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PLGA Nanoparticles Formed by Single- or Double-emulsion with Vitamin E-TPGS
Published on: December 27, 2013
A novel and simple preparative method for uniform-sized PLGA microspheres: Preliminary application in antitubercular
Zhiqiang Liu1, Xia Li2, Bingshui Xiu1
1Department of Bio-diagnosis, Beijing Institute of Basic Medical Sciences, 27 Taiping Road, Haidian District, Beijing 100850, China.
Abstract:
Particle size has been demonstrated as a key parameter influencing the phagocytosis of drug-loaded PLGA microspheres (MS) by the target cells. However, the current preparative methods were either insufficient in controlling the homogeneity of the produced MS, or requires sophisticated and costly equipment. This study aimed to explore a simple and economical method for uniform PLGA MS preparation. Based on the heterogeneous emulsification of routine mechanical stirring, we designed an adjuvant strategy to enhance the homogeneity of MS. By using glass beads as adjutant, the dispersion produced during mechanical stirring was much more homogeneous in the solution. The particles produced were much smaller and the size distribution was much narrower as compared with those produced using the routine mechanical stirring method under the same condition. After enrichment by selective centrifugation, about 60% of the particles of similar size were obtained, providing further evidence for the efficiency of the novel method in controlling particle homogeneity. Further, the method was applied to prepare rifampicin-loaded PLGA MS of the optimized size for macrophage uptake. The functional evaluation showed that the prepared PLGA MS could efficiently deliver an antitubercular drug into macrophages and maintain a higher intracellular concentration by controlled release, suggesting the potential application of the method in PLGA MS-based drug delivery. Collectively, the study provided a simple and economical method for preparing uniform-sized PLGA MS with potential of widespread applications.
Insights
This study presents a simple, economical method using glass beads to create uniform poly(lactic-co-glycolic acid) (PLGA) microspheres (MS). This technique improves drug delivery into macrophages for tuberculosis treatment.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Nanotechnology
Background:
- Particle size critically impacts phagocytosis of poly(lactic-co-glycolic acid) microspheres (MS).
- Existing methods for MS preparation often lack homogeneity control or require expensive equipment.
- Uniform MS are crucial for predictable drug delivery and cellular uptake.
Purpose of the Study:
- To develop a simple, economical, and effective method for preparing uniform poly(lactic-co-glycolic acid) microspheres (MS).
- To enhance the homogeneity and control particle size distribution of MS.
- To evaluate the efficacy of the prepared MS for drug delivery into macrophages.
Main Methods:
- An adjuvant strategy using glass beads was integrated with routine mechanical stirring for heterogeneous emulsification.
- Selective centrifugation was employed to enrich particles of similar size.
- Rifampicin-loaded PLGA MS were prepared using the optimized method and tested for macrophage uptake.
Main Results:
- The addition of glass beads significantly improved dispersion homogeneity, resulting in smaller particle sizes and narrower size distribution.
- Selective centrifugation yielded approximately 60% of similarly sized particles, confirming method efficiency.
- Rifampicin-loaded PLGA MS demonstrated efficient intracellular delivery and controlled release within macrophages.
Conclusions:
- The novel method offers a simple, economical approach to produce uniform-sized PLGA MS.
- This technique enhances control over MS homogeneity, crucial for drug delivery applications.
- The prepared MS show potential for effective antitubercular drug delivery into macrophages.

