Abstract
The objective of the present work was to produce gastroresistant Eudragit® RS100 nanoparticles by a reproducible synthesis approach that ensured mono-disperse nanoparticles under the size of 100 nm. Batch and micromixing nanoprecipitation approaches were selected to produce the demanded nanoparticles, identifying the critical parameters affecting the synthesis process. To shed some light on the formulation of the targeted nanoparticles, the effects of particle size and homogeneity of fluid dynamics, and physicochemical parameters such as polymer concentration, type of solvent, ratio of solvent to antisolvent, and total flow rate were studied. The physicochemical characteristics of resulting nanoparticles were studied applying dynamic light scattering (DLS) particle size analysis and electron microscopy imaging. Nanoparticles produced using a micromixer demonstrated a narrower and more homogenous distribution than the ones obtained under similar conditions in conventional batch reactors. Besides, fluid dynamics ensured that the best mixing conditions were achieved at the highest flow rate. It was concluded that nucleation and growth events must also be considered to avoid uncontrolled nanoparticle growth and evolution at the collection vial. Further, rifampicin-encapsulated nanoparticles were prepared using both approaches, demonstrating that the micromixing-assisted approach provided an excellent control of the particle size and polydispersity index. Not only the micromixing-assisted nanoprecipitation promoted a remarkable control in the nanoparticle formulation, but also it enhanced drug encapsulation efficiency and loading, as well as productivity. To the best of our knowledge, this was the very first time that drug-loaded Eudragit® RS100 nanoparticles (NPs) were produced in a continuous fashion under 100 nm (16.5 ± 4.3 nm) using microreactor technology. Furthermore, we performed a detailed analysis of the influence of various fluid dynamics and physicochemical parameters on the size and uniformity of the resulting nanoparticles. According to these findings, the proposed methodology can be a useful approach to synthesize a myriad of nanoparticles of alternative polymers.
Highlights
In recent years, the synthesis of polymeric nanoparticles (NPs) has gained wide recognition in biomedical applications [1,2,3], playing a pivotal role in a wide variety of pharmaceutical applications such as diagnostics and drug delivery [4]
In the present work we propose micromixer-assisted nanoprecipitation to study the effect of fluid dynamics and physicochemical parameters on the synthesis of polymer nanoparticles of
Considering that the main aim of this work was to identify the key parameters governing the nanoprecipitation of Eudragit® RS100 polymer and to propose a continuous flow approach to circumvent current limitations of batch production, this section is divided into four distinct parts: (1) Selection of class 3 solvents, (2) Analysis of the results obtained by the conventional batch method, (3) Analysis of the results obtained by the micromixer-assisted nanoprecipitation and synthesis optimization, and (4) Study of rifampicin loading and entrapment efficiency by batch and micromixing-assisted approaches
Summary
The synthesis of polymeric nanoparticles (NPs) has gained wide recognition in biomedical applications [1,2,3], playing a pivotal role in a wide variety of pharmaceutical applications such as diagnostics and drug delivery [4]. These NPs are designed to transport and deliver active. The design of polymeric NPs for a therapeutic use should consider the payload required, the targeted site of action, and the route of administration In this sense, the polymer properties can substantially differ if an intravenous or an oral administration were considered
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
