Platinum on Nanodiamond: A Promising Prodrug Conjugated with Stealth Polyglycerol, Targeting Peptide and Acid‐Responsive Antitumor Drug

Abstract

In the fi eld of nanomedicine, nanoparticles with various functions are required for in vivo applications such as biomedical imaging and drug delivery. Therefore, chemical functionalization of nanoparticles has been extensively investigated. Herein, nanodiamond (ND) coated with polyglycerol (PG) and its derivatives is reported to impart good solubility in a physiological environment, a stealth nature to avoid nonspecifi c uptake, a targeting property to be taken up by a specifi c cell, and an acid-responsive drug release property to kill cancer cells. ND is fi rst grafted with PG and the resulting ND-PG has a high solubility in physiological media. Since a large number of hydroxyl groups in PG provide scaffolds for further surface functionalization, the targeting RGD peptide and Pt-based drug are immobilized to give ND-PG-RGD, ND-PG-Pt and ND-PG-RGD-Pt. The ND with intrinsic fl uorescence is also functionalized by PG and RGD to confi rm cellular uptake and intracellular localization fl uorescently. The results of the cell experiments indicate that PG coating shielded fND from the uptake by HeLa and U87MG cells. In contrast, fND-PG-RGD is taken up by U87MG, not HeLa cells, exhibiting high targeting effi cacy. When ND-PG-RGD-Pt is applied, U87MG is selectively killed against HeLa. The multi-functional ND is a promising prodrug in targeting chemotherapy.

Polydopamine Encapsulation of Fluorescent Nanodiamonds for Biomedical Applications

“…[8] Due to their remarkable physicochemical properties, FNDs have been used in biomedical imaging, drug delivery, sensing, and bio-compatible composite materials. [9] …”

Affinity of Glycan‐Modified Nanodiamonds towards Lectins and Uropathogenic Escherichia Coli

“…Next to fullerene‐based glycoclusters, nanodiamonds (NDs) are emerging as particularly well‐suited for multivalent applications . Amongst the advantages of NDs over other carbon‐based materials is that they are completely inert, optically transparent, biocompatible, have the ability to emit light, and can be functionalized in many ways depending on their intended ultimate application . Although in vivo toxicity of nanoparticles is dependent on specific surface characteristics , ND particles did not induce significant cytotoxicity in a variety of cell lines and were used in various biomedical applications …”

Nanodiamonds and Their Applications in Cells

“…Zhao et al used a multifunctional approach to deliver a cancer drug . The functional pieces were polyglycerol (PG) to provide good solubility in aqueous media, RGD peptide (tripeptide Arg‐Gly‐Asp a peptide sequence leading to cell attachment) for targeting and an acid responsive antitumor Pt‐based drug.…”