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Formulation composition, manufacturing process, and characterization of poly(lactide-co-glycolide) microparticles
Kinam Park1, Andrew Otte2, Farrokh Sharifi2
1Purdue University, Biomedical Engineering and Pharmaceutics, 206 S. Martin Jischke Drive, West Lafayette, IN 47907, USA; Akina, Inc., 3495 Kent Avenue, Suite A200, West Lafayette, IN 47906, USA.
Summary
Injectable long-acting poly(lactide-co-glycolide) (PLGA) formulations face slow development due to complex manufacturing. Understanding formulation and process parameters, especially surface morphology, is key to controlling drug release and improving clinical products.
Area of Science:
- Polymer science and drug delivery systems.
- Biomaterials and pharmaceutical technology.
Background:
- Injectable long-acting formulations using poly(lactide-co-glycolide) (PLGA) offer sustained drug delivery for up to six months.
- Despite benefits, the clinical and generic development of PLGA-based drug products has been limited, with few FDA-approved formulations and even fewer small molecule drugs incorporated.
- This slow progress stems from an incomplete understanding of PLGA polymers and the complex interplay of formulation composition and manufacturing variables.
Purpose of the Study:
- To review the critical factors influencing the properties of PLGA microparticle formulations.
- To elucidate the relationship between formulation composition, manufacturing processes, and in vivo drug release kinetics.
- To emphasize the importance of microparticle surface morphology as an indicator of formulation and process control and its impact on drug release.
Main Methods:
- Review of existing literature on poly(lactide-co-glycolide) (PLGA) based injectable long-acting formulations.
- Analysis of formulation composition and manufacturing parameters affecting microparticle properties.
- Focus on in vitro characterization techniques, particularly surface morphology analysis of PLGA microparticles.
- Examination of the correlation between in vitro characteristics and in vivo pharmacokinetic profiles.
Main Results:
- Numerous process parameters significantly impact PLGA formulation properties, with intricate interactions making them difficult to control independently.
- Formulation composition and manufacturing processes directly dictate in vivo drug release kinetics and pharmacokinetic profiles.
- Surface morphology of PLGA microparticles serves as a critical indicator of formulation and manufacturing, directly influencing drug release patterns.
Conclusions:
- A comprehensive understanding of PLGA polymer behavior and the variables in formulation and manufacturing is essential for advancing long-acting injectable drug products.
- Effective in vitro characterization, especially surface morphology analysis, is crucial for quality control, scale-up, and predicting in vivo performance.
- The principles discussed for microparticle systems are also applicable to other long-acting delivery systems like in situ forming and solid implants.
