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Article

Design of Nanocrystalline Suspension of Dutasteride for Intramuscular Prolonged Delivery

College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan 31116, Chungnam, Republic of Korea
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Nanomaterials 2024, 14(22), 1781; https://doi.org/10.3390/nano14221781
Submission received: 25 September 2024 / Revised: 30 October 2024 / Accepted: 2 November 2024 / Published: 5 November 2024

Abstract

The aim of the study is to formulate an injectable nanocrystalline suspension (NS) of dutasteride (DTS), a hydrophobic 5α-reductase inhibitor used to treat benign prostatic hyperplasia and scalp hair loss, for parenteral long-acting delivery. A DTS-loaded NS (DTS-NS, 40 mg/mL DTS) was prepared using a lab-scale bead-milling technique. The optimized DTS-NS prepared using Tween 80 (0.5% w/v) as a nano-suspending agent, was characterized as follows: rod/rectangular shape; particle size of 324 nm; zeta potential of −11 mV; and decreased drug crystallinity compared with intact drug powder. The DTS-NS exhibited a markedly protracted drug concentration-time profile following intramuscular injection, reaching a maximum concentration after 8.40 days, with an elimination half-life of 9.94 days in rats. Histopathological observations revealed a granulomatous inflammatory response at the injection site 7 days after intramuscular administration, which significantly subsided by day 14 and showed minimal inflammation by day 28. These findings suggest that the nanosuspension system is a promising approach for the sustained release parenteral DTS delivery, with a protracted pharmacokinetic profile and tolerable local inflammation.
Keywords: dutasteride; nanocrystalline suspension; long-acting injectable; pharmacokinetics; histopathology dutasteride; nanocrystalline suspension; long-acting injectable; pharmacokinetics; histopathology

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MDPI and ACS Style

Jeong, M.Y.; Shin, D.M.; Kwon, M.K.; Shin, Y.B.; Park, J.S.; Yang, I.G.; Myung, J.H.; Lee, D.G.; Lee, G.Y.; Park, C.W.; et al. Design of Nanocrystalline Suspension of Dutasteride for Intramuscular Prolonged Delivery. Nanomaterials 2024, 14, 1781. https://doi.org/10.3390/nano14221781

AMA Style

Jeong MY, Shin DM, Kwon MK, Shin YB, Park JS, Yang IG, Myung JH, Lee DG, Lee GY, Park CW, et al. Design of Nanocrystalline Suspension of Dutasteride for Intramuscular Prolonged Delivery. Nanomaterials. 2024; 14(22):1781. https://doi.org/10.3390/nano14221781

Chicago/Turabian Style

Jeong, Min Young, Doe Myung Shin, Min Kyeong Kwon, Ye Bin Shin, Jun Soo Park, In Gyu Yang, Jin Hyuk Myung, Dong Geon Lee, Gi Yeong Lee, Chae Won Park, and et al. 2024. "Design of Nanocrystalline Suspension of Dutasteride for Intramuscular Prolonged Delivery" Nanomaterials 14, no. 22: 1781. https://doi.org/10.3390/nano14221781

APA Style

Jeong, M. Y., Shin, D. M., Kwon, M. K., Shin, Y. B., Park, J. S., Yang, I. G., Myung, J. H., Lee, D. G., Lee, G. Y., Park, C. W., Yeo, J. W., Ho, M. J., Choi, Y. S., & Kang, M. J. (2024). Design of Nanocrystalline Suspension of Dutasteride for Intramuscular Prolonged Delivery. Nanomaterials, 14(22), 1781. https://doi.org/10.3390/nano14221781

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