Peptide drug modifications to enhance bioavailability and blood-brain barrier permeability.

Abstract:

:Peptides have the potential to be potent pharmaceutical agents for the treatment of many central nervous system derived maladies. Unfortunately peptides are generally water-soluble compounds that will not enter the central nervous system, via passive diffusion, due to the existence of the blood-brain barrier. Peptides can also undergo metabolic deactivation by peptidases, thus further reducing their therapeutic benefits. In targeting peptides to the central nervous system consideration must be focused both on increasing bioavailability and enhancing brain uptake. To date multiple strategies have been examined with this focus. However, each strategy comes with its own complications and considerations. In this review we assess the strengths and weaknesses of many of the methods currently being examined to enhance peptide entry into the central nervous system.

journal_name

Peptides

journal_title

Peptides

authors

Witt KA,Gillespie TJ,Huber JD,Egleton RD,Davis TP

doi

10.1016/s0196-9781(01)00537-x

subject

Has Abstract

pub_date

2001-12-01 00:00:00

pages

2329-43

issue

12

eissn

0196-9781

issn

1873-5169

pii

S019697810100537X

journal_volume

22

pub_type

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