A novel and simple preparative method for uniform-sized PLGA microspheres: Preliminary application in antitubercular drug delivery.
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.
Department of Bio-diagnosis, Beijing Institute of Basic Medical Sciences, 27 Taiping Road, Haidian District, Beijing 100850, China.
Zhiqiang
Z
Liu
Affiliated Hospital of Academy of Military Medical Sciences, Beijing, China.
Xia
X
Li
Department of Bio-diagnosis, Beijing Institute of Basic Medical Sciences, 27 Taiping Road, Haidian District, Beijing 100850, China.
Bingshui
B
Xiu
Department of Bio-diagnosis, Beijing Institute of Basic Medical Sciences, 27 Taiping Road, Haidian District, Beijing 100850, China.
Cuimi
C
Duan
Medical University of Anhui, Heifei 230000, Anhui Province, China.
Jiangxue
J
Li
Department of Bio-diagnosis, Beijing Institute of Basic Medical Sciences, 27 Taiping Road, Haidian District, Beijing 100850, China.
Xuhui
X
Zhang
Department of Bio-diagnosis, Beijing Institute of Basic Medical Sciences, 27 Taiping Road, Haidian District, Beijing 100850, China.
Xiqin
X
Yang
Research Center for Bioengineering and Sensing Technology, University of Science & Technology Beijing, Beijing 100083, PR China.
Wenhao
W
Dai
Olympia Diagnostics, Inc., Sunnyvale, CA 94086, USA.
Heather
H
Johnson
Department of Bio-diagnosis, Beijing Institute of Basic Medical Sciences, 27 Taiping Road, Haidian District, Beijing 100850, China. Electronic address: zhangheqiu2004@126.com.
Heqiu
H
Zhang
Department of Bio-diagnosis, Beijing Institute of Basic Medical Sciences, 27 Taiping Road, Haidian District, Beijing 100850, China. Electronic address: xyfeng2002@126.com.
Xiaoyan
X
Feng
D000818:Animals; D000995:Antitubercular Agents / Q000494:pharmacology*; D002498:Centrifugation; D016503:Drug Delivery Systems / Q000379:methods*; D042541:Intracellular Space / Q000378:metabolism; D019344:Lactic Acid / Q000737:chemistry*; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008863:Microspheres; D010316:Particle Size; D010587:Phagocytosis / Q000187:drug effects; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D000067996:RAW 264.7 Cells; D012293:Rifampin / Q000494:pharmacology
D000995:Antitubercular Agents; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D012293:Rifampin
Drug delivery; Macrophages; PLGA microspheres; Tuberculosis