Novel tip-loaded dissolving and implantable microneedle array patches for sustained release of finasteride

• Published in: International journal of pharmaceutics 2021-09, Vol.606, p.120885-120885, Article 120885
• Main Authors: Paredes, Alejandro J., Volpe-Zanutto, Fabiana, Permana, Andi Dian, Murphy, Aidan J., Picco, Camila J., Vora, Lalitkumar K., Coulter, Jonathan A., Donnelly, Ryan F.
• Format: Article
• Language: English
• Subjects: Finasteride; Long-acting; Microarray Patches; Microneedles; PLGA
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2021.120885

[Display omitted] •FND is prescribed orally for alopecia and prostatic hyperplasia in lifelong treatments.•Long-acting MAPs could be a patient-friendly option for the delivery of FND.•Bi-layered dissolving and implantable MAPs were obtained by a micromoulding method.•The novel MAPs presented suitable mechanical properties for skin penetration.•FND MAPs were able to deliver the active in a long-acting manner. Finasteride (FND) is a competitive inhibitor of 5α-reductase, an enzyme involved in benign prostatic hyperplasia (BPH) and androgenic alopecia. FND is administered in oral, often lifelong treatments, increasing the pill burden of polymedicated patients. Microneedle array patches (MAPs) are minimally invasive devices that painlessly pierce the outermost layers of the skin, forming slowly-dissolving drug depots in the dermis, which can release drugs over weeks or months, making this platform an attractive, patient-friendly option for long-term treatments. This work describes the development of long-acting dissolving and implantable PLGA MAPs aimed for systemic release of FND for at least two weeks. Mechanically strong tip-loaded MAPs with pyramidal geometry were obtained using micromoulding methodology. In vitro studies revealed that the dissolving and implantable MAPs were able to release the drug for over 7 and 14 days, respectively. Skin deposition experiments in Franz cells demonstrated that after 24 h, dissolving and implantable MAPs were able to deposit 629.00 ± 214.54 μg and 1861.64 ± 383.30 μg of FND in the skin, respectively. On the other hand, transdermal permeation studies showed that both formulations produced a slow release of the drug to the receptor compartment of the Franz cells, with dissolving and implantable MAPs releasing 90.43 ± 6.20 μg and 27.80 ± 3.94 μg of FND after 24 h. The formulations described here could be an alternative to current oral treatments, having the potential to deliver the drug for extended periods, simplifying the treatment of BPH and androgenic alopecia.