Chemical modification of drug molecules as strategy to reduce interactions with mucus.

Abstract:

:Many drug molecules possess inadequate physical-chemical characteristics that prevent to surpass the viscous mucus layer present in the surface of mucosal tissues. Due to mucus protective role and its fast turnover, these drug molecules end up being removed from the body before being absorbed and, thus, before exerting any physiologic affect. Envisaging a better pharmacokinetics profile, chemical modifications, to render drug a more mucopenetrating character, have been introduced to drug molecules backbone towards more effective therapies. Mucus penetration increases when drug molecules are provided with net-neutral charge, when they are conjugated with mucolytic agents and through modifications that makes them resistant to enzymes present in mucus, with the overall increase of their hydrophilicity and the decrease of their molecular weight. All of these characteristics act as a whole and influence each other so they must be well thought when drug molecules are being designed for mucosal delivery.

journal_name

Adv Drug Deliv Rev

authors

Araújo F,Martins C,Azevedo C,Sarmento B

doi

10.1016/j.addr.2017.09.020

subject

Has Abstract

pub_date

2018-01-15 00:00:00

pages

98-106

eissn

0169-409X

issn

1872-8294

pii

S0169-409X(17)30201-6

journal_volume

124

pub_type

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