Development of a weak-base docetaxel derivative that can be loaded into lipid nanoparticles.

@article{Zhigaltsev2010DevelopmentOA,
  title={Development of a weak-base docetaxel derivative that can be loaded into lipid nanoparticles.},
  author={Igor V. Zhigaltsev and Geoff Winters and Masuna Srinivasulu and Jason Crawford and Matthew Wong and Lawrence N. Amankwa and Dawn Waterhouse and Dana Masin and Murray S. Webb and Natashia Harasym and Lindsay Heller and Marcel Bally and Marco A Ciufolini and Pieter R Cullis and Norbert Maurer},
  journal={Journal of controlled release : official journal of the Controlled Release Society},
  year={2010},
  volume={144 3},
  pages={332-40}
}
Hydrophobic uncharged drugs such as docetaxel are difficult to encapsulate and retain in liposomal nanoparticles (LNP). In this work we show that a weak base derivative of docetaxel can be actively loaded into LNP using pH gradient loading techniques to achieve stable drug encapsulation and controlled release properties. Docetaxel was derivatized at the hydroxyl group in the C-2' position to form an N-methyl-piperazinyl butanoic acid ester. The free hydroxyl group in this position is essential… CONTINUE READING

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