| abstract |
A drug derivative suitable for loading into a liposomal nanoparticle carrier is provided herein. In some preferred aspects, the derivative comprises a poorly water-soluble drug derivatized with a weak base moiety which facilitates the active loading of the drug into the LN aqueous interior through trans-membrane pH or ionic gradient of LN. The weak base moiety may optionally comprise a lipophilic domain that facilitates the active loading of the drug into the inner monolayer of the liposome membrane. Advantageously, the LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy and / or other advantages over the corresponding free drug. |