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Updated: Dec 31, 2025
Polymeric Microneedle Array Fabrication by Photolithography
Published on: November 17, 2015
Transdermal delivery of rapamycin with poor water-solubility by dissolving polymeric microneedles for
Jinzhu Mao1, Hua Wang2, Ying Xie1
1Department of Dermatology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology (HUST), Wuhan 430022, China. tjhappy@126.com.
Abstract:
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.
Insights
This study developed dissolving polymeric microneedles loaded with rapamycin (RAPA DMNs) to treat vascular anomalies (VAs). RAPA DMNs offer a safe and effective method for delivering RAPA, overcoming its limitations for VA treatment.
Area of Science:
- Biomaterials Science
- Dermatology
- Pharmacology
Background:
- Angiogenesis is crucial in skin tumors and vascular anomalies (VAs).
- Rapamycin (RAPA) shows potential for inhibiting angiogenesis but faces challenges like poor solubility and high cytotoxicity.
- Existing treatments for VAs often have limitations in efficacy and safety.
Purpose of the Study:
- To develop rapamycin-loaded dissolving polymeric microneedles (RAPA DMNs) for enhanced vascular anomaly treatment.
- To evaluate the efficacy and safety of RAPA DMNs in delivering rapamycin.
- To assess the anti-angiogenic properties of RAPA DMNs.
Main Methods:
- Fabrication of RAPA DMNs using polyvinylpyrrolidone (PVP) for improved rapamycin solubility.
- Assessment of microneedle mechanical strength and drug delivery depth.
- In vitro drug release studies and skin penetration evaluation.
- In vivo studies on mice skin repair and anti-angiogenic effects on HUVECs and VEGF secretion.
Main Results:
- RAPA DMNs possess sufficient mechanical strength to penetrate the stratum corneum, delivering RAPA to a depth of 200 μm.
- Microneedle shafts dissolved completely within 10 minutes ex vivo, releasing 80% of the loaded RAPA.
- RAPA DMN application resulted in rapid skin self-repair within 4 hours.
- Significant inhibition of human umbilical vein endothelial cell (HUVEC) growth and decreased vascular endothelial growth factor (VEGF) secretion were observed.
Conclusions:
- RAPA DMNs provide a promising strategy to overcome the limitations of rapamycin for vascular anomaly treatment.
- The developed microneedle system ensures efficient drug delivery and demonstrates potent anti-angiogenic effects.
- RAPA DMNs represent a safe and effective therapeutic approach for vascular anomalies.
