Available on: https://rjptonline.org/AbstractView.aspx?PID=2020-13-5-45
1. Saito N, Kiyono T. Basic mechanisms of high-risk human papilomavirus-induced carcinogenesis Sa: roles of E6 and E7 protein, Cancer Sci. 2007; 98: 1505-1511.
2. Koch MA, Schuffenhauer A, Scheck M, Wetzel S, Casaulta M, Odermatt A, Ertl P, Waldmamm H. Charting biologically relevant chemical space: Structural classification of natural products (SCONP). U.S.A. 2005.
3. Shukla R, Chanda N, Zambre A, Upendran A, Katti K, Kulkarni RR, Nune SK, Casteel SW, Smith CJ, Vimal JR, Cutler CS, Caldwell C, Kannan R. Luminin reseptor specific therapeutic gold nanoparticles EGCG shows efficacy in treating prostate cancer. U.S.A. 2012.
4. Zou C, Liu H, Feugang JM, Hou Z, Chow H-S, Garcia F. Green TEA compound in chemoprevention of cervical cancer. Int J Gynecol Cancer. 2010; 20(4): 617-624.
5. Wang R, Zhou, Jiang X. Reaction kinetics of degradation and epimerization of epigallocatechin gallate (EGCG): in aqueous system over a wide temperatur range. J Agric Food Chem. 2008; 56: 2694-2701.
6. Gupta, S. Kumar, P. Drug delivery using nanocarriers: Indian Perspective. Proc. Natl. Acad. Sci., India, Sect. B Biol. Sci. 2012; 82(Suppl 1): 167.
7. Yeo Y, Namjin B, and Kinam P. Microencapsulation methode for delivery of protein drug. Biothecnol. Bioprocces Eng. 2001; 6: 213-230.
8. Dube A, Nicolazzo JA, Larson L. Chitosan nanoparticles enhance the intestinal absorption of the green tea catechins (+)–catechin and (-)-epigallocatechin gallate. Eur J Pharm Sci. 2010; 41(2): 25-219.
9. Fan W, Wei Y, Hong ZN. Formation mechanism of monodisperse low molecular weight chitosan nanoparticle by ionic gelation technique. Colloids Surf B Biointerfaces. 2012; 90: 21-27.
10. Sinha VR, Singla AK, Wadhawan S, Kaushi R, Kumria R, Bansal K, Dhawan S. Chitosan microspheres as a potential carrier for drug. Int J Pharm. 2004; 274(1-2): 1-33.
11. Kumar BP, Chandiran IS, Bhavya B, Sindhuri M. Microparticulate Drug Delivery System: Review. Indian J Pharm Sci. 2011; 1: 19-37.
12. Shu XZ, Zhu KJ. The influence of multivalent phosphate structure on the properties of ionically crosslinked chitosan films for cotrolling drug release. Eur J Pharm Biopharm. 2002; 54: 235-243.
13. Ko JA, Park HJ, Hwang SJ, Park JB, Lee JS. Preparation and characterization of chitosan microparticles intended for controlled drug delivery. Int J Pharm. 2002; 249: 165-174.
14. Qiao Y, Cao J, Xie L, Shi X. Cell growth inhibition and gene expression regulation by (-)-epigalocatechin-3-gallate in human cervical cancer cells. Arch Pharm Res. 2009; 32: 1309-1315.
15. Zhang T, Zhang C, Agrahari V, Murowchick JB, Oyler NA, Youan Bi-BC. Spray drying tenofair loaded mucoadhesive and pH-sensitive microsphere intended for HIV prevention. Antiviral Res. 2013; 97: 334-346
16. Atomssa T and Gholap AV. Characterization and determination of catechins in green tea leaves using UV-visible spectrometer. J Eng Technol Res. 2015; 7: 22-31.
17. Agnihotri SA, Mallikarjuna NN, Aminabhavi TM. Recent advances on chitosan based micro and nanoparticles in drug delivery. J. Controlled Rel. 2004; 100: 5-28.
18. Yan F, Zhang C, Zheng Y, Mei L, Tang L, Song C, Sun H, Huang L. The effect of poloxamer 188 on nanoparticle morphology, size, cancer cell uptake, and cytotoxicity. Nanomedicine. 2010; 6: 170-178.
19. Sugita P, Ambarsari L, Lidiniyah. Optimization of ketoprofen loaded chitosan nanoparticle ultrasonication process. International Symposium on Applied Chemistry. Procedia Chem. 2015; 16: 673-680.
20. Ansel HC, Allen LVA, and Popovich NG. Pharmaceutical dosage forms and drug delivery system. Lippincott Williams and Wilkins, Philadelphia.1999.
21. Gold M, VePuri M, H. Block L. Suppository development and production. Pharmaceutical dosage form disperse systems. Second Edition, Revised and Expanded. 1996; 456.
22. Hagerman AE, Dean RT, Davies MJ. Radical chemistry of epigallocatechin gallate and its relevance to protein damage. Arch Biochem Biophys. 2003; 414: 115 – 120.
23. Dashora A, CP Jain. Development and Characterization of Pectin prednisolone Microspheres for Colon Targeted Delivery. Int. J.ChemTech Res. 2009; 1(3): 751-757.
24. Kamuhabwa A, Nshimo C, and de Witte, P. Cytotoxicity of Some Medicinal Plant Extracts Used in Tanzanian Tradisional Medicine. J Ethnopharmacol. 2000; 70: 143-149.