Poly(D,L-lactide-co-glycolide) microspheres containing 5-fluorouracil: optimization of process parameters

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Poly(D,L-lactide-co-glycolide) (PLGA) microspheres are widely used for controlled drug delivery.
• Optimizing PLGA microsphere production is crucial for achieving desired drug release profiles and therapeutic efficacy.
• 5-fluorouracil (5-FU) is a chemotherapeutic agent often formulated into injectable dosage forms.

Purpose of the Study:

• To optimize processing parameters for poly(D,L-lactide-co-glycolide) (PLGA) microspheres loaded with 5-fluorouracil (5-FU).
• To establish mathematical relationships between process parameters and microsphere properties.
• To investigate the impact of emulsion phase volumes on microsphere characteristics.

Main Methods:

• Microspheres were fabricated using a water-in-oil-in-water emulsion solvent evaporation technique.
• A 3(2) factorial design was implemented to systematically vary internal and external emulsion phase volumes.
• Particle size, yield, and encapsulation efficiency were quantified. Scanning electron microscopy (SEM) was used for morphological analysis.

Main Results:

• Increased internal phase volume led to decreased yield and encapsulation efficiency, but increased particle size.
• Increased external phase volume resulted in reduced yield, particle size, and encapsulation efficiency.
• The study demonstrated good batch-to-batch reproducibility of the microspheres.
• SEM revealed that the prepared microspheres existed as aggregates.

Conclusions:

• Processing parameters, specifically internal and external emulsion phase volumes, significantly impact PLGA microsphere characteristics for 5-FU delivery.
• The established relationships provide a basis for optimizing the formulation of 5-FU loaded PLGA microspheres.
• The method allows for the reproducible production of aggregated microspheres, suitable for further investigation in drug delivery applications.