Buserelin acetate microparticle dispersion effects drug release and plasma E(1) levels

Area of Science:

• Pharmacology
• Drug Delivery Systems
• Materials Science

Background:

• Buserelin acetate (BA) is administered via sustained-release microparticle injections.
• Optimizing microparticle dispersion is crucial for controlling drug release and efficacy.

Purpose of the Study:

• To investigate how different dispersion methods affect the release kinetics of buserelin acetate (BA) from microparticles.
• To evaluate the impact of dispersion methods on the onset of drug efficacy, specifically plasma estrone concentrations.

Main Methods:

• In vitro release studies were conducted using various dispersion methods: standard dispersion method (SDM), vibration dispersion method (VDM), and ultrasonication.
• BA release rates and microparticle characteristics (shape, size distribution) were analyzed.
• In vivo studies involved administering BA microparticles to Sprague-Dawley rats to measure plasma estrone (E(1)) levels.

Main Results:

• Increased stirring speed during dispersion enhanced initial BA release (p<0.01).
• The VDM resulted in a higher initial BA release rate compared to SDM (p<0.01).
• Microparticle shape and size distribution remained unchanged across all tested dispersion methods.
• VDM led to lower initial plasma estrone concentrations in rats compared to SDM (p<0.05).

Conclusions:

• Dispersion methods significantly influence BA release rates and the subsequent pharmacokinetic profile.
• While microparticle morphology is unaffected, dispersion techniques critically alter drug release dynamics and can impact therapeutic efficacy.
• Optimizing dispersion methods is essential for predictable buserelin acetate delivery and therapeutic outcomes.