Transdermal delivery of rapamycin with poor water-solubility by dissolving polymeric microneedles for anti-angiogenesis
| Autor: | Yangxue Fu, Liu Pei, Zhu Jinjin, Lianbin Zhang, Jinzhu Mao, Hua Wang, Juan Tao, M. Mahmood Hussain, Liyun Dong, Du Hongyao, Jintao Zhu, Yuce Li, Ying Xie, Yan Li |
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| Rok vydání: | 2020 |
| Předmět: |
Vascular Endothelial Growth Factor A
Polymers Surface Properties Vascular Malformations Angiogenesis Biomedical Engineering Angiogenesis Inhibitors 02 engineering and technology Pharmacology Administration Cutaneous 010402 general chemistry 01 natural sciences Umbilical vein Neovascularization chemistry.chemical_compound Drug Delivery Systems Materials Testing medicine Stratum corneum Humans General Materials Science Particle Size Cells Cultured Cell Proliferation Transdermal Sirolimus Neovascularization Pathologic Water General Chemistry General Medicine 021001 nanoscience & nanotechnology 0104 chemical sciences Bioavailability Vascular endothelial growth factor medicine.anatomical_structure Solubility chemistry medicine.symptom 0210 nano-technology Ex vivo |
| Zdroj: | Journal of Materials Chemistry B. 8:928-934 |
| ISSN: | 2050-7518 2050-750X |
| DOI: | 10.1039/c9tb00912d |
| Popis: | Angiogenesis plays an important role in the occurrence and development of skin tumors and vascular anomalies (VAs). Many drugs have been adopted for the inhibition of angiogenesis, among which rapamycin (RAPA) possesses good application prospects. However, the clinical potential of RAPA for VAs is limited by its poor solubility, low bioavailability, and high cytotoxicity. To extend its application prospect for VAs treatment, in this study, we develop RAPA-loaded dissolving polymeric microneedles (RAPA DMNs) made of polyvinylpyrrolidone (PVP) due to its excellent solubilizing ability. RAPA DMNs are shown to have sufficient mechanical strength to overcome the skin barrier of the stratum corneum and could deliver RAPA to a depth of 200 μm. The microneedle shafts completely dissolve and 80% of the drug could be released within 10 min after insertion ex vivo. The DMNs-penetrated mice skin could repair itself within 4 h after the application of RAPA DMNs. RAPA DMNs also show good anti-angiogenic effect by inhibiting the growth of human umbilical vein endothelial cells (HUVECs) and decreasing the secretion of vascular endothelial growth factor (VEGF). Therefore, RAPA DMNs promisingly provide a safe and efficient approach for VAs treatment. |
| Databáze: | OpenAIRE |
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