Preparation of a novel ginkgolide B niosomal composite drug
Ginkgolide B (GB) and Puerarin (Pue) are active pharmaceutical ingredients for the treatment of Parkinson’s disease (PD); however, both are poorly water-soluble, which limits their bioavailability. The present study used the niosome vesicle encapsulation technique to prepare a novel GB composite dru...
| Main Authors: | , , , , , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
De Gruyter
2020-08-01
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| Series: | Open Chemistry |
| Subjects: | |
| Online Access: | https://doi.org/10.1515/chem-2020-0089 |
| _version_ | 1829517816634540032 |
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| author | Zhou Juntong Wu Xiao Zhao Zhanhong Wang Zhenpeng Li Shumu Chen Chang Yu Shan Qu Xintong Li Kexin Tian Ye Liu Xiaojing Zhang Gaoyu Wang Zhaoxuan Li Chi Kang Ning Huo Qing |
| author_facet | Zhou Juntong Wu Xiao Zhao Zhanhong Wang Zhenpeng Li Shumu Chen Chang Yu Shan Qu Xintong Li Kexin Tian Ye Liu Xiaojing Zhang Gaoyu Wang Zhaoxuan Li Chi Kang Ning Huo Qing |
| author_sort | Zhou Juntong |
| collection | DOAJ |
| description | Ginkgolide B (GB) and Puerarin (Pue) are active pharmaceutical ingredients for the treatment of Parkinson’s disease (PD); however, both are poorly water-soluble, which limits their bioavailability. The present study used the niosome vesicle encapsulation technique to prepare a novel GB composite drug. The conditions for GB–Pue niosomal complex preparation were as follows: a hydration temperature of 60°C, a hydrophilic–lipophilic balance of 10.5, a drug–carrier mass ratio of 8:100, and a surfactant–cholesterol mass ratio of 1.5:1. The niosomal complex suspension was uniformly distributed and milky white in color, with no stratification over a duration of 1 month. It had an average particle size of 187.3 nm, a particle-size distribution of 0.237, a GB encapsulation efficiency (EE) of 68.2%, a GB drug-loading rate of 90.1%, a Pue EE of 40.5%, and a Pue drug-loading rate of 83.3%. The optimal storage temperature for the niosomal complex suspension was 4°C. Following an intravenous injection of the niosomal complex suspension into the rat tail, the area under the curve (AUC) from 0 to 4 h was 54.1 h µg mL−1, with a mean residence time (MRT) of 0.96 h, a distribution half-life (T1/2α) of 0.195 h, and a total clearance of 0.003 L h−1 kg−1. The AUC and MRT of the composite prescription were 1.1- and 1.4-times those of the commercial injection, respectively, showing significantly increased sustained release and bioavailability. Moreover, the distribution of GB in the brain tissue was 1.8-times that of the commercial injection. In conclusion, the novel GB niosomal composite drug, with excellent stability, improved pharmacokinetics, and brain tissue distribution, demonstrates great potential for the delivery of GB and Pue for PD therapeutics. |
| first_indexed | 2024-12-16T14:08:53Z |
| format | Article |
| id | doaj.art-60d167206a7640319d0e2a5777cd34aa |
| institution | Directory Open Access Journal |
| issn | 2391-5420 |
| language | English |
| last_indexed | 2024-12-16T14:08:53Z |
| publishDate | 2020-08-01 |
| publisher | De Gruyter |
| record_format | Article |
| series | Open Chemistry |
| spelling | doaj.art-60d167206a7640319d0e2a5777cd34aa2022-12-21T22:28:50ZengDe GruyterOpen Chemistry2391-54202020-08-011811064107410.1515/chem-2020-0089chem-2020-0089Preparation of a novel ginkgolide B niosomal composite drugZhou Juntong0Wu Xiao1Zhao Zhanhong2Wang Zhenpeng3Li Shumu4Chen Chang5Yu Shan6Qu Xintong7Li Kexin8Tian Ye9Liu Xiaojing10Zhang Gaoyu11Wang Zhaoxuan12Li Chi13Kang Ning14Huo Qing15Department of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaSchool hospital, Beijing Union University, Beijing-100101, People's Republic of ChinaAnalysis and Testing Center, Institute of Chemistry, Chinese Academy of Sciences, Beijing-100190, People's Republic of ChinaAnalysis and Testing Center, Institute of Chemistry, Chinese Academy of Sciences, Beijing-100190, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaDepartment of Biomedicine, Biochemical Engineering College of Beijing Union University, Beijing-100023, People's Republic of ChinaGinkgolide B (GB) and Puerarin (Pue) are active pharmaceutical ingredients for the treatment of Parkinson’s disease (PD); however, both are poorly water-soluble, which limits their bioavailability. The present study used the niosome vesicle encapsulation technique to prepare a novel GB composite drug. The conditions for GB–Pue niosomal complex preparation were as follows: a hydration temperature of 60°C, a hydrophilic–lipophilic balance of 10.5, a drug–carrier mass ratio of 8:100, and a surfactant–cholesterol mass ratio of 1.5:1. The niosomal complex suspension was uniformly distributed and milky white in color, with no stratification over a duration of 1 month. It had an average particle size of 187.3 nm, a particle-size distribution of 0.237, a GB encapsulation efficiency (EE) of 68.2%, a GB drug-loading rate of 90.1%, a Pue EE of 40.5%, and a Pue drug-loading rate of 83.3%. The optimal storage temperature for the niosomal complex suspension was 4°C. Following an intravenous injection of the niosomal complex suspension into the rat tail, the area under the curve (AUC) from 0 to 4 h was 54.1 h µg mL−1, with a mean residence time (MRT) of 0.96 h, a distribution half-life (T1/2α) of 0.195 h, and a total clearance of 0.003 L h−1 kg−1. The AUC and MRT of the composite prescription were 1.1- and 1.4-times those of the commercial injection, respectively, showing significantly increased sustained release and bioavailability. Moreover, the distribution of GB in the brain tissue was 1.8-times that of the commercial injection. In conclusion, the novel GB niosomal composite drug, with excellent stability, improved pharmacokinetics, and brain tissue distribution, demonstrates great potential for the delivery of GB and Pue for PD therapeutics.https://doi.org/10.1515/chem-2020-0089ginkgolide bpuerarinniosomeparkinson’s disease |
| spellingShingle | Zhou Juntong Wu Xiao Zhao Zhanhong Wang Zhenpeng Li Shumu Chen Chang Yu Shan Qu Xintong Li Kexin Tian Ye Liu Xiaojing Zhang Gaoyu Wang Zhaoxuan Li Chi Kang Ning Huo Qing Preparation of a novel ginkgolide B niosomal composite drug Open Chemistry ginkgolide b puerarin niosome parkinson’s disease |
| title | Preparation of a novel ginkgolide B niosomal composite drug |
| title_full | Preparation of a novel ginkgolide B niosomal composite drug |
| title_fullStr | Preparation of a novel ginkgolide B niosomal composite drug |
| title_full_unstemmed | Preparation of a novel ginkgolide B niosomal composite drug |
| title_short | Preparation of a novel ginkgolide B niosomal composite drug |
| title_sort | preparation of a novel ginkgolide b niosomal composite drug |
| topic | ginkgolide b puerarin niosome parkinson’s disease |
| url | https://doi.org/10.1515/chem-2020-0089 |
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