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Multi-Scale Modification of Metallic Implants With Pore Gradients, Polyelectrolytes and Their Indirect Monitoring In vivo
Published on: July 1, 2013
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In-situ forming PLGA implants: Towards less toxic solvents.
F Ramos1, J-F Willart2, C Neut3
1Univ. Lille, Inserm, CHU Lille, U1008, F-59000 Lille, France; Univ. Lille, CNRS, INRAE, Centrale Lille, UMR 8207 UMET, F-59000 Lille, France.
International Journal of Pharmaceutics
|April 15, 2024
Summary
This study explored safer solvents for in-situ forming poly(lactic-co-glycolic acid) (PLGA) implants used in drug delivery. New PEG 400, TEC, and ethanol blends successfully formed implants, controlling drug release and maintaining antimicrobial activity.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Polymer Chemistry
Background:
- In-situ forming implants using poly(lactic-co-glycolic acid) (PLGA) are promising for controlled drug delivery.
- N-methyl-2-pyrrolidine (NMP), a common solvent, presents toxicity concerns for parenteral administration.
- Developing safer solvent systems is crucial for advancing PLGA implant technology.
Purpose of the Study:
- To identify less toxic alternative solvent systems for in-situ forming PLGA implants.
- To evaluate the performance of PLGA implants formulated with novel solvent blends.
- To investigate the release kinetics and antimicrobial efficacy of drugs delivered via these implants.
Main Methods:
- PLGA, ibuprofen, and chlorhexidine dihydrochloride were formulated using various polyethylene glycol 400 (PEG 400), triethyl citrate (TEC), and ethanol blends.
- Implant formation, syringeability, drug release kinetics, antimicrobial activity, wet mass, and pH changes were monitored.
- Release studies were conducted in phosphate buffer at pH 6.8 and 37°C.
Main Results:
- Specific PEG 400:TEC:ethanol blends (85:10:5 and 60:30:10) demonstrated good syringeability and rapid implant formation.
- These formulations controlled the release of ibuprofen and chlorhexidine over several weeks, showing significant antimicrobial activity.
- Distinct drug release mechanisms were observed: ibuprofen exhibited burst release, while chlorhexidine showed an initial lag phase.
Conclusions:
- Polyethylene glycol 400, triethyl citrate, and ethanol offer a less toxic alternative solvent system for in-situ forming PLGA implants.
- The developed formulations provide effective, sustained drug delivery with antimicrobial properties.
- Understanding drug-specific release mechanisms is key for optimizing PLGA-based drug delivery systems.

