Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their PropertiesReportar como inadecuado




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1

State Key Laboratory of Respiratory Diseases, the First Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou 510230, China

2

Department of Pharmacology, College of Pharmacy, Third Military Medical University, Chongqing 400038, China

3

School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China

4

Department of Dematology, Daping Hospital, Third Military Medical University, Chongqing 400042, China





*

Author to whom correspondence should be addressed.



Abstract Emodin 1,3,8-trihydroxy-6-methylanthraquinone has been identified to have the potential to improve lung fibrosis and lung cancer. To avoid the liver and kidney toxicities and the fast metabolism of emodin, emodin-loaded polylactic acid microspheres ED-PLA-MS were prepared and their characteristics were studied. ED-PLA-MS were prepared by the organic phase dispersion-solvent diffusion method. By applying an orthogonal design, our results indicated that the optimal formulation was 12 mg-mL PLA, 0.5% gelatin, and an organic phase:glycerol ratio of 1:20. Using the optimal experimental conditions, the drug loading and encapsulation efficiencies were 19.0 ± 1.8% and 62.2 ± 2.6%, respectively. The average particle size was 9.7 ± 0.7 μm. In vitro studies indicated that the ED-PLA-MS demonstrated a well-sustained release efficacy. The microspheres delivered emodin, primarily to the lungs of mice, upon intravenous injection. It was also detected by microscopy that partial lung inflammation was observed in lung tissues and no pathological changes were found in other tissues of the ED-PLA-MS-treated animals. These results suggested that ED-PLA-MS are of potential value in treating lung diseases in animals. View Full-Text

Keywords: lung-targeted; emodin; microspheres; polylactic acid; sustained-release lung-targeted; emodin; microspheres; polylactic acid; sustained-release





Autor: Xiaohong Chen 1,2, Zifeng Yang 1, Renshan Sun 4, Ziyao Mo 1, Guangyao Jin 1, Fenghuan Wei 3, Jianmin Hu 1, Wenda Guan 1 and Nanshan Zhong 1,*

Fuente: http://mdpi.com/



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