作者: Igor Jigaltsev , Pieter Cullis , Marcel Bally , Marco Ciufolini , Norbert Maurer
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摘要: Drag derivatives are provided herein which suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the comprise a poorly water-soluble drag derivatized with weak-base moiety that facilitates active of through LN transmembrane pH or ion gradient aqueous interior LN. The can optionally lipophilic domain to inner monolayer membrane. Advantageously, formulations exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative corresponding free drags.