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Fabrication of PEG-PLGA Microparticles with Tunable Sizes for Controlled Drug Release Application

Polymeric microparticles of polyethyleneglycol-polylactic acid-co-glycolic acid (PEG-PLGA) are widely used as drug carriers for a variety of applications due to their unique characteristics. Although existing techniques for producing polymeric drug carriers offer the possibility of achieving greater...

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Autores principales: Sagoe, Paul Nana Kwame, Velázquez, Eduardo José Machado, Espiritusanto, Yohely Maria, Gilbert, Amelia, Orado, Thalma, Wang, Qiu, Jain, Era
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10534673/
https://www.ncbi.nlm.nih.gov/pubmed/37764454
http://dx.doi.org/10.3390/molecules28186679
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author Sagoe, Paul Nana Kwame
Velázquez, Eduardo José Machado
Espiritusanto, Yohely Maria
Gilbert, Amelia
Orado, Thalma
Wang, Qiu
Jain, Era
author_facet Sagoe, Paul Nana Kwame
Velázquez, Eduardo José Machado
Espiritusanto, Yohely Maria
Gilbert, Amelia
Orado, Thalma
Wang, Qiu
Jain, Era
author_sort Sagoe, Paul Nana Kwame
collection PubMed
description Polymeric microparticles of polyethyleneglycol-polylactic acid-co-glycolic acid (PEG-PLGA) are widely used as drug carriers for a variety of applications due to their unique characteristics. Although existing techniques for producing polymeric drug carriers offer the possibility of achieving greater production yield across a wide range of sizes, these methods are improbable to precisely tune particle size while upholding uniformity of particle size and morphology, ensuring consistent production yield, maintaining batch-to-batch reproducibility, and improving drug loading capacity. Herein, we developed a novel scalable method for the synthesis of tunable-sized microparticles with improved monodispersity and batch-to-batch reproducibility via the coaxial flow-phase separation technique. The study evaluated the effect of various process parameters on microparticle size and polydispersity, including polymer concentration, stirring rate, surfactant concentration, and the organic/aqueous phase flow rate and volume ratio. The results demonstrated that stirring rate and polymer concentration had the most significant impact on the mean particle size and distribution, whereas surfactant concentration had the most substantial impact on the morphology of particles. In addition to synthesizing microparticles of spherical morphology yielding particle sizes in the range of 5–50 µm across different formulations, we were able to also synthesize several microparticles exhibiting different morphologies and particle concentrations as a demonstration of the tunability and scalability of this method. Notably, by adjusting key determining process parameters, it was possible to achieve microparticle sizes in a comparable range (5–7 µm) for different formulations despite varying the concentration of polymer and volume of polymer solution in the organic phase by an order of magnitude. Finally, by the incorporation of fluorescent dyes as model hydrophilic and hydrophobic drugs, we further demonstrated how polymer amount influences drug loading capacity, encapsulation efficiency, and release kinetics of these microparticles of comparable sizes. Our study provides a framework for fabricating both hydrophobic and hydrophilic drug-loaded microparticles and elucidates the interplay between fabrication parameters and the physicochemical properties of microparticles, thereby offering an itinerary for expanding the applicability of this method for producing polymeric microparticles with desirable characteristics for specific drug delivery applications.
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spelling pubmed-105346732023-09-29 Fabrication of PEG-PLGA Microparticles with Tunable Sizes for Controlled Drug Release Application Sagoe, Paul Nana Kwame Velázquez, Eduardo José Machado Espiritusanto, Yohely Maria Gilbert, Amelia Orado, Thalma Wang, Qiu Jain, Era Molecules Article Polymeric microparticles of polyethyleneglycol-polylactic acid-co-glycolic acid (PEG-PLGA) are widely used as drug carriers for a variety of applications due to their unique characteristics. Although existing techniques for producing polymeric drug carriers offer the possibility of achieving greater production yield across a wide range of sizes, these methods are improbable to precisely tune particle size while upholding uniformity of particle size and morphology, ensuring consistent production yield, maintaining batch-to-batch reproducibility, and improving drug loading capacity. Herein, we developed a novel scalable method for the synthesis of tunable-sized microparticles with improved monodispersity and batch-to-batch reproducibility via the coaxial flow-phase separation technique. The study evaluated the effect of various process parameters on microparticle size and polydispersity, including polymer concentration, stirring rate, surfactant concentration, and the organic/aqueous phase flow rate and volume ratio. The results demonstrated that stirring rate and polymer concentration had the most significant impact on the mean particle size and distribution, whereas surfactant concentration had the most substantial impact on the morphology of particles. In addition to synthesizing microparticles of spherical morphology yielding particle sizes in the range of 5–50 µm across different formulations, we were able to also synthesize several microparticles exhibiting different morphologies and particle concentrations as a demonstration of the tunability and scalability of this method. Notably, by adjusting key determining process parameters, it was possible to achieve microparticle sizes in a comparable range (5–7 µm) for different formulations despite varying the concentration of polymer and volume of polymer solution in the organic phase by an order of magnitude. Finally, by the incorporation of fluorescent dyes as model hydrophilic and hydrophobic drugs, we further demonstrated how polymer amount influences drug loading capacity, encapsulation efficiency, and release kinetics of these microparticles of comparable sizes. Our study provides a framework for fabricating both hydrophobic and hydrophilic drug-loaded microparticles and elucidates the interplay between fabrication parameters and the physicochemical properties of microparticles, thereby offering an itinerary for expanding the applicability of this method for producing polymeric microparticles with desirable characteristics for specific drug delivery applications. MDPI 2023-09-18 /pmc/articles/PMC10534673/ /pubmed/37764454 http://dx.doi.org/10.3390/molecules28186679 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Sagoe, Paul Nana Kwame
Velázquez, Eduardo José Machado
Espiritusanto, Yohely Maria
Gilbert, Amelia
Orado, Thalma
Wang, Qiu
Jain, Era
Fabrication of PEG-PLGA Microparticles with Tunable Sizes for Controlled Drug Release Application
title Fabrication of PEG-PLGA Microparticles with Tunable Sizes for Controlled Drug Release Application
title_full Fabrication of PEG-PLGA Microparticles with Tunable Sizes for Controlled Drug Release Application
title_fullStr Fabrication of PEG-PLGA Microparticles with Tunable Sizes for Controlled Drug Release Application
title_full_unstemmed Fabrication of PEG-PLGA Microparticles with Tunable Sizes for Controlled Drug Release Application
title_short Fabrication of PEG-PLGA Microparticles with Tunable Sizes for Controlled Drug Release Application
title_sort fabrication of peg-plga microparticles with tunable sizes for controlled drug release application
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10534673/
https://www.ncbi.nlm.nih.gov/pubmed/37764454
http://dx.doi.org/10.3390/molecules28186679
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