Fabrication of nanocrystal forms of ᴅ-cycloserine and their application for transdermal and enteric drug delivery systems.

Autor:	Tsai HA; Department of Research and Development, SyneuRx International (Taiwan) Corp., 20F-8, No. 99, Sec. 1, Xintai 5th Rd., Xizhi District, New Taipei City 221, Taiwan., Shih TM; Department of Research and Development, SyneuRx International (Taiwan) Corp., 20F-8, No. 99, Sec. 1, Xintai 5th Rd., Xizhi District, New Taipei City 221, Taiwan., Tsai T; Department of Research and Development, SyneuRx International (Taiwan) Corp., 20F-8, No. 99, Sec. 1, Xintai 5th Rd., Xizhi District, New Taipei City 221, Taiwan., Hu JW; Department of Research and Development, SyneuRx International (Taiwan) Corp., 20F-8, No. 99, Sec. 1, Xintai 5th Rd., Xizhi District, New Taipei City 221, Taiwan., Lai YA; Department of Research and Development, SyneuRx International (Taiwan) Corp., 20F-8, No. 99, Sec. 1, Xintai 5th Rd., Xizhi District, New Taipei City 221, Taiwan., Hsiao JF; Department of Research and Development, SyneuRx International (Taiwan) Corp., 20F-8, No. 99, Sec. 1, Xintai 5th Rd., Xizhi District, New Taipei City 221, Taiwan., Tsai GE; Department of Research and Development, SyneuRx International (Taiwan) Corp., 20F-8, No. 99, Sec. 1, Xintai 5th Rd., Xizhi District, New Taipei City 221, Taiwan.; Department of Psychiatry and Biobehavioral Sciences, UCLA School of Medicine, 10833 Le Conte Ave, Los Angeles, CA 90095, USA.
Jazyk:	angličtina
Zdroj:	Beilstein journal of nanotechnology [Beilstein J Nanotechnol] 2024 Apr 25; Vol. 15, pp. 465-474. Date of Electronic Publication: 2024 Apr 25 (Print Publication: 2024).
DOI:	10.3762/bjnano.15.42
Abstrakt:	ᴅ-cycloserine (DCS), an FDA-approved medicine for the treatment of tuberculosis, is also a partial agonist at the glycine recognition site of N -methyl-ᴅ-aspartate (NMDA) receptor and has shown significant treatment efficacy for central nervous system (CNS) disorders including depression, schizophrenia, Alzheimer's disease, and post-traumatic stress disorder. The physicochemical properties of DCS, however, limit the options of formulation and medicinal applications of DCS, and warrants further investigation for the development of CNS therapeutics. Nanocrystals play an important role in pharmaceutic design and development. The properties of nanocrystals are remarkably different from their bulk material counterpart, attributed to the large surface-area-to-volume ratio which can improve the bioavailability. In this study, for the first time, DCS, a highly water-soluble compound, has formed nanocrystals and this was confirmed by scanning electronic microscopy and X-ray powder diffraction. Furthermore, DCS nanocrystals were applied to several formulations to test their stability and then to the in vitro Franz diffusion test with reservoir patch formulation as well as in vivo pharmacokinetics study with enteric capsules. We tested these formulations regarding their nanocrystal physical properties, size effect, and dissolution rate, respectively. We found that DCS nanocrystals showed good performance in the Franz diffusion test and rodent pharmacokinetic studies due to the nanoparticle size and faster dissolution as compared with the commercial DCS powder. These DCS nanocrystal formulations could offer a new approach for the development of an advanced drug delivery system for the treatment of CNS disorders. (Copyright © 2024, Tsai et al.)
Databáze:	MEDLINE
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