Leveraging TRPV1 for intracellular delivery of membrane impermeant compounds in the brain

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Abstract
Large-pore ion channels present a window of opportunity for cell-specific intracellular drug delivery. Here, we demonstrate that the capsaicin receptor, TRPV1, can be used for delivery of the membrane impermeant lidocaine derivative QX-314 into neurons in the brain in vivo by using drug-induced hyperlocomotion as a behavioral readout and we validated our findings with ex vivo electrophysiological recordings. Our studies present evidence that this strategy can be used to deliver membrane impermeant compounds in the brain.
Funding Information
  • National Science Foundation (NSF GRFP 1937963)
  • National Institute on Drug Abuse (R01 DA040630)

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