Safe and Efficient Intracellular Release of SN38 via Lysosomal-Responsive SN38-G Loaded Liposomes.

ABSTRACT: Liposomal formulations remain mostly suited for amphiphilic drugs of mild potency. This high selectivity challenges the formulation of potent chemotherapeutics that are preponderantly hydrophobic. Spontaneous accumulation of certain hydrophobic drugs within the lipid bilayer of liposomes leads to aggregation, destabilization, and inadequate drug retention. Here, we depict an alternative approach to load such hydrophobic drugs using SN38, the active form of CPT-11 (Irinotecan, Camptosar), through SN38 glucuronide (SN38-G), its hydrophilic glucuronide prodrug derivative. SN38-G was esterified in acidic methanol or ethanol to produce amphiphilic derivatives SN38-G^met and SN38-G^eth compatible with liposomal core encapsulation. By employing an internally alkaline pH, core-

SUBMITTER: Burnouf PA 

PROVIDER: S-EPMC12284848 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature