OPTIMIZATION OF FORMULATION PARAMETERS AND CHARACTERIZATION OF SIMVASTATIN LOADED CHITOSAN NANOPARTICLES.
- Research scholar, PRIST University, Puducherry campus,24/4, Uruvaiyar road, Abishegapakkam, Puducherry.
- Director, PRIST University, Puducherry campus,24/4, Uruvaiyar road,Abishegapakkam, Puducherry.
- Teaching fellow, Department of biotechnology, Anna University, Chennai.
- Abstract
- Keywords
- References
- Cite This Article as
- Corresponding Author
This study aimed to optimize and characterize formulation factors in the preparation of drug-loaded polymeric nanoparticulate drug delivery system by employing response surface methodology (design of expert– DOE). Nanoparticles were prepared by three different methods namely solvent evaporation, solvent diffusion, and cross-linking method. Effect of important factors like method of preparation, surfactant type, stabilizer type on particle size, and percentage entrapment efficiency were studied using DOE. The prepared formulations show particle size and % entrapment efficiency in the range of 602.11 ± 12.5 to 1005.55 ±98.6 nm and 77.01±0.003 to 97.01±0.21% respectively. Based on the result formulation prepared with nonionic surfactant (Tween 80), synthetic polymeric stabilizer (poly vinyl alcohol- PVA) and solvent evaporation method were found to be effective. After selection of optimized formulation, twelve formulations were prepared by altering key processing parameters like stabilizer and surfactant concentration and effective formulation was selected on the basis of in vitro release. Among various concentrations, formulation with combination of 0.50% w/v of PVA and 0.02% w/v of Tween 80 had sustain release property, stability and biocompatibility.
- Abdel-MottalebMMA,Mortada ND, El-ShamyAA,Awad GAS.( 2009) Physically cross-linked polyvinyl alcohol for the topical delivery of fluconazole.DrugDevInd Pharm. 35(3), 311–320.
- Agnihotri SA, MallikarjunaNN, Aminabhavi TM (2004 ) Recent advances on chitosan-based micro- and nanoparticles in drug delivery. J Controlled Release. 100, 5–28.
- Alsante KM, Hatajik TD, Lohr LL, et al., (2003)Solving impurity/degradation problems: case studies S. Ahuja, K.M. Alsante (Eds.), Handbook of Isolation and Characterization of Impurities in Pharmaceutical, Academics Press, New York, p. 380
- Boccardi G. (2005) Oxidative susceptibility testing S.W. Baertschi (Ed.), Pharmaceutical Stress Testing-Predicting Drug Degradation, Taylor and Francis, New York p. 220.
- Chawla V, Tiwary AK, Gupta S (2000) Characterization of polyvinylalcohol microspheres of diclofenac sodium: Application of statistical design. Drug DevInd Pharm. 26, 675–680.
- Chen JP, Yang PC, Ma YH, Wu T (2011) Characterization of chitosan magnetic nanoparticles
- for in situ delivery of tissue plasminogen activator. CarbohydrPolym. 84, 364–372.
- Danhier, F.; Ucakar, B.; Vanderhaegen, M.-L.; Brewster, M.E.; Arien, T.; Préat, V (2014). Nanosuspension for the delivery of a poorly soluble anti-cancer kinase inhibitor. Eur. J. Pharm Biopharm. 88, 252–260.
- Dodane V, Vilivalam VD (1998) Pharmaceutical applications of chitosan. PSTT.6, 246–253.
- Dudhani AR, Kosaraju SL (2010) Bioadhesive chitosan nanoparticles: Preparation and characterization. Carbohydrate Polym. 81, 243–251.
- Fu Y, Kao WJ (2010) Drug release kinetics and transport mechanisms of non-degradable and degradable polymeric delivery systems. Expert Opin Drug Deliv.7, 429–444.
- Garud N, Garud A (2012) Preparation and in-vitro evaluation of metformin microspheres using non-aqueous solvent evaporation technique. Trop JPharmaceut Res. 11(4), 577–583.
- George, M.; Ghosh, I. (2013)Identifying the correlation between drug/stabilizer properties and critical quality attributes (CQAs) of nanosuspension formulation prepared by wet milling technology. Eur.J.Phar.Sci. 48(1-2):142-152.
- H A SS, GPD C, Ravindran BR (2014) BSA Nanoparticle Loaded Atorvastatin Calcium - A New Facet for an Old Drug. PLoS ONE 9(2): e86317. doi:10.1371/journal.pone.0086317.
- Hoeller S, Sperger A, Valenta C (2009) Lecithin based nanoemulsions: a comparative study of the influence of non-ionic surfactants and the cationic phytosphingosine on physicochemical behaviour and skin permeation.Int J Pharm. 370(1–2), 181–186.
- Huanbutta K, Sriamornsak P, Luangtana-Anan M, Limmatvapirat S, Puttipipatkhachorn S, et al. (2013) Application of multiple stepwise spinning disk processing for the synthesis of poly(methyl acrylates) coated chitosan diclofenac sodium nanoparticles for colonic drug delivery. Eur J Pharm Sci. 50, 303–311.
- Jain A, Jain SK (2013) Formulation and optimization of temozolomide nanoparticles by 3 factor 2 level factorial design. Biomatter. 3, 1-8.
- JuntanonK,NiamlangS,RujiravanitR,Sirivat A (2008) Electrically controlled release of sulfosalicylic acid from crosslinked poly(vinyl alcohol) hydrogel. Int J Pharm. 356(1–2), 1–11.
- KhanAA, MudassirJ,Mohtar N, Darwis Y (2013) Advanced drug delivery to the 680 lymphatic system: Lipid-based nanoformulations.Int J Nanomed. 681, 2733–2744.
- Kim, S.; Lee, J (2010). Effective polymeric dispersants for vacuum, convection and freeze drying of drug nanosuspensions. Int. J. Pharm.397, 218–224.
- Krishna Sailaja A, Amareshwar P, Chakravarty P (2011) Different techniques used for the preparation of nanoparticles using natural polymers and their application. Int J Pharm PharmSci. 3(2), 45–50.
- Liu, P.; Viitala, T.; Kartal-Hodzic, A.; Liang, H.; Laaksonen, T.; Hirvonen, J.; Peltonen, L (2015) Interaction studies between indomethacin nanocrystals and PEO/PPO copolymer stabilizers. Pharm. Res.32, 628–639.
- Ludwig A ( 2005) The use of mucoadhesive polymers in ocular drug delivery.AdvDrugDeliv Rev . 571, 595–639.
- Mahesh, K.V.; Singh, S.K.; Gulati, M (2014). A comparative study of top-down and bottom-up approaches for the preparation of nanosuspensions of glipizide. Powder Technol. 256, 436–449.
- Mao S, Shi Y, Li L,et al (2008)Effects of process and formulation parameters on characteristics and internal morphology of poly(d,l-lactide-co-glycolide) microspheres formed by the solvent evaporation method.Eur J Pharm Biopharm. 68, 214–223.
- Mennini N, Furlanetto S, Maestrelli F, Pinzauti S, Mura P (2008) Response surface methodology in the optimization of chitosan-Capectinate bead formulations. Eur J Pharm Sci. 35, 318–325.
- Mitra A, Lin S (2003) Effect of surfactant on fabrication and characterization of paclitaxel-loaded polybutylcyanoacrylatenanoparticulate delivery systems J Pharm Pharmacol. 55, 895–902.
- Murtaza G (2011) Development of glutaraldehydecrosslinked metronidazole loaded chitosan microcapsules: Analysis of dissolution data using DD solver. Latin Am J Pharm. 30, 1389–1395.
- Ngwa G (2010) Forced degradation studies as an integral part of HPLC stability indicating method development Drug Deliv. Technol. 10 (5), pp. 56–59
- Patil SS, Mohan Gupta VR, Gupta SK, Hiremath D (2014) Formulation and characterization of TPP cross-linked chitosan microspheres loaded with lornoxicam. J Biomed Pharm Res. 3,51–58.
- Peltonen, L.; Hirvonen, J 2010 Pharmaceutical nanocrystals by nanomilling: Critical process parameters, particle fracturing and stabilization methods. J. Pharm. Pharmacol.62, 1569–1579.
- PillayV,SibandaW,Danckwerts MP (2005) Sequential design of a novel PVA-based crosslinkedethylenichomopolymer for extended drug delivery. Int J Pharm. 301(1–2), 89–101.
- PrakashKatakam, YadagiriPhalguna, DommatiHarinarayana (2014) Formulation, characterization and in vitro evaluation of capecitabine loaded polycaprolactone-chitosan nanospheres. Bangladesh PharmaceutJ.17(1), 18–24.
- Prieto C, Calvo L (2013) Performance of the biocompatible surfactant tween 80, for the formation of microemulsions suitable for new pharmaceutical processing. J ApplChem.2013, 1–10.
- Quintanar-Guerrero D, Fessi H, Allémann E, et al (1996) Influence of stabilizing agents and preparative variables on the formation of poly(d,l-lactic acid) nanoparticles by an emulsification-diffusion technique. Int J Pharm. 143, 133–141.
- Ravi Sankar V, Dhachinamoorthi D, Chandra Shekar KB( 2013) Formulation and evaluation of novel aspirin nanoparticles loaded suppositories. J PharmaceutSci. 13, 258–266.
- Reis CP, Neufeld RJ, RibeiroAJ, Veiga F (2006) Nanoencapsulation I. Methods for preparation of drug-loaded polymeric nanoparticles.Nanomedicine. 2,8–21.
- Riva R, Ragelle H, Rieux A, Duhem N, Jerome C, Preat V (2011) Chitosan and chitosan derivatives in drug delivery and tissue engineering. AdvPolym Sci. 244, 19–44.
- Roy P, Shahiwala A (2009) Statistical optimization of ranitidine HCl floating pulsatile delivery system for chronotherapy of nocturnal acid breakthrough. Eur J Pharm Sci. 37, 363–369.
- Sabir A, Evans B, Jain S (2001) Formulation and process optimization to eliminate 735 picking from market image tablets.Int J Pharm. 215, 123–135.
- Singh B, Kumar R, Ahuja N (2005) Optimizing drug delivery systems using 737 systematic “design of experiments”. Part I: Fundamental aspects.CritRevTher Drug Carrier Syst. 22, 27–105.
- Wong HL, Chattopadhyay N, Wu XY, Bendayan R (2010) Nanotechnology applications for improved delivery of antiretroviral drugs to the brain.Adv Drug Delivery Rev. 62, 503–517.
- Valo, H.; Arola, S.; Laaksonen, P.; Torkkeli, M.; Peltonen, L.; Linder, M.B.; Serimaa, R.; Kuga, S.; Hirvonen, J.; Laaksonen, T (2013) Drug release from nanoparticles embedded in four different nanofibrillar cellulose aerogels. Eur. J. Pharm. Sci. 50, 69–77.
[N. Selvasudha M. Pharm, Kailasam Koumaravelou, and N. Sri Durgadevi M.Pharm. (2017); OPTIMIZATION OF FORMULATION PARAMETERS AND CHARACTERIZATION OF SIMVASTATIN LOADED CHITOSAN NANOPARTICLES. Int. J. of Adv. Res. 5 (Feb). 2386-2400] (ISSN 2320-5407). www.journalijar.com
PRIST University, Puducherry campus, 24/4, Uruvaiyar road, Abishegapakkam Puducherry.