Abstract
Objective: To compare the characteristics of rutin-loaded PLGA (poly(lactic-coglycolic acid)) nanoparticles prepared using a single emulsion evaporation method (bulk method) and a nanoprecipitation method using microfluidics.
Methods: Rutin-loaded PLGA nanoparticles were produced using different methods and characterized for size, zeta potential, entrapment efficiency (EE) and drug loading (DL). A design of experiments approach was used to identify the effect of method parameters to optimize the formulation. DSC was used to investigate the solid-state characteristics of rutin and PLGA and identify any interactions in the rutin-loaded PLGA nanoparticles. The release of rutin from PLGA nanoparticles was examined in biorelevant media and phosphate buffer (PBS).
Results: The optimal formulation of rutin-loaded PLGA nanoparticles produced using a microfluidics method resulted in a higher entrapment efficiency of 34 ± 2% and a smaller size of 123 ± 4 nm compared to a bulk method (EE 27 ± 1%, size 179 ± 13 nm). The solidstate of rutin and PLGA changed from crystalline to amorphous with the preparation of rutin- loaded PLGA nanoparticles. More importantly, using microfluidics, rutin released faster from rutin-loaded PLGA nanoparticles in biorelevant media and PBS with higher burst release compared to the rutin release from the nanoparticles prepared by using the bulk method.
Conclusion: Rutin can be encapsulated in nanoparticles formulated with different methods with mean sizes of less than 200 nm. Microfluidics produced more uniform rutin-loaded PLGA nanoparticles with a higher EE, DL and faster release compared to a bulk production method.
Keywords: Antioxidant, design of experiments, microfluidics, PLGA nanoparticles, rutin, emulsion evaporation method.
Graphical Abstract
[http://dx.doi.org/10.1016/0891-5849(95)02227-9] [PMID: 8743980]
[http://dx.doi.org/10.1016/j.foodchem.2015.03.024] [PMID: 25863606]
[http://dx.doi.org/10.1016/S0955-2863(02)00208-5] [PMID: 12550068]
[http://dx.doi.org/10.1016/0006-2952(88)90169-4] [PMID: 2830882]
[http://dx.doi.org/10.1016/S0969-806X(98)00347-8]
[http://dx.doi.org/10.1021/jf9026124] [PMID: 19916501]
[http://dx.doi.org/10.1006/abbi.1996.0146] [PMID: 8638942]
[http://dx.doi.org/10.1016/j.neuint.2011.06.014] [PMID: 21740943]
[http://dx.doi.org/10.1139/apnm-2013-0091] [PMID: 24053516]
[http://dx.doi.org/10.1002/tox.20662] [PMID: 21254320]
[http://dx.doi.org/10.1039/c3fo30389f] [PMID: 23584161]
[http://dx.doi.org/10.1016/S0014-5793(97)00467-5] [PMID: 9199494]
[http://dx.doi.org/10.1081/PDT-100100556] [PMID: 10934740]
[http://dx.doi.org/10.1007/s002280000197] [PMID: 11151743]
[http://dx.doi.org/10.1517/13543784.2013.805744] [PMID: 23795677]
[http://dx.doi.org/10.3390/polym3031377] [PMID: 22577513]
[http://dx.doi.org/10.1016/j.ijpharm.2008.04.042] [PMID: 18621492]
[http://dx.doi.org/10.3390/nano6020026] [PMID: 28344283]
[http://dx.doi.org/10.1016/S0142-9612(00)00115-0] [PMID: 11055295]
[http://dx.doi.org/10.1016/j.ijpharm.2017.11.044] [PMID: 29175645]
[http://dx.doi.org/10.1016/j.ijpharm.2017.10.006] [PMID: 29017804]
[http://dx.doi.org/10.1039/b802562b] [PMID: 18584088]
[http://dx.doi.org/10.1016/j.jcis.2008.03.033] [PMID: 18402975]
[http://dx.doi.org/10.1016/j.aquatox.2017.11.017] [PMID: 29197232]
[http://dx.doi.org/10.1038/mtna.2012.28] [PMID: 23344179]
[http://dx.doi.org/10.1016/j.ijpharm.2014.10.030] [PMID: 25455778]
[http://dx.doi.org/10.1016/j.ijpharm.2018.06.042] [PMID: 29933062]
[http://dx.doi.org/10.1016/j.ijpharm.2007.08.034] [PMID: 17913411]
[PMID: 26528074]
[PMID: 22114486]
[http://dx.doi.org/10.1039/C5NR03543K] [PMID: 26415866]
[http://dx.doi.org/10.1007/s13204-018-0790-0]
[http://dx.doi.org/10.1016/j.colsurfa.2017.04.062]
[http://dx.doi.org/10.1002/btpr.67] [PMID: 19194932]
[http://dx.doi.org/10.1155/2014/162962] [PMID: 25574384]
[http://dx.doi.org/10.1016/S0378-5173(99)00412-3] [PMID: 10699709]
[http://dx.doi.org/10.1021/nl801736q] [PMID: 18656990]
[http://dx.doi.org/10.1039/C6LC01049K] [PMID: 27991629]
[http://dx.doi.org/10.2174/156720112800389070] [PMID: 22283645]
[http://dx.doi.org/10.1002/app.11109]
[http://dx.doi.org/10.1021/acs.oprd.7b00247]
[http://dx.doi.org/10.1007/s12645-012-0027-y] [PMID: 26069494]
[http://dx.doi.org/10.1002/app.41943]
[http://dx.doi.org/10.1039/C7RA04748G]
[http://dx.doi.org/10.1021/ja00090a032]
[http://dx.doi.org/10.1002/app.28122]