ROSUVASTATIN CALCIUM LOADED CHITOSAN NANOPARTICLES: PREPARATION EVALUATION AND IN VITRO RELEASE STUDIES
Keywords:Rosuvastatin calcium, Biodegradable, Particle size analysis, Ionotropic gelation
Objective: The objective of the present study was to develop sustained release biodegradable polymeric nanoparticles of rosuvastatin calcium.
Methods: Nanoparticles were prepared by modified ionotropic gelation method using 3² full factorial designs. From the preliminary trials, the constraints for independent variables X1 (concentration. of chitosan) and X2 (concentration. of sodium tripolyphosphate) have been fixed. Factors included concentration of chitosan and sodium tripolyphosphate, have been examined to investigate effect on particle size, encapsulation efficiency, zeta potential, % release, scanning electron microscopy, Fourier transfer infrared study and X-ray diffraction and release study of rosuvastatin calcium nanoparticles. 0
Results: The prepared nanoparticles were white, free-flowing and spherical in shape. The infrared spectra showed stable character of rosuvastatin calcium in the drug-loaded nanoparticles and revealed the absence of drug polymer interactions. The chitosan nanoparticles have a particle diameter ranging approximately 114.5±3.61 to 724±.2.51 nm and a zeta potential-13.12 to-52.63 mV. The in vitro release behavior from all the drug loaded batches were found to follow first order and provided sustained release over a period of 10 h. The Zeta potential of all the batches were in the range of-13.12 to-52.63 mv. The release profiles of all batches were very well fitted by Korsmeyer Peppas model.
Conclusion: The best-fit release kinetics was achieved with Korsmeyer peppas model. The release of rosuvastatin calcium was influenced by the drug to polymer ratio and particle size. These results indicate that rosuvastatin calcium nanoparticles could be effective in sustaining drug release for a prolonged period.
Drug bank of Rosuvastatin calcium, DB01098. Available from: https://www.accessdata.fda.gov/drugsatfda_dochitosan/label/2005/21366slr005lbl.pdf. [Last accessed on 01 Jan 2017]
Michael S. Chemical pharmacokinetic and pharmacodynamic properties of statins: an update. Blackwell Publishing Fundamental Clin Pharmaco 2004;19:117–25.
Rai Muhammad Sarfraz, M Ahmad, Mahmood A. Development and evaluation of rosuvastatin calcium-based microparticles for solubility enhancement: an in vitro study. Adv Polymer Technol 2017;36:1-4.
Venkateswara R, Navaneetha K. Formulation and evaluation of sustain release tablets of Ramipril. Pharmatutor 2014;2:110-9.
Bhatia S. Nanoparticles types, classification, characterization, fabrication methods and drug delivery applications; natural polymer drug delivery systems, international springer publishing Switzerland; 2016. p. 33-93.
Ranjit K, Abdul B. Nanoparticles: an overview preparation, characterization and applications. Int Res J Pharm 2013;4:48-57.
Saleem V, Azharuddin SK, Ali S, Patil C, Studies on different chitosan polyelectrolyte complex hydrogels for modified release of diltiazem hydrochloride. Int J Pharm Pharma Sci 2010;2:64-7.
Chouksey R, Kumar J, Pandey H, Maithil A. Development and bioavailability studies of atorvastatin nanoemulsion. Inter J Pharm Life Sci 2011;2:982-8.
Elgadir M Abd. Impact of chitosan composites and chitosan nanoparticle composites on various drug deliveries. J Food Drug Anal 2015;23:619-29.
Hirpara R. Long circulating PEGylated-chitosan nanoparticles of rosuvastatin calcium: development and in vitro and in vivo evaluations. Inter J Bio Macro 2018;107:2190–200.
Sharare N. Chitosan nanoparticles and their applications in drug delivery: a review. Cur Res Drug Dis 2014;1:17-25.
Sangeetha S, Deepika K, Thrishala B, Chaitanya CH, Harish G, Damodharan N. Formulation and in vitro evaluation of sodium alginate nanospheres containing Ofloxacin. Intel J Appl Pharm Sci 2010;2:1-3.
Srikanth Reddy S, Suresh G. Design and evaluation of self-nano emulsifying drug delivery systems of manidipine for enhancement of solubility. Asian J Pharm Clin Res 2019;12:288-95.
Suresh Kumar R, Debnath S, Ganesh GNK. Chitosan nanoparticles by ionotropic gelation containing L-arginine. Res J Pharm Tech 2009;2:80-5.
Calvo P, Remunan Lopez C, Vila Jato JL, Alonso MJ. Novel hydrophilic chitosan-polyethylene oxide nanoparticles as protein carriers. J Appl Polym Sci 1997;63:125-32.
Purwantiningsih S, Laksmi A, Lidiniyah. Optimization of ketoprofen-laoded chitosan nanoparticles by the ultrasonication process. Procedia Chem 2015;6:673–80.
Trideva Sastri K, Radha GV. Development of self nano-emulsifying drug delivery system for antihypertensive agent felodipine: a systematic approach for lipid nanoformulation with improved oral bioavailability in rats. Int J Appl Pharm 2020;12:86-94.
Dandagi P, Rath SP, Gadad AP, Mastiholimath V. Taste masked quinine sulphate loaded solid lipid nanoparticles for flexible paediatric dosing. Indian J Pharma Edu Res 2014;48:93-9.
Shawky N, Malak A. Formulation of coated polymer reinforced gellan gum beads of tizanidine HCL using fractional factorial design. Int J Pharm Pharm Sci 2012;4:369-79.
ICH Q1A (R2), Stability Testing of New Drug Substances and Products, International Conference on Harmonization. U. S. Department of Health and Human Service Food and Drug Administration; 2003. p. 4–20.
Bohrey S, Chourasiya V, Pandey A. Polymeric nanoparticles containing diazepam: preparation, optimization, characterization, in vitro drug release and release kinetic study. Nano Convergence 2016;3:1-7.
Bhoskar M, Patil P. Development and evaluation of paclitaxel loaded nanoparticles using factorial design. Int J Curr Pharm Res 2015;7:64-72.
Sanjaymitra PVSS, Ganesh GNK. Dissolution and solubility enhancement strategies: current and novel. J Crit Rev 2018;5:1-10.
Jadhav P, Yadav A. Formulation, optimization, and in vitro evaluation of polymeric nanosuspension of flurbiprofen. Asian J Pharm Clin Res 2019;12:183-91.
Gulati N, Nagaich U, Saraf SA. Intranasal delivery of chitosan nanoparticles for migraine therapy. Sci Pharm 2013;81:843–54.
Raman Rohilla, Tarun G, Bariwal J, Amit K, Goutam R. Development, optimization and characterization of glycyrrhetinic acid–Chitosan nanoparticles of atorvastatin for liver targeting. Drug Delivery 2016;23:2290-7.