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Formulating erythropoietin-loaded sustained-release PLGA microspheres without protein aggregation
1Shanghai Jiao Tong University, School of Pharmacy, No 800 Dong Chuan Road, Shanghai 200240, China.
Summary
We developed a novel method to encapsulate erythropoietin (EPO) into poly(lactic-co-glycolic acid) (PLGA) microspheres, enhancing its stability and enabling sustained release. This formulation significantly boosts red blood cell production with fewer injections and reduced immunogenicity.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Protein Formulation
Background:
- Erythropoietin (EPO) is a protein hormone crucial for red blood cell production, but it is prone to denaturation and aggregation when exposed to water-organic solvent interfaces.
- Conventional EPO formulations require frequent injections, limiting patient compliance and therapeutic efficacy.
- Developing stable, long-acting EPO formulations is essential for effective anemia treatment.
Purpose of the Study:
- To develop a simple and efficient method for microencapsulating erythropoietin (EPO) into poly(lactic-co-glycolic acid) (PLGA) microspheres.
- To enhance EPO stability against denaturation and aggregation during formulation.
- To achieve sustained release of EPO and evaluate its in vivo efficacy and immunogenicity.
Main Methods:
- An aqueous-aqueous emulsion technique was employed at reduced temperatures, utilizing dextran and polyethylene glycol (PEG) to protect EPO.
- The formulation involved freezing, lyophilization, and washing with dichloromethane to remove the continuous phase.
- EPO was encapsulated into 1-4 micrometer PLGA microspheres, conferring resistance to organic solvents.
Main Results:
- Microencapsulation resulted in minimal EPO aggregation (<2%) and enhanced resistance to organic solvents.
- EPO-loaded PLGA microspheres exhibited sustained-release kinetics with minimal burst release (<20%) and incomplete overall release (<20%).
- A single injection of EPO-PLGA microspheres in mice led to a red blood cell elevation comparable to twelve injections of solution formulation, with no significant increase in anti-EPO IgG levels.
Conclusions:
- The developed aqueous-aqueous emulsion method provides a simple and effective approach for stable EPO microencapsulation in PLGA.
- The EPO-loaded PLGA microspheres offer a promising sustained-release drug delivery system with improved therapeutic outcomes and reduced immunogenicity.
- This formulation represents a significant advancement for anemia management, potentially improving patient compliance and treatment efficacy.
