Aerosolized Niosome Formulation Containing Gemcitabine and Cisplatin for Lung Cancer Treatment: Optimization, Characterization and In Vitro Evaluation

Abstract

Gemcitabine (Gem) and cisplatin (Cis) are currently being used for lung cancer treatment, but they are highly toxic in high dosages. This research aimed to develop a niosome formulation containing a low-dosage Gem and Cis (NGC), as an alternative formulation for lung cancer treatment. NGC was prepared using a very simple heating method and was further optimized by D-optimal mixture design. The optimum NGC formulation with particle size, polydispersity index (PDI), and zeta potential of 166.45 nm, 0.16, and −15.28 mV, respectively, was obtained and remained stable at 27 °C with no phase separation for up to 90 days. The aerosol output was 96.22%, which indicates its suitability as aerosolized formulation. An in vitro drug release study using the dialysis bag diffusion technique showed controlled release for both drugs up to 24 h penetration. A cytotoxicity study against normal lung (MRC5) and lung cancer (A549) cell lines was investigated. The results showed that the optimized NGC had reduced cytotoxicity effects against both MRC5 and A549 when compared with the control (Gem + Cis alone) from very toxic (IC50 < 1.56 µg/mL) to weakly toxic (IC50 280.00 µg/mL) and moderately toxic (IC50 = 46.00 µg/mL), respectively, after 72 h of treatment. These findings revealed that the optimized NGC has excellent potential and is a promising prospect in aerosolized delivery systems to treat lung cancer that warrants further investigation.

pH-Responsive, Adorned Nanoniosomes for Codelivery of Cisplatin and Epirubicin: Synergistic Treatment of Breast Cancer

“…Furthermore, synergistic effects of CIS in combination with anticancer drugs such as gemcitabine and paclitaxel have been investigated against breast cancer and other diseases. 15 , 60 , 61 Remarkably, as in our research, FPNCE yielded CIs lower than 1, which indicated synergism.…”

Fluorinated triazoles as privileged potential candidates in drug development—focusing on their biological and pharmaceutical properties

“…It has been reported that the incorporation of fluorine into this small molecule—triazole—imparts a significant enhancement to their biological activities in comparison to their non-fluorinated counterparts ( Langer et al, 2011 ; Ali et al, 2013 ), for instance, fluconazole and gemcitabine. Until now, modifications of the triazole moiety have proved to be highly effective with lesser toxicity and improved potency ( Mohamad Saimi et al, 2021 ).…”

Niosomes as Nano-carrier Based Targeted Drug Delivery System

“…The results revealed that the optimized formulation had reduced cytotoxicity against both MRC5 and A549 cell lines when compared with the control system (Gem + Cis alone) from highly toxic (IC50 < 1.56 µg/mL) to weakly toxic (IC50 280.00 µg/mL) and fairly toxic (IC50 = 46.00 µg/mL), respectively, after 72 h of treatment. These findings promised that the optimized aerosolized niosomal formulation has excellent anti-tumor activity and can be used as promising drug delivery system 7 .…”