Utilization of Microfluidics for the Preparation of Polymeric Nanoparticles for the Antioxidant Rutin: A Comparison with Bulk Production

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. Method: 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.

Glass Transition Temperature of PLGA Particles and the Influence on Drug Delivery Applications

“…Microfluidic technology is a novel method to produce narrow size distribution PLGA particles with high drug encapsulation. A microfluidic chip is made up of micro size channels which ensures the mixing of inlet flows to be completed within milliseconds [ 33 ]. Electrospray jetting can also be utilized to prepare PLGA particles.…”

“…In order to achieve promised pharmacodynamics, biodistribution, and toxicity levels, the key physicochemical properties need to be appropriately studied. Particle size, size distribution, surface morphology, zeta potential, and loading efficiency are most commonly characterized because these parameters are the key factors that determine the drug release behaviors [ 32 , 33 ]. It has been proposed, however, that the glass transition temperature ( T g ) will also impact the drug release behavior of polymeric nanoparticles [ 34 , 35 , 36 ].…”

Microfluidics Technology for the Design and Formulation of Nanomedicines

“…Hanh T.H. Vu et al [164] have used PLGA to encapsulate rutin (citrus flavonoid) as a PNP using different methods. One of them is prepared using the bulk method (single emulsion evaporation method), and the other is by microfluidics.…”

Lactoferrin-Loaded PEG/PLA Block Copolymer Targeted With Anti-Transferrin Receptor Antibodies for Alzheimer Disease

“…The Lf-PPN was synthesized using nanoprecipitation methods by adding drug and polymer to the water. 54 Transmission electron microscopy analysis reveals the Lf-PPN displays well-organized spherical structure ( Figure 1A). The physicochemical property of the Lf-PPN was examined after synthesis of each step, which is represented in Table 1.…”