Novel therapeutic nano-particles (lipocores): trapping poorly water soluble compounds

2'-(2-bromohexadecanoyl)-paclitaxel conjugate nanoparticles for the treatment of non-small cell lung cancer in an orthotopic xenograft mouse model

“…In the tubulin polymerization assay (Figure 2), Br-C16-PX at 10 µM exhibited a lower tubulin stabilization effect compared to PX at the same concentration presumably due to the modification of the 2′-OH group. [15][16][17] However, when the Br-C16-PX was increased to 34 µM, accelerated microtubule polymerization was observed similar to PX at 10 µM, indicating a tubulin stabilization effect of the conjugate.…”

“…Cytotoxicity of the Br-C16-PX NPs was investigated instead and results showed an IC 50 that was 62.2-fold higher than free PX, which is consistent with other reported 2′-PX conjugates. 9,[15][16][17] The lipid-based NPs with Br-C16-PX were optimized to have a drug loading as high as 40% (w/w, drug/oil) and a drug entrapment of 66.45%±0.02%. In contrast, previously reported PX BTM NPs and C22-PX BTM NPs had a drug loading of only 7.5% and 7.7% by weight, respectively, 18,19 likely due to relatively low affinity of PX to the Miglyol oil core in the PX BTM NPs or excess amount of surfactant in the C22-PX BTM NPs.…”

“…This was expected and consistent with other reported studies of 2′-PX conjugate since the 2′-OH group is crucial to the cytotoxicity and tubulin polymerization activity of PX. 9,[15][16][17] The blank NPs did not show significant cytotoxicity (drug equivalent IC 50 3080.5±406.6 nM), indicating some cytotoxic effect of the Br-C16-PX conjugate. …”

Pharmakotherapie mittels Nanomedizin

“…Ziel dieser Behandlungsansätze ist eine Opti mierung des lokalen therapeutischen Ef fektes. Durch Transportsysteme im na nopartikulären Maßstab werden darüber hinaus manche schwerlösliche oder insta bile Wirkstoffe überhaupt erst verfügbar gemacht [5].…”

Preparation, Characterization and Pharmacokinetics of Liposomes-Encapsulated Cyclodextrins Inclusion Complexes for Hydrophobic Drugs

“…Consequently, the administration of a large amount of carrier may be required to reach a therapeutic concentration (Perkins et al, 2000). Moreover, the stability of liposomes may be problematic because of the interaction between lipophilic drugs and lipid bilayers (Torchilin, 1985;Takino et al, 1994).…”