FORMULATION OPTIMIZATION AND CHARACTERIZATION OF GANCICLOVIR LOADED DRY CHITOSAN NANOPARTICLES
DOI:
https://doi.org/10.22159/ajpcr.2017.v10i3.16205Abstract
ABSTRACT
Objective: The objective of this work was to formulate, optimize, and characterize ganciclovir (GCV) loaded dry chitosan nanoparticles (CSNPs).
Methods: The GCV loaded CSNPs was prepared by ionic gelation method. Box–Behnken design was employed to optimize the influence of independent
process and formulation variables like drug to polymer ratio, concentration of sodium tripolyphosphate, and stirring time (min) on the dependent
variables such as particle size (PS) and drug encapsulation efficiency (% EE). The optimum conditions were determined by regression analysis of the
output data.
Results: The independent variables had interactive effects and they affected both the responses. The optimum formulation had PS within the range of
100-120 nm and % EE between 85% and 86%. The prepared GCV loaded CSNPs were dried by fluidized bed drying method. Fourier transform infrared
spectra showed there was no physicochemical interaction between GCV and CS. Powder X-ray diffraction study showed less intense crystalline peaks
indicated that GCV may exist in the formulation as amorphous nanodispersion or molecular dispersion form. Differential scanning calorimetry study
was performed which indicated that the drug was molecularly dispersed inside the matrix of CS. Higuchi model was the best to fit the in vitro release
data for the GCV loaded CSNPs.
Conclusion: From the results, it can be concluded that the GCV loaded dry CSNPs were formulated, optimized, and characterized using desired
pharmacotechnical properties.
Keywords: Chitosan nanoparticles, Box–Behnken design, Sodium tripolyphosphate, Ionic gelation.
Downloads
References
REFERENCES
Hamidi M, Azadi A, Rafiei P. Hydrogel nanoparticles in drug delivery. Adv Drug Deliv Rev 2008;60(15):1638-49.
Agnihotri SA, Mallikarjuna NN, Aminabhavi TM. Recent advances on chitosan-based micro-and nanoparticles in drug delivery. J Control Release 2004;100(1):5-28.
Wang XY, Jiang XP, Li Y, Zeng S, Zhang YW. Preparation Fe3O4@chitosan magnetic particles for covalent immobilization of lipase from Thermomyces lanuginosus. Int J Biol Macromol 2015;75:44-50.
Anderson RD, Griffy KG, Jung D, Dorr A, Hulse JD, Smith RB. Ganciclovir absolute bioavailability and steady-state pharmacokinetics after oral administration of two 3000-mg/d dosing regimens in human immunodeficiency virus-and cytomegalovirus-seropositive patients. Clin Ther 1995;17(3):425-32.
Li M, Si L, Pan H, Rabba AK, Yan F, Qiu J, et al. Excipients enhance intestinal absorption of ganciclovir by P-gp inhibition: Assessed in vitro by everted gut sac and in situ by improved intestinal perfusion. Int J Pharm 2011;403(1-2):37-45.
Merodio M, Arnedo A, Renedo MJ, Irache JM. Ganciclovir-loaded albumin nanoparticles: Characterization and in vitro release properties. Eur J Pharm Sci 2001;12(3):251-9.
Ren J, Zou M, Gao P, Wang Y, Cheng G. Tissue distribution of borneol-modified ganciclovir-loaded solid lipid nanoparticles in mice after intravenous administration. Eur J Pharm Biopharm 2013;83(2):141-8.
Kajiwara E, Kawano K, Hattori Y, Fukushima M, Hayashi K, Maitani Y. Long-circulating liposome-encapsulated ganciclovir enhances the efficacy of HSV-TK suicide gene therapy. J Control Release 2007;120(1-2):104-10.
Georgieva D., Kostova B., Rachev D. Nanosized polymeric carriers for dexamethasone controlled delivery. J Chem 2015;7 Suppl 3:1767-72.
Ruby JJ, Pandey VP. Chitosan nanoparticles as a nasal drug delivery for memantine hydrochloride. Int J Pharm Pharm Sci 2014;7(1):34-7.
Calvo P, Remuñan-López C, Vila-Jato JL, Alonso MJ. Chitosan and chitosan/ethylene oxide-propylene oxide block copolymer nanoparticles as novel carriers for proteins and vaccines. Pharm Res 1997;14 Suppl 10:1431-6.
Egashira K. Pharmaceutical Composition Containing Statin-Encapsulated Nanoparticle. Google Patents; 2007.
Bei D, Marszalek J, Youan BB. Formulation of dacarbazine-loaded cubosomes-part I: Influence of formulation variables. AAPS Pharm Sci Technol 2009;10(3):1032-9.
Elmowafy E, Osman R, El-Shamy AE, Awad GA. Stable colloidal chitosan/alginate nanocomplexes: Fabrication, formulation optimization and repaglinide loading. Int J Pharm Pharm Sci 2014;6(2):520-5.
Desai MP, Labhasetwar V, Amidon GL, Levy RJ. Gastrointestinal uptake of biodegradable microparticles: Effect of particle size. Pharm Res 1996;13(12):1838-45.
Ray M, Pal K, Anis A, Banthia AK. Development and characterization of chitosan-based polymeric hydrogel membranes. Des Monomers Polym 2010;13(3):193-206.
Sambandam B, Kumar S, Ayyaswamy A, Yadav BV, Thiyagarajan D. Synthesis and characterization of poly DL lactide (PLA) nanoparticles for the delivery of quercetin. Int J Pharm Pharm Sci 2015;7 Suppl 5:42-9.
Guhagarkar SA, Gaikwad RV, Samad A, Malshe VC, Devarajan PV. Polyethylene sebacate-doxorubicin nanoparticles for hepatic targeting. Int J Pharm 2010;401(1-2):113-22.
Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm 2010;67:217-23.
Dangi RS, Shakya S. Preparation, optimization and characterization of PLGA nanoparticle. Int J Pharm Life Sci 2013;4(7):2810-8.
Bhumkar DR, Pokharkar VB. Studies on effect of pH on cross-linking of chitosan with sodium tripolyphosphate: A technical note. AAPS Pharm Sci Technol 2006;7(2):E50.
Anbarasan B, Menon VV, Niranjana V, Sundara R. Optimization of the formulation and in-vitro evaluation of chloroquine loaded chitosan nanoparticles using ionic gelation method. J Chem Pharm Sci 2013;6 Suppl 1:66-72.
Tharanathan RN, Kittur FS. Chitin - the undisputed biomolecule of great potential. Crit Rev Food Sci Nutr 2003;43(1):61-87.
Cordova M, Cheng M, Trejo J, Johnson SJ, Willhite GP, Liang JT, et al. Delayed HPAM gelation via transient sequestration of chromium in polyelectrolyte complex nanoparticles. Macromolecules 2008;41 Suppl 12:4398-404.
Singh J, Gupta S, Kaur H. Prediction of in vitro drug release mechanisms from extended release matrix tablets using SSR/R2 technique. Trends Appl Sci Res 2011;6 Suppl4:400-9.
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.
