Designing Highly Stable Poly(sarcosine)-Based Telodendrimer Micelles with High Drug Content Exemplified with Fulvestrant

Polymeric micelles have been extensively used as nanocarriers for the delivery of chemotherapeutic agents, aiming to improve their efficacy in cancer treatment. However, poor loading capacity, premature drug release, non-uniformity, and reproducibility still remain major challenges. To create a stable polymeric micelle with high loading, telodendrimer was developed nanocarrier fulvestrant, an example that has extremely water solubility (sub-nanomolar range). Telodendrimers were prepared by synthesis hydrophilic linear poly(sarcosine) growing lysine dendron from chain terminal amine divergent synthesis. At periphery dendritic block, either 4, 8, or 16 fulvestrant molecules conjugated creating hydrophobic block. Having part carrier not only reduces usage inert materials but also prevents drugs leakage release diffusion. The self-assembled demonstrated good colloidal stability (cmc < 2 μM) buffer uniform size. In addition, these could solubilize additional yielding excellent overall capacity up 77 wt % total load (summation encapsulated). Importantly, size be tuned between 25 150 nm controlling (i) ratio blocks (ii) amount encapsulated fulvestrant. versatility telodendrimer-based systems both efficiency stability, addition possessing other tuneable properties, makes it promising system range active pharmaceutical ingredients therapeutic targets.