AI Article Synopsis
- Nanoemulsions (NE) are effective drug delivery systems that offer enhanced stability and efficacy for medications like docetaxel (DTX).
- The study aimed to formulate a safe and stable NE for DTX using various excipients, optimizing parameters like droplet size and drug release.
- The optimized NE formulation showed promising results, with high cell uptake and strong cytotoxic effects on cancer cells while demonstrating safety in animal tests, suggesting its potential as a viable alternative therapy for DTX.
Article Abstract
Context: Nanoemulsions (NE) are one of the robust delivery tools for drugs due to their higher stability and efficacy.
Objectives: The purpose of present investigation is to develop stable, effective and safe NE of docetaxel (DTX).
Methods: Soybean oil, lecithin, Pluronic F68, PEG 4000 and ethanol were employed as excipients and NEs were prepared by hot homogenization followed by ultra-sonication. NEs were optimized and investigated for different in vitro and in vivo parameters viz. droplet size, poly dispersity index, charge; zeta potential, drug content and in vitro drug release, in vitro cytotoxicity, in vitro cell uptake and acute toxicity. Transmission electron microscopy was performed to study morphology and structure of NEs. Stability studies of the optimized formulation were performed.
Results: Droplet size, poly dispersity index, zeta potential, drug content and in vitro drug release were found to be 233.23 ± 4.3 nm, 0.24 ± 0.010, -43.66 ± 1.9 mV, 96.76 ± 1.5%, 96.25 ± 2.1%, respectively. NE F11 exhibited higher cell uptake (2.83 times than control) and strong cytotoxic activity against MCF-7 cancer cells (IC50; 13.55 ± 0.21 µg/mL at 72 h) whereas no toxicity or necrosis was observed with liver and kidney tissues of mice at a dose of 20 mg/kg. Transmission electron microscopy ensured formation of poly-dispersed and spherical droplets in nanometer range. NE F11 (values indicated above) was selected as the optimized formulation based on the aforesaid parameters.
Conclusion: Conclusively, stable, effective and safe NE was developed which might be used as an alternative DTX therapy.
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| http://dx.doi.org/10.3109/10717544.2014.920430 | DOI Listing |
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