FORMULATION AND EVALUATION OF CHITOSAN NANOPARTICLES FOR IMPROVED EFFICACY OF ITRACONAZOLE ANTIFUNGAL DRUG
DOI:
https://doi.org/10.22159/ajpcr.2018.v11s4.31723Keywords:
Itraconazole, Nanoparticles, Ionic gelation method, ChitosanAbstract
Objective: The main objective of the study was to formulate and evaluate the chitosan nanoparticles to improve the therapeutic efficacy of itraconazole by loading in nanoparticle drug delivery system. Designing the formulation of the drug itraconazole prolongs the therapeutic concentration of the drug in the blood and which will lower the frequency of dosing and also improves the efficacy of the drug.
Methods: Itraconazole nanoparticles are prepared by ionic gelation method; here, chitosan is used as polymer. The formulated nanoparticles are evaluated for external morphological studies by scanning electron microscope (SEM), drug content, in vitro drug release studies, as well as infrared (IR) spectral analysis.
Results: The Fourier transform IR spectra show that there was no interaction between drug and polymers; hence, they are compatible. Percentage entrapment efficiency, drug content, and percentage yield were higher for F3 formulation. The particle size analysis shows that every particle in the formulations gave the range of 148–227 nm, respectively; increasing in the particle size observed with varying concentration of polymer. SEM analysis of the nanoparticles shows that all the formulations were spherical and smooth with ideal surface morphology. As the concentration of polymer, the drug release decreased proportionally. The stability studies were carried out on the optimized formulation for 2 months at 30±2°C and 60±5% RH and 40±2°C and 75±5% RH; finally, it was observed that there was no change in drug content and in vitro drug release profile even after storage at 30±2°C and 60±5% RH and 40±2°C and 75±5% RH for 2 months.
Conclusion: Itraconazole is one among the most widely used antifungal drugs. Designing the formulation of drug itraconazole prolongs therapeutic drug concentration in the blood and decreases dosage frequency and also enhances the efficacy of drug.
Downloads
References
Jain NK. Controlled and Novel Drug Delivery. 1st ed. New Delhi: CBS Publishers; 2005. p. 452.
Pappas PG, Kauffman CA, Andes D. Clinical practice guidelines for the management of candidiasis: Update by the infectious diseases society of America. Clin Infect Dis 2009;48:503-5.
Soppimath KS, Aminabhavi TM, Kulkarni AR, Rudzinski WE. Biodegradable polymeric nanoparticles as drug delivery devices. J Control Rel 2001;70:1-20.
Gevaria HB, Gami S, Patel N. Formulation and characterization of levofloxacin – Loaded biodegradable nanoparticles. Asain J Pharm 2011;1:114-9.
Yvette NK, Robert G, Eric A. Preparation and characterization of sterile and freeze-dried nanoparticles. Int J Pharm 2002;233:239-52.
Clisson ME, Pinto-Alphandary H, Ourevitch M, Andremont A, Couvreur P. Development of ciprofloxacin-loaded nanoparticles: A physicochemical study of the drug carrier. J Control Release 1998;56:23-32.
Abazinge M, Jackson T, Yang Q. Comparision of in vitro and in vivo release characteristics of sustained release of loxacin drug delivery. Drug Deliv 2000;7:77-81.
Benybaby N, Harsha NS, Jayaveera KN, Abraham A. Formulation and evaluation of levofloxacin nanoparticles by ionic gelation method. J Pharm Pharm Sci 2012;1:7-9.
Jeganath S, Senthilkumaran K. Development and evaluation of sustained release aceclofenac microspheres using chitosan polymers and techniques in management of rheumatoid arthritis. Int J Res Pharm Nano Sci 2012;1:27-34.
Tamizhrasi1 S, Shukla A, Shivkumar T, Rathi V, Rathi JC. Formulation and evaluation of lamivudine loaded polymethacrylic acid nanoparticles. Int J Pharm Tech Res 2009;3:411-5.
Cetin M, Atila A, Kadioglu Y. Formulation and in vitro characterization of eudragit l100 and eudragit L100-PLGA nanoparticles containing diclofenac sodium. Aaps Pharm Tech 2010;3:1250-6.
Zhang G, Niu A, Peng S, Jiang M, Fengtu Y, Li M, et al. Formation of novel polymeric nanoparticles. Accounts Chem Res 2001;34:249-56.
Leroux JC, Allémann E, De Jaeghere F, Doelker E, Gurny R. Biodegradable nanoparticles—from sustained release formulations to improved site specific drug delivery. J Control Release 1996;3:339-50.
Leroueil-Le Verger M, Fluckiger L, Kim YI, Hoffman M, Maincent P. Preparation and characterization of nanoparticles containing an antihypertensive agent. Eur J Pharm Biopharm 1998;46:137-43.
Song CX, Labhasetwar V, Murphy H, Qu X, Humphrey WR, Shebuski RJ, et al. Formulation and characterization of biodegradable nanoparticles for intravascular local drug delivery. J Control Release 1997;43:197-212.
Niwa T, Takeuchi H, Hino T, Kunou N, Kawashima Y. Preparations of biodegradable nanospheres of water-soluble and insoluble drugs with D, L-lactide/glycolide copolymer by a novel spontaneous emulsification solvent diffusion method, and the drug release behavior. J Control Release 1993;25:89-98.
Ubrich N, Bouillot P, Pellerin C, Hoffman M, Maincent P. Preparation and characterization of propranolol hydrochloride nanoparticles: A comparative study. J Control Release 2004;2:291-300.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.