Abstract
The aim of this study is to investigate using nanoemulsion formulations as drug-delivery vehicles of paclitaxel (PX), a poor water-soluble anticancer drug. Two commercially available nanoemulsion fat formulations (Clinoleic 20% and Intralipid 20%) were loaded with PX and characterised based on their size, zeta potential, pH and loading efficiency. The effect of formulation on the cytotoxicity of PX was also evaluated using MTT assay.The droplet size of the Clinoleic emulsion increased from 254.1nm to 264.7nm when paclitaxel (6mg/ml) was loaded into the formulation, compared to the drug-free formulation. Similarly, the droplet size of Intralipid increased from 283.3 to 294.6nm on inclusion of 6mg/ml paclitaxel. The Polydispersity Indexes (PDIs) of all the nanoemulsion formulations (Clinoleic and Intralipid) were less than 0.2 irrespective of paclitaxel concentration indicating that all nanoemulsion formulations used were homogeneously sized. The pH range for the Clinoleic formulations (7.1–7.5) was slightly higher than that of the Intralipid formulations (6.5–6.9). The zeta potential of linoleic had a greater negative value than that of Intralipid.Loading efficiencies for paclitaxel were 70.4–80.2% and 44.2–57.4% for Clinoleic and Intralipid formulations, respectively. Clinoleic loaded with paclitaxel decreased the viability of U87-MG cell to 6.4±2.3%, compared to Intralipid loaded with paclitaxel (21.29±3.82%). Both nanoemulsions were less toxic to the normal glial cells (SVG-P12), decreasing the cell viability to 25–35%. This study suggests that nanoemulsions are useful and potentially applicable vehicles of paclitaxel for treatment of glioma.
Highlights
Paclitaxel (PX) is widely used for its anticancer activity against ovarian carcinoma, head and neck cancers, breast cancer, lung cancer and AIDS related Kaposi’s sarcoma (Rowinsky and Donehower, 1995)
Clinical trials have demosnstrated that Abraxane1, a formulation of paclitaxel loaded onto albumin nanoparticles can provide enhanced penetration of the anticancer drug in the tumour by 33% compared to Taxol1 (Garber, 2004)
The Polydispersity Index (PI) results indicated that all the nanoemulsion formulations (Clinoleic and Intralipid) were homogeneous, regardless of paclitaxel concentration in the emulsions
Summary
Paclitaxel (PX) is widely used for its anticancer activity against ovarian carcinoma, head and neck cancers, breast cancer, lung cancer and AIDS related Kaposi’s sarcoma (Rowinsky and Donehower, 1995). The commercially established formulation of Cremophor EL-based paclitaxel is “Taxol1”. This formulation causes serious toxic effects such as nephrotoxicity, hypersensitivity reactions, neurotoxicity, laboured breathing, hypotension and lethargy (Singla et al, 2002). Clinical trials have demosnstrated that Abraxane, a formulation of paclitaxel loaded onto albumin nanoparticles can provide enhanced penetration of the anticancer drug in the tumour by 33% compared to Taxol (Garber, 2004).
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