Transdermal Delivery of Luteinizing Hormone-releasing Hormone with Chitosan Microneedles: A Promising Tool for Androgen Deprivation Therapy

Long-term administration of luteinizing hormone-releasing hormone analogs (LHRHa) is the main type of androgen-deprivation therapy (ADT) for lethal prostate cancer. A fully insertable microneedle system, composed of embeddable chitosan microneedles and a dissolvable polyvinyl alcohol/polyvinyl pyrrolidone supporting array, was developed for sustained delivery of LHRHa to the skin. A porcine cadaver skin test showed that chitosan microneedles can be fully embedded within the skin and microneedle-created micropores reseal within 7 days. The measured LHRHa loading amount was 73.3±2.8 μg per microneedle patch. After applying goserelin-containing microneedles to mice, serum LH levels increased initially and then declined below baseline at day 7. In contrast, serum testosterone levels increased to reach a peak at day 14 and then declined to a castration level at day 21. Additionally, such a castration level was maintained for 2 weeks. Therefore, transdermal delivery of goserelin with embeddable chitosan microneedles can produce a castrated state in mice. Such a system is a promising, feasible means of delivering ADT.

Anticancer research. 2017 Dec [Epub]

Ming-Yang Chen, Yi-Ying Chen, Hsin-Tzu Tsai, Tzong-Shin Tzai, Mei-Chin Chen, Yuh-Shyan Tsai

Department of Urology, Madou Sin-Lau Hospital, Sin-Lau Medical Foundation, the Presbyterian Church in Taiwan, Tainan, Taiwan, R.O.C., Department of Chemical Engineering, National Cheng Kung University, Tainan, Taiwan, R.O.C., Department of Urology, National Cheng Kung University Hospital, College of Medicine, National Cheng Kung University, Tainan, Taiwan, R.O.C., Department of Urology, School of Medicine, China Medical University, Taichung, Taiwan, R.O.C., Department of Chemical Engineering, National Cheng Kung University, Tainan, Taiwan, R.O.C. ., Department of Urology, National Cheng Kung University Hospital, College of Medicine, National Cheng Kung University, Tainan, Taiwan, R.O.C. .