An effective strategy for development of docetaxel encapsulated gold nanoformulations for treatment of prostate cancer.

Nanoformulation based drug delivery is one of the most important research areas in the field of nanomedicine, which provides promising alternatives to the limitations of conventional chemotherapy. Nano drug delivery enables improved pharmacokinetic profile, bioavailability and therapeutic efficiency compared to the regular chemotherapeutic drugs. Herein, we have established a simple method for the synthesis of docetaxel (Dtx) encapsulated poly (ethylene glycol) (PEG) functionalized gold nanoparticles (AuNPs) for targeted drug delivery to prostate cancer. AuNPs were synthesized by the citrate ion reduction method followed by functionalization with thiol-PEG-amine (SH-PEG-NH2). SH-PEG-NH2 functionalized AuNPs were conjugated with the targeting vehicle, folic acid (FA). The anticancer drug, Dtx was encapsulated within AuNPs by the non-covalent linkage method. The physicochemical characteristics of the synthesized nanoformulations were extensively characterized by various spectral and microscopic studies. HR-TEM indicates the average size of the AuNPs is 16 nm and the nanoformulations is 18 nm. The encapsulation efficiency of the Dtx is ~ 96% which is confirmed by the elemental mapping analysis. The in vitro drug release profile of Dtx and AuNPs nanoformulations were studied by the dialysis membrane method. The anticancer activity of docetaxel encapsulated AuNPs were evaluated with prostate cancer cell lines (PC3). The drug encapsulated nanoformulations reduced the cell viability to about 40% (40 µM concentration at 24, 48 and 72 h of treatment). The optical microscopy observation reveals that the damage of prostate cancer cells after exposure to Dtx encapsulated AuNPs. The good cytotoxic activity of the present nanoformulation against prostate cancer cell lines enables its application for targeted drug delivery to prostate cancer.

Evaluation of cytotoxic activity of docetaxel loaded gold nanoparticles for lung cancer drug delivery.

The effective use of the gold nanoparticle (AuNPs) conjugated drugs for targeted drug delivery applications is one of the most promising research areas in the field of cancer. Herein, we aimed to establish a nano drug conjugated with docetaxel as a possible therapy option. Gold nanoparticles were synthesized by chemical reduction method. This is followed by the conjugation with an anticancer drug, docetaxel (Dtx) by a non-covalent method and folic acid (FA) was conjugated by a covalent method. The physicochemical characteristics of the synthesized AuNPs, Dtx and FA were studied by various analytical techniques such as UV-vis spectroscopy (UV-vis), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), Raman spectroscopy, X-ray photoelectron spectroscopy (XPS), field emission scanning electron microscope (FE-SEM) high-resolution transmission electron microscope (HR-TEM) and energy dispersive X-ray spectroscopy (EDS). The surface morphology and microstructure of the synthesized AuNPs and gold conjugates (AuNPs-Dtx-FA) were examined by FESEM and HR-TEM. The average size of the spherical shaped AuNPs was observed in the range of 5-18 nm. XPS and EDS spectra were examined the oxidation state and chemical composition of the synthesized nanoparticles. The cytotoxicity of the synthesized AuNPs nano-conjugates was evaluated by in-vitro studies against lung cancer cell line (H520). The chemical reduction method followed here in the development of AuNPs is a simple and one-step process, which exhibits the excellent binding specificity, biocompatibility and feasible for the large scale up process of the AuNPs.