Improvement of Transdermal Delivery of Sumatriptan Succinate Using a Novel Self-dissolving Microneedle Array Fabricated from Sodium Hyaluronate in Rats
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- Wu Dan
- Department of Biopharmaceutics, Kyoto Pharmaceutical University
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- Quan Ying-shu
- CosMED Pharmaceutical Co., Ltd.
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- Kamiyama Fumio
- CosMED Pharmaceutical Co., Ltd.
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- Kusamori Kosuke
- Department of Biopharmaceutics, Kyoto Pharmaceutical University
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- Katsumi Hidemasa
- Department of Biopharmaceutics, Kyoto Pharmaceutical University
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- Sakane Toshiyasu
- Department of Biopharmaceutics, Kyoto Pharmaceutical University
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- Yamamoto Akira
- Department of Biopharmaceutics, Kyoto Pharmaceutical University
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The purpose of the present study was to develop an alternative transdermal formulation containing sumatriptan succinate (SS) for the treatment of migraine. Novel self-dissolving SS-loaded microneedle arrays (MNs) were fabricated from sodium hyaluronate and their efficacy for transdermal delivery of SS was characterized. The resulting MNs maintained their skin piercing abilities for at least 30 min after being placed at a high relative humidity of 75%. Rapid release of SS from the MNs was also observed in vitro. Optical coherence tomography images demonstrated that MNs were able to successfully pierce into rat skin without any bending or cracking, and needles were completely dissolved within 1 h. MNs significantly increased transepidermal water loss; however, skin barrier function gradually recovered to control levels within 24 h, in contrast to the skin damage observed after tape stripping treatment. These findings indicated that the micropores created by MNs quickly resealed, and that the skin damage was reversible. Furthermore, a dose-dependent plasma concentration of SS was obtained after transdermal delivery using SS-loaded MNs in rats. Absorption of SS delivered by MNs was similar to that observed after subcutaneous injection and was associated with high bioavailability (ca. 90%), which was much higher than that produced by oral administration. These findings suggested that application of SS-loaded MNs to the skin provided an effective alternative approach to enhance the transdermal delivery of SS without serious skin damage, and would be likely to improve patient compliance.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 38 (3), 365-373, 2015
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204631332992
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- NII論文ID
- 130004872279
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- NII書誌ID
- AA10885497
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- ISSN
- 13475215
- 09186158
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- NDL書誌ID
- 026193151
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- PubMed
- 25757917
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 使用不可