Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers

摘要

A method for controlling the release of drugs or other passenger moleculars from carrier conjugates, and a class of conjugates that releases drugs when ingested by a cell or subjected to acidic conditions, are disclosed. These conjugates contain a passenger molecule which is attached to a spacer molecule through an acidic bonding group, such as carboxyl, that is in a "cis" configuration with another acidic group, and a carrier molecule that is bonded to the spacer molecule at another site. When subjected to a mile increase in acidity, such as occurs within a lysosome of a cell, the drug or other passenger molecule is hydrolyzed from the conjugate and released in unmodified, active form.