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Design, synthesis, and neuroprotective effects of dual‐brain targeting naproxen prodrug
Author(s) -
Wang Linhui,
Zhang Li,
Zhao Yi,
Fu Qiuyi,
Xiao Wenjiao,
Lu Runxin,
Hai Li,
Guo Li,
Wu Yong
Publication year - 2018
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201700382
Subject(s) - prodrug , naproxen , ascorbic acid , chemistry , neuroprotection , pharmacology , in vivo , drug , biochemistry , medicine , biology , alternative medicine , food science , microbiology and biotechnology , pathology
A new dual‐targeting naproxen prodrug conjugated with glucose and ascorbic acid for central nervous system (CNS) drug delivery was designed and synthesized in order to effectively deliver naproxen to the brain. Naproxen could be released from the prepared prodrugs when incubated with various buffers, mouse plasma, and brain homogenate. Also, the prodrug showed superior neuroprotective effect in vivo over naproxen. Our results suggest that chemical modification of therapeutics with warheads of glucose and ascorbic acid represents a promising and efficient strategy for the development of brain targeting prodrugs by utilizing the endogenous transportation mechanism of the warheads.