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Pharmaceutics 2017, 9(3), 29; doi:10.3390/pharmaceutics9030029

Efficient Transdermal Delivery of Alendronate, a Nitrogen-Containing Bisphosphonate, Using Tip-Loaded Self-Dissolving Microneedle Arrays for the Treatment of Osteoporosis

1
Department of Biopharmaceutics, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8414, Japan
2
CosMED Pharmaceutical Co., Ltd, Minami-ku, Kyoto 601-8014, Japan
3
Department of Pharmaceutical Technology, Kobe Pharmaceutical University, Higashinada-ku, Kobe 658-8558, Japan
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 13 July 2017 / Revised: 11 August 2017 / Accepted: 14 August 2017 / Published: 17 August 2017
(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
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Abstract

To improve the transdermal bioavailability and safety of alendronate (ALN), a nitrogen-containing bisphosphonate, we developed self-dissolving microneedle arrays (MNs), in which ALN is loaded only at the tip portion of micron-scale needles by a dip-coating method (ALN(TIP)–MN). We observed micron-scale pores in rat skin just after application of ALN(TIP)–MN, indicating that transdermal pathways for ALN were created by MN. ALN was rapidly released from the tip of MNs as observed in an in vitro release study. The tip portions of MNs completely dissolved in the rat skin within 5 min after application in vivo. After application of ALN(TIP)–MN in mice, the plasma concentration of ALN rapidly increased, and the bioavailability of ALN was approximately 96%. In addition, the decrease in growth plate was effectively suppressed by this efficient delivery of ALN in a rat model of osteoporosis. Furthermore, no skin irritation was observed after application of ALN(TIP)–MN and subcutaneous injection of ALN, while mild skin irritation was induced by whole-ALN-loaded MN (ALN–MN)—in which ALN is contained in the whole of the micron-scale needles fabricated from hyaluronic acid—and intradermal injection of ALN. These findings indicate that ALN(TIP)–MN is a promising transdermal formulation for the treatment of osteoporosis without skin irritation. View Full-Text
Keywords: self-dissolving microneedle arrays; dip-coating method; alendronate; transdermal absorption; skin irritation; osteoporosis self-dissolving microneedle arrays; dip-coating method; alendronate; transdermal absorption; skin irritation; osteoporosis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Katsumi, H.; Tanaka, Y.; Hitomi, K.; Liu, S.; Quan, Y.-S.; Kamiyama, F.; Sakane, T.; Yamamoto, A. Efficient Transdermal Delivery of Alendronate, a Nitrogen-Containing Bisphosphonate, Using Tip-Loaded Self-Dissolving Microneedle Arrays for the Treatment of Osteoporosis. Pharmaceutics 2017, 9, 29.

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