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Fabricating Highly Open Porous Microspheres (HOPMs) via Microfluidic Technology

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A one-step modified method to reduce the burst initial release from PLGA microspheres.

Caihong Zheng¹, Wenquan Liang

¹Women's Hospital Affiliated College of Medical Sciences, Zhejiang University, Hangzhou 310006, PR China. chzheng@zju.edu.cn

|January 14, 2010

Summary

This study modified poly(lactic-co-glycolic acid) (PLGA) microspheres using alginate, calcium chloride, and chitosan. The modified PLGA microspheres significantly reduced initial protein burst release and closed surface pores.

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Area of Science:

Biomaterials Science
Drug Delivery Systems
Polymer Chemistry

Background:

Poly(lactic-co-glycolic acid) (PLGA) microspheres are widely used for controlled protein delivery.
A significant challenge is the initial burst release of entrapped proteins, which can lead to adverse effects.
Developing strategies to mitigate this burst release is crucial for improving therapeutic efficacy.

Purpose of the Study:

To evaluate a one-step modified method for entrapping bovine serum albumin (BSA) into PLGA microspheres.
To reduce the initial burst release of BSA from PLGA microspheres.
To assess the impact of the modification on entrapment efficiency and particle size.

Main Methods:

A modified one-step method was employed involving the addition of alginate to the internal aqueous phase with BSA.
Calcium chloride and chitosan were incorporated into the external phase.
Standard procedures were maintained for other process parameters.

Main Results:

The modified PLGA microspheres exhibited a marked inhibition of initial protein release.
A slight increase in entrapment efficiency was observed.
Particle size remained unchanged after the modification.
Scanning electron microscopy (SEM) revealed the closure of surface pores on the modified microspheres.

Conclusions:

The one-step modification effectively reduces the initial burst release of proteins from PLGA microspheres.
This method offers a promising approach for enhancing protein delivery systems by improving drug loading and controlling release kinetics.
The observed pore closure suggests a mechanism for improved drug retention within the microspheres.