Chitosan Nanoparticles as a Drug Delivery System for 1,2,4-Triazole Derivatives: Release and Antimicrobial Activity

Authors

  • Nehal Salahuddin Department of Chemistry, Faculty of Science, Tanta University, Tanta 31527, Egypt
  • Ahmed A. Elbarbary Department of Chemistry, Faculty of Science, Tanta University, Tanta 31527, Egypt
  • Mohamed L. Salem Department of zoology, Faculty of Science, Tanta University, Tanta 31527, Egypt. Department of zoology, Faculty of Science, Tanta University, Tanta 31527, Egypt.
  • Samar Elksass Department of Chemistry, Faculty of Science, Tanta University, Tanta 31527, Egypt

DOI:

https://doi.org/10.53555/nnpbs.v2i4.755

Keywords:

Chitosan nanoparticles, 1,2,4-Triazole derivatives, Sodium tripolyphosphate, Ionic gelation, In vitro release, Antimicrobial activity

Abstract

Chitosan (CS) 1,2,4-triazole derivatives including in the formulation tripolyphosphate (TPP) as crosslinking agent was prepared by a simple one step method using ultrasonic technique. The resultant nanoparticles were characterized by x-ray diffraction (XRD), Fourier transform infrared analysis (FT-IR), thermal gravimetric analysis (TGA), derivative thermal gravimetric analysis (D-TGA), transmission electron microscopy (TEM) and scanning electron microscopy (SEM). The results indicate that spherical nanoparticles with an average size of 21, 14.6, 23.95, 29.5 nm and their standard deviation (SD) were ±5, ±5.3, ±5.3, ±7.9 nm for CSTPP, CSTPPIII, CSTPPIV and CSTPPV, respectively were successfully prepared. The in vitro release and mechanism of 1,2,4-triazoles at different pH values was investigated. From values of R2 the mechanism of drug release is following zero order mechanism at pH 6.8; however in pH 2, CSTPPIII, CSTPPIV and CSTPPV are following Hixson-Crowell, zero order and Korsmeyer-Peppas equation, respectively .The antibacterial activity against the gram negative bacteria and gram positive bacteria was examined.

References

1. Hamidi M, Azadi A, Rafiei P. Hydrogel nanoparticles in drug delivery. Adv Drug Deliv Rev 2008;
60:1638-1649.
2. Olteanu CE. Application of functionalized chitosan. Scientific Study & Research 2007; VIII(3):256-277.
3. Gavhane YN, Gurav AS, Yadav AV. Chitosan and Its applications: A review of literature. IJRPBS
2013; 4(1):312-331.
4. Fan W, Yan W, Xu Z, Ni H. Formation mechanism of monodisperse, low molecular weight chitosan
nanoparticles by ionic gelation technique. Colloids Surf, B 2012; 90:21–27.
5. Zhang H, Alsarra IA, Neau SH. An in vitro evaluation of a chitosan contain in gmultiparticulate system
for macromolecule delivery to the colon. Int J Pharm 2002; 239:197-205.
6. Ibezim EC, Andrade CT, Marcia C, Barretto B, Odimegwu DC, De Lima FF. Ionically cross-linked
chitosan/tripolyphosphate microparticles for the controlled delivery of pyrimethamine. Ibnosina J Med
BS 2011; 3(3):77-88.
7. Konecsni K, Low NH, Nickerson MT. Chitosan–tripolyphosphate submicron particles as the carrier of
entrapped rutin. Food Chem 2012; 134:1775-1779.
8. Hosseini SF, Zandi M, Rezaei M, Farahmandghavi F. Two-step method for encapsulation of oregano
essential oil in chitosan nanoparticles, Preparation, characterization and in vitro release study. Carbohydr
Polym 2013; 95:50-56.
9. Hu B, Pan C, Sun Y, Hou Z, Ye H, Hu B, Zeng XX. Optimization of fabrication parameters to produce
chitosan–tripolyphosphate nanoparticles for delivery of tea catechins. J Agric Food Chem 2008; 56:7451-
7458.
10. Hemant KSY, Singh MN, Shivakumar HG. Chitosan/sodium tripolyphosphate cross linked
microspheres for the treatment of gastric ulcer. Der Pharmacia Lettre 2010; 2(6):106-113.
11. Sharma V, Shrivastava B, Bhatia R, Bachwani M, Khandelwal R, Ameta J. Exploring potential of 1,2,4-
triazole: A brief review. Pharmacologyonline 2011; (1):1192-1222.
12. Weidinger H, Kranz J. Synthesen mit imidsäureestern, II. Synthese von 1,3,4-thiodiazolen. Chem Ber
1963; 96(4):1059-1063.
13. Cansiz A, Çetin A, Kutulay P, Koparir M. Synthesis of tautomeric forms of 5-(2-Hydroxyphenyl)-4-
substituted-3H-1,2,4-triazole-3-thione. Chem Asian J 2009; 21(1):617-626.
14. Lawrie G, Keen I, Drew B, Chandler-Temple A, Rintoul L, Fredericks P, Grøndahl L. Interactions
between alginate and chitosan biopolymers characterized using FTIR and XPS. Bio-macromolecules
2007; 8:2533–2541.
15.Zamora-Mora V, Fernández-Gutiérrez M, San Román J, Goya G, Hernández R, Mijangos C. Magnetic
core–shell chitosan nanoparticles, rheological characterization and hyperthermia application. Carbohydr
Polym 2014; 102:691–698.
16. Jingou J, Shilei H, Weiqi L, Danjun W, Tengfei W, Yi X. Preparation characterization of hydrophilic
and hydrophobic drug in combine loaded chitosan/cyclodextrin nanoparticles and in vitro release study.
Colloids Surf, B 2011; 83:103-107.
17. Tang ESK, Huang M, Lim LY. Ultrasonication of chitosan and chitosan- nanoparticles. Int J Pharm
2003; 265:103-114.
18. Qi L, Xu Z, Jiang X, Hu C, Zou X. Preparation and antibacterial activity of chitosan nanoparticles.
Carbohydr Res 2004; 339:2693-2700.
19. Peniche C, Zaldivar D, Bulay A, Roman JS. Study of the thermal degradation of poly (furfuryl
methacrylate) by thermogravimetry. Polym Degrad Stab1993; 40:287-295.
20. Helander IM, Nurmiaho-Lassila EL, Ahvenainen R, Rhoades J, Roller S. Chitosan disrupts the barrier
properties of the outer membrane of Gram-negative bacteria. Int J Food Microbiol 2001; 71:235-244

Downloads

Published

2016-04-30

How to Cite

Salahuddin, N., Elbarbary, A. A., Salem, M. L., & Elksass, S. (2016). Chitosan Nanoparticles as a Drug Delivery System for 1,2,4-Triazole Derivatives: Release and Antimicrobial Activity. Journal of Advance Research in Pharmacy and Biological Science (ISSN 2208-2360) , 2(4), 64-73. https://doi.org/10.53555/nnpbs.v2i4.755