Intranasal administration of liposomes: Potential brain delivery with prospective ophthalmic reach

• Published in: Journal of drug delivery science and technology Vol. 101; p. 106254
• Main Authors: Tsuji, Shohei, Hatano, Riku, Nakamura, Shinsuke, Kudo, Urara, Aoshima, Kota, Fujimori, Honoka, Takagi, Yuya, Obayashi, Mayuna, Ito, Takaaki, Yamazoe, Eriko, Kuse, Yoshiki, Otsu, Wataru, Shimazawa, Masamitsu, Tahara, Kohei
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.11.2024
• Subjects: Central nervous system (CNS); Intranasal administration; Liposome; Nose-to-brain; Liposome; Intranasal administration; Central nervous system (CNS); Nose-to-brain
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2024.106254

The low efficacy of drug transportation from the bloodstream to specific tissues remains a challenge in drug delivery to the central nervous system (CNS), primarily because of the presence of the blood-brain and blood-retinal barriers. There is a need for non-invasive drug delivery techniques to the CNS given the intrusive nature of and potential patient burden associated with intraventricular, intrathecal, and intravitreal administration. Recently, the focus has shifted towards intranasal (i.e., nose-to-brain) drug delivery. Furthermore, there have been reports indicating that the use of drug nanocarriers, such as liposomes, facilitates efficient drug delivery via the intranasal pathway. This study investigates the brain penetration capabilities of intranasally administered liposomes using the hydrophobic fluorescent molecule, 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl lindodicarbocyanine, 4-chlorobenzene sulfonate salt (DiD), as a model compound. The primary objective of this study was to elucidate the penetration of intranasally administered liposomes into the CNS, including the eyes. An examination of DiD distribution in the dissected brain and ocular tissues showed that DiD concentrations were elevated specifically at the limbus of the ocular tissue when surface-modified liposomes were employed. These findings suggest that intranasal liposome administration can deliver drugs to the posterior ophthalmic region, specifically the optic nerve, in addition to the brain. This figure was created using BioRender.com. [Display omitted]