Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes
Paeoniflorin, the main component of total glucosides of paeony (TGP), shows good therapeutic effects in arthritis, but has low bioavailability when administered orally. Avoiding such a deficiency for topical administration would expand its clinical application. This study aimed to avoid these limita...
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| Format: | Article |
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MDPI AG
2018-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/23/12/3371 |
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| author | Yahua Cui Yujia Mo Qi Zhang Wanwan Tian Yutao Xue Jie Bai Shouying Du |
| author_facet | Yahua Cui Yujia Mo Qi Zhang Wanwan Tian Yutao Xue Jie Bai Shouying Du |
| author_sort | Yahua Cui |
| collection | DOAJ |
| description | Paeoniflorin, the main component of total glucosides of paeony (TGP), shows good therapeutic effects in arthritis, but has low bioavailability when administered orally. Avoiding such a deficiency for topical administration would expand its clinical application. This study aimed to avoid these limitations by using nanotechnology (ethosomes) and a physical approach (microneedles). Paeoniflorin-loaded ethosomal formulation (TGP-E) was optimized and evaluated in terms of entrapment efficiency (EE), particle size (PS), zeta potential (ZP), polydispersity index (PDI) and morphology. TGP-E was prepared by the hot injection method and optimized by single-factor tests and an orthogonal experimental design. The optimized paeoniflorin-loaded ethosomes had EE of 27.82 ± 1.56%, PS of 137.9 ± 7.57 nm with PDI of 0.120 ± 0.005, ZP of −0.74 ± 0.43 mV. Ethosomes showed a nearly spherical shape under the transmission electron microscope (TEM). The optimal microneedle-assisted (MN-assisted) conditions were obtained at a microneedle length of 500 μm, a pressure of 3 N and an action time of 3 min. The cumulative penetration amounts (<i>Q<sub>n</sub></i>) of TGP solution transdermal (ST) and MN-assisted TGP solution transdermal (MST) were 24.42 ± 8.35 μg/cm<sup>2</sup> and 548.11 ± 10.49 μg/cm<sup>2</sup>, respectively. <i>Q<sub>n</sub></i> of TGP-E transdermal (PT) and MN-assisted TGP-E transdermal (MPT) were 54.97 ± 4.72 μg/cm<sup>2</sup> and 307.17 ± 26.36 μg/cm<sup>2</sup>, respectively. These findings indicate that use of ethosomes and microneedles can both enhance the penetration ofpaeoniflorin, but for the water-soluble drug, there is no obvious synergism between nanotechnology and microneedles for enhancing penetration in a transdermal drug delivery system. |
| first_indexed | 2024-12-10T07:07:39Z |
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| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-10T07:07:39Z |
| publishDate | 2018-12-01 |
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| series | Molecules |
| spelling | doaj.art-9f4a38d1933a478f8e6a5195a34087ad2022-12-22T01:58:08ZengMDPI AGMolecules1420-30492018-12-012312337110.3390/molecules23123371molecules23123371Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded EthosomesYahua Cui0Yujia Mo1Qi Zhang2Wanwan Tian3Yutao Xue4Jie Bai5Shouying Du6School of Chinese Materia Medica, Beijing University of Chinese Medicine, Fangshan District, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Fangshan District, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Fangshan District, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Fangshan District, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Fangshan District, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Fangshan District, Beijing 102488, ChinaSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, Fangshan District, Beijing 102488, ChinaPaeoniflorin, the main component of total glucosides of paeony (TGP), shows good therapeutic effects in arthritis, but has low bioavailability when administered orally. Avoiding such a deficiency for topical administration would expand its clinical application. This study aimed to avoid these limitations by using nanotechnology (ethosomes) and a physical approach (microneedles). Paeoniflorin-loaded ethosomal formulation (TGP-E) was optimized and evaluated in terms of entrapment efficiency (EE), particle size (PS), zeta potential (ZP), polydispersity index (PDI) and morphology. TGP-E was prepared by the hot injection method and optimized by single-factor tests and an orthogonal experimental design. The optimized paeoniflorin-loaded ethosomes had EE of 27.82 ± 1.56%, PS of 137.9 ± 7.57 nm with PDI of 0.120 ± 0.005, ZP of −0.74 ± 0.43 mV. Ethosomes showed a nearly spherical shape under the transmission electron microscope (TEM). The optimal microneedle-assisted (MN-assisted) conditions were obtained at a microneedle length of 500 μm, a pressure of 3 N and an action time of 3 min. The cumulative penetration amounts (<i>Q<sub>n</sub></i>) of TGP solution transdermal (ST) and MN-assisted TGP solution transdermal (MST) were 24.42 ± 8.35 μg/cm<sup>2</sup> and 548.11 ± 10.49 μg/cm<sup>2</sup>, respectively. <i>Q<sub>n</sub></i> of TGP-E transdermal (PT) and MN-assisted TGP-E transdermal (MPT) were 54.97 ± 4.72 μg/cm<sup>2</sup> and 307.17 ± 26.36 μg/cm<sup>2</sup>, respectively. These findings indicate that use of ethosomes and microneedles can both enhance the penetration ofpaeoniflorin, but for the water-soluble drug, there is no obvious synergism between nanotechnology and microneedles for enhancing penetration in a transdermal drug delivery system.https://www.mdpi.com/1420-3049/23/12/3371Paeoniflorintotal glucosides of paeonyethosomesmicroneedletransdermal |
| spellingShingle | Yahua Cui Yujia Mo Qi Zhang Wanwan Tian Yutao Xue Jie Bai Shouying Du Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes Molecules Paeoniflorin total glucosides of paeony ethosomes microneedle transdermal |
| title | Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes |
| title_full | Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes |
| title_fullStr | Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes |
| title_full_unstemmed | Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes |
| title_short | Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes |
| title_sort | microneedle assisted percutaneous delivery of paeoniflorin loaded ethosomes |
| topic | Paeoniflorin total glucosides of paeony ethosomes microneedle transdermal |
| url | https://www.mdpi.com/1420-3049/23/12/3371 |
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