Enhancement of oral bioavailability of cyclosporine A: comparison of various nanoscale drug-delivery systems
Kai Wang,1–3 Jianping Qi,1 Tengfei Weng,1,2 Zhiqiang Tian,1 Yi Lu,1 Kaili Hu,4 Zongning Yin,2 Wei Wu1 1School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of Ministry of Education, Shanghai, People’s Republic of China; 2West China School of Pharmacy, Sic...
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Dove Medical Press
2014
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oai:doaj.org-article:c35361f1864f40f78bfcc56e981a09192021-12-02T03:58:30ZEnhancement of oral bioavailability of cyclosporine A: comparison of various nanoscale drug-delivery systems1178-2013https://doaj.org/article/c35361f1864f40f78bfcc56e981a09192014-10-01T00:00:00Zhttp://www.dovepress.com/enhancement-of-oral-bioavailability-of-cyclosporine-a-comparison-of-va-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Kai Wang,1–3 Jianping Qi,1 Tengfei Weng,1,2 Zhiqiang Tian,1 Yi Lu,1 Kaili Hu,4 Zongning Yin,2 Wei Wu1 1School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of Ministry of Education, Shanghai, People’s Republic of China; 2West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, People’s Republic of China; 3Tropical Crops Genetic Resources Institute, Hainan Provincial Engineering Research Center for Blumea Balsamifera, Chinese Academy of Tropical Agricultural Sciences, Danzhou, Hainan, People’s Republic of China; 4Murad Research Center for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, People’s Republic of ChinaAbstract: A variety of nanoscale delivery systems have been shown to enhance the oral absorption of poorly water-soluble and poorly permeable drugs. However, the performance of these systems has seldom been evaluated simultaneously. The aim of this study was to compare the bioavailability enhancement effect of lipid-based nanocarriers with poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) to highlight the importance of the lipid composition, with cyclosporine A (CyA) as a model drug. CyA-loaded PLGA NPs, nanostructured lipid carriers (NLCs), and self-microemulsifying drug-delivery systems (SMEDDS) were prepared. The particle size of PLGA NPs (182.2±12.8 nm) was larger than that of NLCs (89.7±9.0 nm) and SMEDDS (26.9±1.9 nm). All vehicles are charged negatively. The entrapment efficiency of PLGA NPs and NLCs was 87.6%±1.6% and 80.3%±0.6%, respectively. In vitro release tests indicated that the cumulative release of CyA was lower than 4% from all vehicles, including Sandimmun Neoral®, according to the dialysis method. Both NLCs and SMEDDS showed high relative oral bioavailability, 111.8% and 73.6%, respectively, after oral gavage administration to beagle dogs, which was not statistically different from commercial Sandimmun Neoral®. However, PLGA NPs failed to achieve efficient absorption, with relative bioavailability of about 22.7%. It is concluded that lipid-based nanoscale drug-delivery systems are superior to polymeric NPs in enhancing oral bioavailability of poorly water-soluble and poorly permeable drugs. Keywords: cyclosporine A, PLGA nanoparticle, nanostructured lipid carrier, self-microemulsifying drug-delivery systems, bioavailabilityWang KQi JPWeng TFTian ZQLu YHu KLYin ZNWu WDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 4991-4999 (2014) |
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Medicine (General) R5-920 |
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Medicine (General) R5-920 Wang K Qi JP Weng TF Tian ZQ Lu Y Hu KL Yin ZN Wu W Enhancement of oral bioavailability of cyclosporine A: comparison of various nanoscale drug-delivery systems |
| description |
Kai Wang,1–3 Jianping Qi,1 Tengfei Weng,1,2 Zhiqiang Tian,1 Yi Lu,1 Kaili Hu,4 Zongning Yin,2 Wei Wu1 1School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of Ministry of Education, Shanghai, People’s Republic of China; 2West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, People’s Republic of China; 3Tropical Crops Genetic Resources Institute, Hainan Provincial Engineering Research Center for Blumea Balsamifera, Chinese Academy of Tropical Agricultural Sciences, Danzhou, Hainan, People’s Republic of China; 4Murad Research Center for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, People’s Republic of ChinaAbstract: A variety of nanoscale delivery systems have been shown to enhance the oral absorption of poorly water-soluble and poorly permeable drugs. However, the performance of these systems has seldom been evaluated simultaneously. The aim of this study was to compare the bioavailability enhancement effect of lipid-based nanocarriers with poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) to highlight the importance of the lipid composition, with cyclosporine A (CyA) as a model drug. CyA-loaded PLGA NPs, nanostructured lipid carriers (NLCs), and self-microemulsifying drug-delivery systems (SMEDDS) were prepared. The particle size of PLGA NPs (182.2±12.8 nm) was larger than that of NLCs (89.7±9.0 nm) and SMEDDS (26.9±1.9 nm). All vehicles are charged negatively. The entrapment efficiency of PLGA NPs and NLCs was 87.6%±1.6% and 80.3%±0.6%, respectively. In vitro release tests indicated that the cumulative release of CyA was lower than 4% from all vehicles, including Sandimmun Neoral®, according to the dialysis method. Both NLCs and SMEDDS showed high relative oral bioavailability, 111.8% and 73.6%, respectively, after oral gavage administration to beagle dogs, which was not statistically different from commercial Sandimmun Neoral®. However, PLGA NPs failed to achieve efficient absorption, with relative bioavailability of about 22.7%. It is concluded that lipid-based nanoscale drug-delivery systems are superior to polymeric NPs in enhancing oral bioavailability of poorly water-soluble and poorly permeable drugs. Keywords: cyclosporine A, PLGA nanoparticle, nanostructured lipid carrier, self-microemulsifying drug-delivery systems, bioavailability |
| format |
article |
| author |
Wang K Qi JP Weng TF Tian ZQ Lu Y Hu KL Yin ZN Wu W |
| author_facet |
Wang K Qi JP Weng TF Tian ZQ Lu Y Hu KL Yin ZN Wu W |
| author_sort |
Wang K |
| title |
Enhancement of oral bioavailability of cyclosporine A: comparison of various nanoscale drug-delivery systems |
| title_short |
Enhancement of oral bioavailability of cyclosporine A: comparison of various nanoscale drug-delivery systems |
| title_full |
Enhancement of oral bioavailability of cyclosporine A: comparison of various nanoscale drug-delivery systems |
| title_fullStr |
Enhancement of oral bioavailability of cyclosporine A: comparison of various nanoscale drug-delivery systems |
| title_full_unstemmed |
Enhancement of oral bioavailability of cyclosporine A: comparison of various nanoscale drug-delivery systems |
| title_sort |
enhancement of oral bioavailability of cyclosporine a: comparison of various nanoscale drug-delivery systems |
| publisher |
Dove Medical Press |
| publishDate |
2014 |
| url |
https://doaj.org/article/c35361f1864f40f78bfcc56e981a0919 |
| work_keys_str_mv |
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