Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride

被引:47
|
作者
He, Jingjing [1 ]
Zhang, Zichen [1 ]
Zheng, Xianzi [1 ]
Li, Lu [1 ]
Qi, Jianping [1 ]
Wu, Wei [1 ,2 ]
Lu, Yi [1 ]
机构
[1] Fudan Univ, Key Lab Smart Drug Delivery MOE, Sch Pharm, Shanghai 201203, Peoples R China
[2] Fudan Univ, Pudong Med Ctr, Shanghai Pudong Hosp, Ctr Med Res & Innovat, Shanghai 201399, Peoples R China
关键词
microneedles; propranolol hydrochloride; dermal delivery; hyaluronic acid; polyvinyl pyrrolidone; infantile hemangioma; TRANSDERMAL DELIVERY; DRUG-DELIVERY; INFANTILE HEMANGIOMAS; SKIN PENETRATION; IONTOPHORESIS; PATCH; MAGNETOPHORESIS; FORMULATION; BARRIER; WAVES;
D O I
10.3390/pharmaceutics13040579
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
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页数:15
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