Paclitaxel-Nanodiamond Nanocomplexes Enhance Aqueous Dispersibility and Drug Retention in Cells

Dae Gon Lim, Joo Hyun Jung, Hyuk Wan Ko, Eunah Kang, Seong Hoon Jeong

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34 Citations (Scopus)


Nanodiamonds (NDs) with 5 nm crystalline structures have been recognized as emerging carbon delivery vehicles due to their biocompatible inertness, high surface-to-volume ratio, and energy absorbance properties. In this study, carboxylated nanodiamond (ND-COOH) was reduced to hydroxylated nanodiamond (ND-OH) for stable and pH-independent colloidal dispersity. The poorly water-soluble paclitaxel (PTX) was physically loaded into ND-OH clusters, forming amorphous PTX nanostructure on the interparticle nanocage of the ND substrate. Stable physical PTX loading onto the ND substrate with stable colloidal stability showed enhanced PTX release. ND-OH/PTX complexes retained the sustained release of PTX by up to 97.32% at 70 h, compared with the 47.33% release of bare crystalline PTX. Enhanced PTX release from ND substrate showed low cell viability in Hela, MCF-9, and A549 cancer cells due to sustained release and stable dispersity in a biological aqueous environment. Especially, the IC50 values of ND-OH/PTX complexes and PTX in Hela cells were 0.037 μg/mL and 0.137 μg/mL, respectively. Well-dispersed cellular uptake of suprastructure ND-OH/PTX nanocomplexes was directly observed from the TEM images. ND-OH/PTX nanocomplexes assimilated into cells might provide convective diffusion with high PTX concentration, inducing initial necrosis. This study suggests that poorly water-soluble drugs can be formulated into a suprastructure with ND and acts as a highly concentrated drug reservoir directly within a cell.

Original languageEnglish
Pages (from-to)23558-23567
Number of pages10
JournalACS Applied Materials and Interfaces
Issue number36
Publication statusPublished - 2016 Sep 14

Bibliographical note

Funding Information:
This research was supported by the Bio & Medical Technology Development Program of the NRF, funded by the Korean government, MSIP (NRF-2014M3A9A9073811), and Basic Science Research Program through the National Research Foundation of Korea(NRF), funded by the Ministry of Science, CT and Future Planning (NRF-2015R1C1A2A01053307)

Publisher Copyright:
© 2016 American Chemical Society.

All Science Journal Classification (ASJC) codes

  • Materials Science(all)


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