PREPARATION AND CHARACTERIZATION OF METFORMIN LOADED STEARIC ACID COUPLED F127 NANOPARTICLES
DOI:
https://doi.org/10.22159/ajpcr.2018.v11i8.26444Keywords:
Metformin HCl, Nanoparticles, Pluronic F127, Polyvinyl alcohol, Stability studiesAbstract
Objective: The objective of this study was to prepare and evaluate metformin nanoparticles (MN) using stearic acid-coupled F127 (SAF127) copolymer and polyvinyl alcohol by emulsion solvent evaporation technique.
Method: Metformin is the first-line drug for the treatment of type II diabetes mellitus belongs to Biopharmaceutical Classification System Class III. The prepared MN was characterized for particle size, polydispersity index (PDI), zeta potential, drug entrapment, percentage yield, in vitro drug release, and stability studies. The compatibility studies were performed by Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC). The crystallographic and surface properties were studied by X-ray diffractometry and scanning electron microscopy, respectively.
Results: The mean particle diameter of prepared nanoparticles ranged from 207.8 to 977.64 nm, PDI value ranged from 0.146 to 0.694, and zeta potential ranged from −20.5 to −6.97 mV. The drug entrapment efficiency of these nanoparticles varies between 18.81 to 69.01 %. The drug to SAF127 copolymer (10/30 w/w) ratio (MN3) showed optimum results. The MN3 had spherical morphology with semi-amorphous nature. The results of FTIR and DSC analysis showed that there was no significant interaction between drug and excipients. The prepared polymeric nanoparticles were stable at 5±3°C up to 3 months. In vitro release of drug from MN3 was 20.52% in the first 1 h and remaining drug was released up to 30 h.
Conclusion: The results of this study confirmed the sustained drug release profile of metformin loaded SAF127 copolymer nanoparticles. These nanoparticles can be best stored up to 3 months.
Downloads
References
Mishra MK, Ray D, Barik BB. Microcapsules and transdermal patch: A comparative approach for improved delivery of antidiabetic drug. AAPS Pharm Sci Tech 2009;10: 928-34.
Barwal I, Sood A, Sharma M, Singh B, Yadav SC. Development of stevioside Pluronic F-68 copolymer based PLA-nanoparticles as an antidiabetic nanomedicine. Colloids Surfaces B Biointerfaces 2013;101:510-16.
El-Gendy N, Hosny A, Abdelbary A. Microencapsulation approach for orally extended delivery of glipizide: In vitro and in vivo evaluation. Indian J Pharm Sci 2012;74:319-30.
Sankhyan A, Pawar PK. Metformin loaded non-ionic surfactant vesicles: optimization of formulation, effect of process variables and characterization. DARU J Pharm Sci 2013;21: 7.
Kai S, Huang L, Zhao Y, Guo S. Polymeric metformin and its use as a therapeutic agent and as a delivery vehicle. WO 2016144766 A1.
Rani R, Dahiya S, Dhingra D, Dilbaghi N, Kim KH, Kumar S. Evaluation of anti-diabetic activity of glycyrrhizin-loaded nanoparticles in nicotinamide-streptozotocin-induced diabetic rats. Eur J Pharm Sci 2017;06:220-30.
Mohamed MN, Khaleid MA, Mohamed S. Formulation and evaluation of extended release metformin hydrochloride beads. Int. J Pharm Pharm Sci 2014;6:433-41.
Monther FM, Inam SA, Najwan KJ. Design, synthesis and preliminary pharmacological evaluation of new metformin derivatives. Int J Pharm Pharm Sci 2017;9:279-93.
Corti G, Capasso G, Maestrelli F, Cirri M, Mura P. Physical-chemical characterization of binary systems of metformin hydrochloride with triacetyl-β-cyclodextrin. J Pharm Biomed Anal 2007;45:480-86.
Verma P, Kamboj V. Synthesis and antidiabetic activity of N’-[3-(alkyl/ aryl substituted)-4-oxo-1,3-thiazolidin-2-yleidene]-2-(pyrazin-2- yloxy)acetohydrazide. Acta Pharma Sci 2010;52:411-15.
Javidfar S, Pilehvar-Soltanahmadi Y, Farajzadeh R, Lotfi-Attari J, Shafiei-Irannejad V, Hashemi M, et al. The inhibitory effects of nano-encapsulated metformin on growth and hTERT expression in breast cancer cells. J Drug Deliv Sci Technol 2017;43:19-26.
Kamboj VK, Verma PK. Poloxamers based nanocarriers for drug delivery system. Der Pharma Lett 2015;7:264-69.
Elbahwy IA, Ibrahim HM, Ismael HR, Kasem AA. Enhancing bioavailability and controlling the release of glibenclamide from optimized solid lipid nanoparticles. J Drug Deliv Sci Technol 2017;38:78-89.
Lu Y, Park K. Polymeric micelles and alternative nanosized delivery vehicles for poorly soluble drugs. Int J Pharm 2013;453:198-14.
Gao Q, Liang Q, Yu F, Xu J, Zhao Q, Sun B. Synthesis and characterization of novel amphiphilic copolymer stearic acid-coupled F127 nanoparticles for nano-technology based drug delivery system. Colloids Surfaces B Biointerfaces 2011;88:741-48.
Shariatinia Z, Zahraee Z. Controlled release of metformin from chitosan-based nanocomposite films containing mesoporous MCM-41 nanoparticles as novel drug delivery systems. J Colloid Interface Sci 2017;501:60-76.
Kumar S, Bhanjana G, Verma RK, Dhingra D, Dilbaghi N, Kim KH. Metformin-loaded alginate nanoparticles as an effective anti-diabetic agent for controlled drug release. J Pharm Pharmacol 2017;69:143-50.
Lokhande AB, Mishra S, Kulkarni RD, Naik JB. Influence of different viscosity grade ethylcellulose polymers on encapsulation and in vitro release study of drug-loaded nanoparticles. J Pharm Res 2013;7:414-20.
Prakash C, Kamboj VK, Ahlawat, P, Kumar V. Structural and molecular alterations in arsenic-induced hepatic oxidative stress in rats: A FTIR study. Toxicol Environ Chem 2015;97:1408-21.
Snima KS, Jayakumar R, Lakshmanan VK. In vitro and in vivo biological evaluation of O-carboxymethyl chitosan encapsulated metformin nanoparticles for pancreatic cancer therapy. Pharm Res 2014;31:3361-70.
Hu LD, Liu Y, Tang X, Zhang Q. Preparation and in vitro/in vivo evaluation of sustained-release metformin hydrochloride pellets. Eur J Pharm Biopharm 2006;64:185-92.
Patil P, Bhoskar M. Optimization and evaluation of spray dried chitosan nanoparticles containing doxorubicin. Int J Curr Pharm Res 2014;6:7-15.
Birnbaum DT, Kosmala JD, Brannon-Peppas L. Optimization of preparation techniques for poly(lactic acid-co-glycolic acid) nanoparticles. J Nano Res 2000:2:173-81.
Jain S Saraf S. Influence of processing variables and in vitro characterization of glipizide loaded biodegradable nanoparticles. Diabetes Metab Syndr Clin Res Rev 2009;3: 113-17.
Kusum VD, Bhosale UV. Formulation and optimization of polymeric nano drug delivery system of acyclovir using 32 full factorial design. Int J Pharm Tech Res 2009;1:644-53.
Mokale V, Rajput R, Patil J, Yadava S, Naik J. Formulation of metformin hydrochloride nanoparticles by using spray drying technique and in vitro evaluation of sustained release with 32-level factorial design approach. Dry Technol 2016;34:1455-61.
Domingos RF, Baalousha MA, Ju-Nam Y, Reid MM, Tufenkji N, Lead JR, et al. Characterizing manufactured nanoparticles in the environment: Multimethod determination of particle sizes. Environ Sci Technol 2009;43:7277-84.
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.