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Characterization and Evaluation of Nano-niosomes Encapsulating Docetaxel against Human Breast, Pancreatic, and
Mohammadreza Ajdari1, Aliyeh Ranjbar1, Khashayar Karimian2
1Nanomedicine and Nanobiology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.
Background:
Docetaxel (DXL) is an antineoplastic agent for cancer treatment, the therapeutic efficiency of which is limited due to low solubility, hydrophobicity, and tissue specificity.
Objective:
In this study, nano-niosomes were introduced for improving therapeutic index of DXL.
Material And Methods:
In this experimental study, two nano-niosomes were synthesized using Span 20® and Span 80® and a thin film hydration method with DXL loading (DXL-Span20 and DXL-Span80). Characterization, in-vitro cytotoxicity and bioavailability of the nano-niosomes was also evaluated via in-vivo experiments.
Results:
DXL-Span20 and DXL-Span80 have vesicles size in a range of 84-90 nm and negative zeta potentials. DXL entrapment efficiencies were obtained as 69.6 and 74.0% for DXL-Span20 and DXL-Span80, respectively; with an in-vitro sustained release patterns. Cytotoxicity assays were performed against MDA-MB-231, Calu-6, and AsPC-1 cell lines, and the results indicated that DXL loading into nano-niosomes led to decrement in values of half-maximal inhibitory concentration (IC50) at least 2.5 times and at most 6.5 times, compared to free DXL. Moreover, the rat blood bioavailability of DXL after intraperitoneal administration and the pharmacokinetic parameters indicated higher DXL plasma level and the higher effectiveness of DXL-Span80 compared to DXL-Span20.
Conclusion:
Carrying DXL by the nano-niosomes led to enhanced cytotoxicity (and lower IC50 values) and higher efficacy with enhanced pharmacokinetic parameters.
Insights
Nano-niosomes improved docetaxel (DXL) cancer therapy by enhancing its effectiveness and reducing toxicity. These nanocarriers significantly boosted DXL
Area of Science:
- Nanotechnology
- Pharmaceutical Sciences
- Drug Delivery
Background:
- Docetaxel (DXL) is an antineoplastic agent with limited therapeutic efficiency due to poor solubility and specificity.
- Addressing DXL's limitations is crucial for improving cancer treatment outcomes.
Purpose of the Study:
- To enhance the therapeutic index of docetaxel (DXL) by formulating it into nano-niosomes.
- To evaluate the physicochemical properties, in-vitro cytotoxicity, and in-vivo bioavailability of DXL-loaded nano-niosomes.
Main Methods:
- Two types of nano-niosomes were synthesized using Span 20® and Span 80® via thin film hydration.
- Docetaxel (DXL) was loaded into the nano-niosomes (DXL-Span20 and DXL-Span80).
- Characterization, in-vitro cytotoxicity assays, and in-vivo pharmacokinetic studies in rats were performed.
Main Results:
- Nano-niosomes exhibited vesicle sizes of 84-90 nm and negative zeta potentials.
- DXL entrapment efficiencies were 69.6% (DXL-Span20) and 74.0% (DXL-Span80), with sustained in-vitro release.
- DXL-loaded nano-niosomes demonstrated significantly lower IC50 values (2.5-6.5 times) against cancer cell lines compared to free DXL.
- In-vivo studies showed enhanced DXL bioavailability and plasma levels, with DXL-Span80 being more effective.
Conclusions:
- Nano-niosomes effectively improved docetaxel's (DXL) cytotoxicity and pharmacokinetic profile.
- Formulating DXL into nano-niosomes enhances its therapeutic potential for cancer treatment.
- Span 80-based nano-niosomes showed superior efficacy compared to Span 20-based ones.
