Abstract
The development of effective strategies for local administration of chemotherapeutic drugs, thus minimizing the adverse side effects to patients, is one of the key challenges in biomedicine and cancer research. This work reports the formulation and characterization of PluronicF127 microemulsions to enhance the bioavailability of Cisplatin (Cis). The size of Cis microemulsion was about 12.0 nm, as assessed by dynamic light scattering analysis. In vitro cytotoxic activity of free Cis and F127/Cis microemulsions were studied on malignant (C152 and MCF7) and normal (HUVEC) cells via tetrazolium (MTT) colorimetric assay. Cell morphology was also monitored. In vitro assessments revealed thatF127/Cis microemulsions induced cytotoxicity/morphological changes to a lesser extent than free Cis. Regarding in vivo experiments, F127/Cis microemulsions were injected intraperitoneally at 7 and 14 mg/kg doses into adult male Wistar rats to assess histologic and biochemical changes. In this case, the bulk Cis group caused severe histopathological changes and significant increases in serum liver enzymes and serum kidney function markers. The group treated with the 14 mg/kg dose of F127/Cis microemulsions also showed severe fatty changes and significant increases in serum liver enzymes, blood urea nitrogen, and creatinine levels. The group treated with the low dose of nano-Cis showed a significant increase in serum liver enzymes levels accompanied by mild fatty changes of the liver. Theoretical surveys were performed to get an understanding of the interplay between F127 and Cis. Results reveal that hydrogen bonding (HB) interactions with F127have an influence on the molecular properties of Cis and may playa role in the lower toxicity of F127/Cis in comparison to free Cis.
Highlights
Cisdiamminedichloroplatinum (II), commonly known as Cisplatin (Cis), is a platinum coordinate compound that is highly soluble in water and soluble in N,N-dimethylformamide, and dimethylprimanide [1]
Free Cis significantly decreased the viability of MCF7 and C152 cells in a concentration-dependent manner (p < 0.05)
The same pattern, but to a lesser extent, was observed when HUVECs were treated with increasing concentrations of free Cis
Summary
Cisdiamminedichloroplatinum (II), commonly known as Cisplatin (Cis), is a platinum coordinate compound that is highly soluble in water and soluble in N,N-dimethylformamide, and dimethylprimanide [1]. It acquired FDA approval in 1978 for the treatment of testicular and ovarian cancer. Cis has been extensively used in clinical studies, but the mechanism of internalization in cancer cells remains ambiguous. The traditional chemotherapeutic drug delivery approaches suffer from the off-site drug accumulation at the desired site. This often leads to organ toxicity [8]
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