DESIGN AND EVALUATION OF FLUTAMIDE-LOADED POLYCAPROLACTONE NANOPARTICLES BY 23 FACTORIAL DESIGN AND NANOPRECIPITATION METHOD
DOI:
https://doi.org/10.22159/ajpcr.2018.v11s4.31739Keywords:
Nanoprecipitation method, Polymeric nanoparticles, Prostate cancerAbstract
Objective: The present work was aimed to prepare and evaluate polymeric nanoparticles (NPs) of flutamide by nanoprecipitation method and factorial. The influences of various formulation components such as polymer, organic phase volume, and surfactant on the characteristics of NPs were investigated.
Methods: The polycaprolactone (PCL) loaded with drug was evaluated for surface morphology, surface charge, particles size, encapsulation efficiency, drug content, and in vitro release studies. Fourier transform infrared studies were indicated no interaction between the drug and polymer.
Results: The results of the drug release study of NPs may fit with different kinetic equations. The particle size varied from 128 to 317 nm and zeta potential was in negative and its value found to be - 46.4 mv. The content of flutamide was found in between 74%±0.72 to 92%±0.53 in flutamide loaded PCL NPs. The minimum and maximum entrapment efficiencies were found to be of 75%±0.66 and 92%±0.70. The percentage yields of all formulations were in the range of 46.05%±1.56–86.78%±1.32. The in vitro drug release followed zero order with sustained behavior for a period of 24 h. Results of accelerated storage conditions of optimized formulation revealed that no significant changes in formulation F2.
Conclusion: The present investigation opens new frontiers in developing flutamide NPs for targeting delivery to the prostate for the prostate cancer treatment which also overcome the problems associated with conventional formulations such as multiple-dose therapy, poor patient compliance, and high treatment cost.
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Ferlay I, Shin HR, Bray F. Cancer Incidence and Mortality Worldwide: IARC Cancer Base. Lyon: International Agency for Research on Cancer; 2010. p. 45-66.
Goldspiel BR, Kohler DR. Flutamide: An antiandrogen for advanced prostate cancer. DICP 1990;24:616-23.
Elgindy N, Elkhodairy K, Molokhia A, Elzoghby A. Lyophilization monophase solution technique for improvement of the physicochemical properties of an anticancer drug, flutamide. Eur J Pharm Biopharm 2010;74:397-405.
Sandrap P, Moes AJ. Influence of manufacturing parameters on the size characteristics and release profiles of nifedipine from poly (D, L-lactide-co-glycolide) microspheres. In J Pharm 1993;98:157-164.
Baumgartner S, Kristl J, Vrecer F, Vodopivec P, Zorko B. Optimisation of floating matrix tablets and evaluation of their gastric residence time. Int J Pharm 2000;195:125-35.
Murthy RS. Controlled and Novel Drug Delivery. 1st ed. New Delhi: CBS Publisher; 1997. p. 27-51.
Sinha VR, Bansal K, Kaushik R, Kumria R, Trehan A. Poly-epsilon-caprolactone microspheres and nanospheres: An overview. Int J Pharm 2004;278:1-23.
Kumari A, Yadav SK, Yadav SC. Biodegradable polymeric nanoparticles based drug delivery systems. Colloids Surf B Biointerfaces 2010;75:1-8.
Ige PP, Dipsingh SN. Preparation and in vitro-in vivo evaluation of surface-modified poly(lactide-co-glycolide) nanoparticles as controlled release carriers for flutamide delivery. J Microencapsul 2015;32:231-9.
Yadav BV, Ravichandiran V, Kumar SS. Preparation and characterization of gemcitabine loaded mpeg-PCL polymeric nanoparticles for improved transportation across blood brain barrier. Int J Pharm Sci 2016;8:82-90
Martel CL, Gumerlock PH, Meyers FJ, Lara PN. Current strategies in the management of hormone refractory prostate cancer. Cancer Treat Rev 2003;29:171-87.
Surenya RS, Snima KS, Shantikumar N, Kumar LV. Assessment of poly (vinyl alcohol) coated flutamide nanoparticulates and their efficacy on prostate cancer cells. Curr Drug Deliv 2016;2:312-39.
Elzoghby AO, Helmy MW, Samy WM, Elgindy NA. Novel ionically crosslinked casein nanoparticles for flutamide delivery: Formulation, characterization, and in vivo pharmacokinetics. Int J Nanomedicine 2013;8:1721-32.
Lachman L, Liberman HA. The Theory and Practice of Industrial Pharmacy. 3rd ed. Philadelphia, PA: Lea and Febiger; 1990. p. 171-96.
Song X, Zhao Y, Hou S, Xu F, Zhao R, He J, et al. Dual agents loaded PLGA nanoparticles: Systematic study of particle size and drug entrapment efficiency. Eur J Pharm Biopharm 2008;69:445-53.
Cegnar M, Kos J, Kristl J. Cystatin incorporated in poly (lactide-co-glycolide) nanoparticles: Development and fundamental studies on preservation of its activity. Eur J Pharm Sci 2004;22:357-64..
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