Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo
Xiaolong Tang,1,2,* He Zhu,3,* Ledong Sun,4,* Wei Hou,2 Shuyu Cai,1 Rongbo Zhang,1 Feng Liu5 1Stem Cell Engineering Research Center, School of Medicine, Anhui University of Science and Technology, Huainan, People’s Republic of China; 2State Key Laboratory of Virology, Life Sciences Colleg...
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Dove Medical Press
2014
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oai:doaj.org-article:1b6c206cd42a4a2f8e3a7e4955d66c3f2021-12-02T08:20:26ZEnhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo1178-2013https://doaj.org/article/1b6c206cd42a4a2f8e3a7e4955d66c3f2014-11-01T00:00:00Zhttp://www.dovepress.com/enhanced-antifungal-effects-of-amphotericin-b-tpgs-b-pcl-ran-pga-nanop-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Xiaolong Tang,1,2,* He Zhu,3,* Ledong Sun,4,* Wei Hou,2 Shuyu Cai,1 Rongbo Zhang,1 Feng Liu5 1Stem Cell Engineering Research Center, School of Medicine, Anhui University of Science and Technology, Huainan, People’s Republic of China; 2State Key Laboratory of Virology, Life Sciences College, Wuhan University, Wuhan, Hubei, People’s Republic of China; 3Institute of Skin Damage and Repair, General Hospital of Beijing Military Command, Beijing, People’s Republic of China; 4Department of Dermatology, Zhujiang Hospital, Southern Medical University, Guangzhou, Guangdong, People’s Republic of China; 5Department of Anesthesiology, Children’s Hospital, Chongqing Medical University; Key Laboratory of Child Development and Disorders of the Ministry of Education, Chongqing, People’s Republic of China *These authors contributed equally to this work Background: Amphotericin B (AMB) is a polyene antibiotic with broad spectrum antifungal activity, but its clinical toxicities and poor solubility limit the wide application of AMB in clinical practice. Recently, new drug-loaded nanoparticles (NPs) – diblock copolymer D-α-tocopheryl polyethylene glycol 1000 succinate-b-poly(ε-caprolactone-ran-glycolide) (PLGA-TPGS) – have received special attention for their reduced toxicity, and increased effectiveness of drug has also been reported. This study aimed to develop AMB-loaded PLGA-TPGS nanoparticles (AMB-NPs) and evaluate their antifungal effects in vitro and in vivo.Methods: AMB-NPs were prepared with a modified nanoprecipitation method and then characterized in terms of physical characteristics, in vitro drug release, stability, drug-encapsulation efficiency, and toxicity. Finally, the antifungal activity of AMB-NPs was investigated in vitro and in vivo.Results: AMB-NPs were stable and spherical, with an average size of around 110 nm; the entrapment efficacy was closed to 85%, and their release exhibited a typically biphasic pattern. The actual minimum inhibitory concentration of AMB-NPs against Candida albicans was significantly lower than that of free AMB, and AMB-NPs were less toxic on blood cells. In vivo experiments indicated that AMB-NPs achieved significantly better and prolonged antifungal effects when compared with free AMB.Conclusion: The AMB-PLGA-TPGS NP system significantly improves the AMB bioavailability by improving its antifungal activities and reducing its toxicity, and thus, these NPs may become a good drug carrier for antifungal treatment. Keywords: drug delivery, anti-infection, nanocarrier, C. albicans, amphotericin BTang XZhu HSun LHou WCai SZhang RLiu FDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 5403-5413 (2014) |
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Medicine (General) R5-920 Tang X Zhu H Sun L Hou W Cai S Zhang R Liu F Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo |
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Xiaolong Tang,1,2,* He Zhu,3,* Ledong Sun,4,* Wei Hou,2 Shuyu Cai,1 Rongbo Zhang,1 Feng Liu5 1Stem Cell Engineering Research Center, School of Medicine, Anhui University of Science and Technology, Huainan, People’s Republic of China; 2State Key Laboratory of Virology, Life Sciences College, Wuhan University, Wuhan, Hubei, People’s Republic of China; 3Institute of Skin Damage and Repair, General Hospital of Beijing Military Command, Beijing, People’s Republic of China; 4Department of Dermatology, Zhujiang Hospital, Southern Medical University, Guangzhou, Guangdong, People’s Republic of China; 5Department of Anesthesiology, Children’s Hospital, Chongqing Medical University; Key Laboratory of Child Development and Disorders of the Ministry of Education, Chongqing, People’s Republic of China *These authors contributed equally to this work Background: Amphotericin B (AMB) is a polyene antibiotic with broad spectrum antifungal activity, but its clinical toxicities and poor solubility limit the wide application of AMB in clinical practice. Recently, new drug-loaded nanoparticles (NPs) – diblock copolymer D-α-tocopheryl polyethylene glycol 1000 succinate-b-poly(ε-caprolactone-ran-glycolide) (PLGA-TPGS) – have received special attention for their reduced toxicity, and increased effectiveness of drug has also been reported. This study aimed to develop AMB-loaded PLGA-TPGS nanoparticles (AMB-NPs) and evaluate their antifungal effects in vitro and in vivo.Methods: AMB-NPs were prepared with a modified nanoprecipitation method and then characterized in terms of physical characteristics, in vitro drug release, stability, drug-encapsulation efficiency, and toxicity. Finally, the antifungal activity of AMB-NPs was investigated in vitro and in vivo.Results: AMB-NPs were stable and spherical, with an average size of around 110 nm; the entrapment efficacy was closed to 85%, and their release exhibited a typically biphasic pattern. The actual minimum inhibitory concentration of AMB-NPs against Candida albicans was significantly lower than that of free AMB, and AMB-NPs were less toxic on blood cells. In vivo experiments indicated that AMB-NPs achieved significantly better and prolonged antifungal effects when compared with free AMB.Conclusion: The AMB-PLGA-TPGS NP system significantly improves the AMB bioavailability by improving its antifungal activities and reducing its toxicity, and thus, these NPs may become a good drug carrier for antifungal treatment. Keywords: drug delivery, anti-infection, nanocarrier, C. albicans, amphotericin B |
format |
article |
author |
Tang X Zhu H Sun L Hou W Cai S Zhang R Liu F |
author_facet |
Tang X Zhu H Sun L Hou W Cai S Zhang R Liu F |
author_sort |
Tang X |
title |
Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo |
title_short |
Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo |
title_full |
Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo |
title_fullStr |
Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo |
title_full_unstemmed |
Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo |
title_sort |
enhanced antifungal effects of amphotericin b-tpgs-b-(pcl-ran-pga) nanoparticles in vitro and in vivo |
publisher |
Dove Medical Press |
publishDate |
2014 |
url |
https://doaj.org/article/1b6c206cd42a4a2f8e3a7e4955d66c3f |
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