Abstract
Amphiphilic poly(esteracetal) micelles encapsulate potent immune modulatory drugs, but fall apart and release them upon dual pH or enzymatic stimuli.
Highlights
Delivering pharmaceutically active molecules to their specific therapeutic target by using nanosized carrier systems has attracted major interest to overcome current limitations of drug therapies.[1,2] Many hydrophobic drugs suffer from low solubility and unspecific binding which cause non-controllable toxicities.[3,4] This includes novel promising anticancer or immune therapeutics which accumulate insufficiently at their target sites
The structure of the product could be validated by 1H-NMR, 13C-NMR, COSY- and HSQC-NMR spectroscopy and the results are shown in Fig. S1– S4.† As we observed that MDO slowly degraded over time into 3-hydroxypropanoic acid and acetaldehyde, it was stored at −18 °C and always distilled freshly prior to use
By size exclusion chromatography (SEC) and by diffusion ordered spectroscopy (DOSY) NMR and MALDI-ToF MS analyses a distinct shift to higher molecular weights/slower diffusion species was achieved for all block copolymers, while signals of the remaining unmodified methoxy poly(ethylene glycol) (mPEG) macroinitiator were generally absent (Fig. S16, S19, S22 and S25†)
Summary
Delivering pharmaceutically active molecules to their specific therapeutic target by using nanosized carrier systems has attracted major interest to overcome current limitations of drug therapies.[1,2] Many hydrophobic drugs suffer from low solubility and unspecific binding which cause non-controllable toxicities.[3,4] This includes novel promising anticancer or immune therapeutics which accumulate insufficiently at their target sites As a result, their related off-target effects limit any clinical translatability. The acid-degradable acetal group ensures rapid carrier degradation and cargo release in acidic environments such as in immunosuppressive cancers and their draining lymph nodes, while the ester functionalities further enable long-term enzymatic carrier clearance from the body In this context, our work aims at providing first proof-of-concept studies on applying amphiphilic poly (esteracetal)s in immunodrug delivery. Our findings confirm the high potential of amphiphilic poly(esteracetal)s in immunodrug delivery and may contribute towards improving the translatability of further promising immunodrugs
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