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Abstract To overcome the drug resistance in MCF7 cancer cells and enhance their sensitivity to cisplatin, a liposomal (Lip) nanocarrier modified by arginine-glycine-aspartic acid (RGD) to co-deliver cisplatin (Cis) and miRNA biomolecule (miR-34a) was investigated. The efficiency of this nanocarrier was evaluated through in vitro and in vivo assays against MCF7 and 4T1 cells, respectively. The in vitro results demonstrated that the miR34a-Cis-Lip-RGD formulation had significantly higher efficiency and also a higher apoptotic effect compared to both miR34a-Cis and miR34a-Cis-Lip (76.24%, 58.29%, and 56.2%, respectively). Additionally, miR34a-Cis-Lip exhibited an overall CI value below 1, indicating a synergistic effect of Cis and miR-34a within the Lip system. The miR34a-Cis-Lip-RGD increased the Bax gene expressions compared to both miR34a-Cis-Lip and Cis-miR34a, possibly due to the integrin receptors on the cells, leading to higher uptake. The efficiency of miR34a-Cis-Lip-RGD in reducing tumor size was significantly higher than Cis-miR34a and miR34a-Cis-Lip. The lower volume of the tumor in the group treated with Cis-miR34a-Lip-RGD is presumed to be attributed to improved cellular uptake facilitated by the RGD modification, which enhances the targeted delivery of the therapeutic payload to cancer cells. The overall weight of the mice in all the groups did not exhibit significant changes. This consistent weight maintenance implies the safety of the designed delivery system for vital organs, indicating that the designed delivery system may offer a promising solution to minimize unwanted side effects associated with conventional cancer treatments.

Background: Quercetin is a flavonoid having anti-cancer properties; however, it has low stability, insufficient bioavailability, and poor solubility. This study aimed to load quercetin on nanoliposomes to enhance its efficiency against SW48 colorectal cancer cells. The cytotoxicity of free-quercetin and quercetin-loaded nanoliposomes on the expression of the epidermal growth factor receptor (EGER) gene was investigated. Methods: This present in vitro study was conducted at Yasuj University of Medical Sciences (Yasuj, Iran) in 2021. In this in vitro study, the lipid thin-film hydration method was used to synthesize quercetin-loaded liposomes. Additionally, high-performance liquid chromatography (HPLC) analyses, dynamic light scattering (DLS), and transmission electron microscopy (TEM) investigations were used to characterize nanomaterials. Following that, MTT, flow cytometry, and real-time PCR were used to investigate the cytotoxicity of quercetin-loaded liposomes on the colorectal cancer cells SW48 cell line, the incidence of apoptosis, and the expression of the EGFR gene in these cells. Statistical analysis was performed using the SPSS (version 26.0), and the graphs were created with the GraphPad Prism version 8.4.3. P

Curcumin is one of the natural anticancer drugs but its efficiency is limited by low stability, insufficient bioavailability, poor solubility, and poor permeability. Dorema aucheri (Bilhar) is a herb with precious pharmaceutical properties. This study aimed to develop a nanoliposome-based curcumin and Bilhar extract codelivery system. The nanocompounds were synthesized using the lipid thin-film hydration method and characterized by transmission electron microscopy, and dynamic light scattering techniques, and their cytotoxicity and apoptotic effect on the primary oral cancer cell line were evaluated via 2,5-diphenyl-2H-tetrazolium bromide assay and flow cytometry. Moreover, the expression of the epidermal growth factor receptor (EGFR) gene in the treated cells was assessed using the real-time polymerase chain reaction technique. Based on the results, nanoliposomes had a size of 91 ± 10 nm with a polydispersity index of 0.13. Free curcumin, the extract, and the curcumin-extract combination showed dose-dependent toxicity against cancer cells; yet, the extract (IC50: 86 µg/ml) and curcumin-extract (IC50: 65 µg/ml) activities were much more than curcumin (IC50: 121 µg/ml). Also, the curcumin and extract loaded on liposomes showed a dose and time-dependent cytotoxicity. After loading the curcumin-extract compound on nanoliposomes, their IC50 decreased from 180 µg/ml (within 24 hr) to 43 µg/ml (within 72 hr), indicating their sustainable release and activity. Likewise, this compound induced the highest apoptosis percentage (95%) in cancerous cells and inhibited the expression of the EGFR gene in the cells by 81% ± 3%. These findings demonstrated the effectiveness of the Bilhar extract against oral cancer cells. Also, in combination with curcumin, it showed an additive activity that considerably improved after loading on nanoliposomes.