Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride
Oral propranolol hydrochloride has been the first-line treatment for infantile hemangioma (IH), whereas systemic exposure to propranolol has the potential of causing serious adverse reactions. Dermal delivery of propranolol is preferable due to high local drug concentration and fewer adverse effects...
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| Format: | Article |
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MDPI AG
2021-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/4/579 |
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| author | Jingjing He Zichen Zhang Xianzi Zheng Lu Li Jianping Qi Wei Wu Yi Lu |
| author_facet | Jingjing He Zichen Zhang Xianzi Zheng Lu Li Jianping Qi Wei Wu Yi Lu |
| author_sort | Jingjing He |
| collection | DOAJ |
| description | Oral propranolol hydrochloride has been the first-line treatment for infantile hemangioma (IH), whereas systemic exposure to propranolol has the potential of causing serious adverse reactions. Dermal delivery of propranolol is preferable due to high local drug concentration and fewer adverse effects. However, propranolol hydrochloride (BCS class I) is highly hydrophilic and has difficulty in penetrating the stratum corneum (SC) barrier. Dissolving microneedles (MNs) are an efficient tool for overcoming the barrier of the SC and enhancing dermal drug delivery. In this study, propranolol hydrochloride-loaded dissolving MNs were fabricated by using hyaluronic acid and polyvinyl pyrrolidone as matrix materials. Controllable drug loading in needle tips was achieved by a two-step casting procedure. The needles were good in mechanical strength for penetrating the SC while presented excellent dissolving capability for releasing propranolol hydrochloride. In comparison with the solution counterpart, irrespective of being applied to intact skin or solid MNs-pretreated skin, dissolving MNs significantly increased the permeability and skin retention of propranolol. In conclusion, dissolving MNs could be a potential approach for enhancing dermal delivery of propranolol to treat IH. |
| first_indexed | 2024-03-10T12:11:25Z |
| format | Article |
| id | doaj.art-510884e732214d2886f3fbeec5717ef3 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T12:11:25Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-510884e732214d2886f3fbeec5717ef32023-11-21T16:10:40ZengMDPI AGPharmaceutics1999-49232021-04-0113457910.3390/pharmaceutics13040579Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol HydrochlorideJingjing He0Zichen Zhang1Xianzi Zheng2Lu Li3Jianping Qi4Wei Wu5Yi Lu6Key Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, ChinaKey Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, ChinaKey Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, ChinaKey Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, ChinaKey Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, ChinaKey Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, ChinaKey Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, ChinaOral propranolol hydrochloride has been the first-line treatment for infantile hemangioma (IH), whereas systemic exposure to propranolol has the potential of causing serious adverse reactions. Dermal delivery of propranolol is preferable due to high local drug concentration and fewer adverse effects. However, propranolol hydrochloride (BCS class I) is highly hydrophilic and has difficulty in penetrating the stratum corneum (SC) barrier. Dissolving microneedles (MNs) are an efficient tool for overcoming the barrier of the SC and enhancing dermal drug delivery. In this study, propranolol hydrochloride-loaded dissolving MNs were fabricated by using hyaluronic acid and polyvinyl pyrrolidone as matrix materials. Controllable drug loading in needle tips was achieved by a two-step casting procedure. The needles were good in mechanical strength for penetrating the SC while presented excellent dissolving capability for releasing propranolol hydrochloride. In comparison with the solution counterpart, irrespective of being applied to intact skin or solid MNs-pretreated skin, dissolving MNs significantly increased the permeability and skin retention of propranolol. In conclusion, dissolving MNs could be a potential approach for enhancing dermal delivery of propranolol to treat IH.https://www.mdpi.com/1999-4923/13/4/579microneedlespropranolol hydrochloridedermal deliveryhyaluronic acidpolyvinyl pyrrolidoneinfantile hemangioma |
| spellingShingle | Jingjing He Zichen Zhang Xianzi Zheng Lu Li Jianping Qi Wei Wu Yi Lu Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride Pharmaceutics microneedles propranolol hydrochloride dermal delivery hyaluronic acid polyvinyl pyrrolidone infantile hemangioma |
| title | Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride |
| title_full | Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride |
| title_fullStr | Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride |
| title_full_unstemmed | Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride |
| title_short | Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride |
| title_sort | design and evaluation of dissolving microneedles for enhanced dermal delivery of propranolol hydrochloride |
| topic | microneedles propranolol hydrochloride dermal delivery hyaluronic acid polyvinyl pyrrolidone infantile hemangioma |
| url | https://www.mdpi.com/1999-4923/13/4/579 |
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