Development of uniform fenofibrate-loaded biodegradable microparticle by membrane emulsification
Copyright © 2023 Elsevier B.V. All rights reserved..
Fenofibrate has shown therapeutic effects on diabetic retinopathy. However, fenofibrate can be rapidly cleared from the eye after a single intravitreal injection. Here, we aim to develop fenofibrate loaded PLGA microparticles (Feno-MP) with high drug loading and sustained in vitro release up to 6 months suitable for intravitreal injection. First, orthogonal array experimental design was applied for formulation optimization. The selected formulation parameters were used to formulate Feno-MP using homogenization method and direct membrane emulsification method. Both methods generated Feno-MP with high drug loading and sustained in vitro drug release more than 140 days. Unlike the polydisperse Feno-MP prepared using homogenization method, membrane emulsification method generated Feno-MP with uniform size distribution. By controlling the membrane pore size, 1.5 µm, 8 µm and 16 µm Feno-MP were formulated and we found that larger Feno-MP demonstrated higher drug loading, more sustained drug release in vitro with less burst drug release than the smaller Feno-MP. In conclusion, we developed Feno-MP with high drug loading and sustained release profile, and elucidated that changing the particle size could have notable impacts on drug loading and release kinetics. Formulating Feno-MP with uniform size distribution by membrane emulsification method would benefit the batch-to-batch repeatability.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:650 |
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| Enthalten in: |
International journal of pharmaceutics - 650(2024) vom: 25. Jan., Seite 123675 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Meng, Tuo [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 08.01.2024 Date Revised 07.02.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ijpharm.2023.123675 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Copyright © 2023 Elsevier B.V. All rights reserved. | ||
| 520 | |a Fenofibrate has shown therapeutic effects on diabetic retinopathy. However, fenofibrate can be rapidly cleared from the eye after a single intravitreal injection. Here, we aim to develop fenofibrate loaded PLGA microparticles (Feno-MP) with high drug loading and sustained in vitro release up to 6 months suitable for intravitreal injection. First, orthogonal array experimental design was applied for formulation optimization. The selected formulation parameters were used to formulate Feno-MP using homogenization method and direct membrane emulsification method. Both methods generated Feno-MP with high drug loading and sustained in vitro drug release more than 140 days. Unlike the polydisperse Feno-MP prepared using homogenization method, membrane emulsification method generated Feno-MP with uniform size distribution. By controlling the membrane pore size, 1.5 µm, 8 µm and 16 µm Feno-MP were formulated and we found that larger Feno-MP demonstrated higher drug loading, more sustained drug release in vitro with less burst drug release than the smaller Feno-MP. In conclusion, we developed Feno-MP with high drug loading and sustained release profile, and elucidated that changing the particle size could have notable impacts on drug loading and release kinetics. Formulating Feno-MP with uniform size distribution by membrane emulsification method would benefit the batch-to-batch repeatability | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Fenofibrate | |
| 650 | 4 | |a Homogenization | |
| 650 | 4 | |a Intravitreal drug delivery | |
| 650 | 4 | |a Membrane emulsification | |
| 650 | 4 | |a Orthogonal array design | |
| 650 | 4 | |a PLGA microparticle | |
| 650 | 7 | |a Fenofibrate |2 NLM | |
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| 650 | 7 | |a Polylactic Acid-Polyglycolic Acid Copolymer |2 NLM | |
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| 650 | 7 | |a Delayed-Action Preparations |2 NLM | |
| 700 | 1 | |a Sudarjat, Hadi |e verfasserin |4 aut | |
| 700 | 1 | |a Momin, Mohammad |e verfasserin |4 aut | |
| 700 | 1 | |a Ma, Jian-Xing |e verfasserin |4 aut | |
| 700 | 1 | |a Xu, Qingguo |e verfasserin |4 aut | |
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