Mohammadreza Ajdari - Nanomedicine and Nanobiology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
Aliyeh Ranjbar - Nanomedicine and Nanobiology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
Khashayar Karimian - Arasto Pharmaceutical Chemicals Inc., Yousefabad, Jahanarar Avenue, Tehran, Iran
Maryam Karimi - Nanomedicine and Nanobiology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
Hossein Heli - Nanomedicine and Nanobiology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
Naghmeh Sattarahmady - Nanomedicine 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 ۲۰® and Span ۸۰® and a thin film hydration method with DXL loading (DXL-Span۲۰ and DXL-Span۸۰). Characterization, in-vitro cytotoxicity and bioavailability of the nano-niosomes was also evaluated via in-vivo experiments. Results: DXL-Span۲۰ and DXL-Span۸۰ have vesicles size in a range of ۸۴-۹۰ nm and negative zeta potentials. DXL entrapment efficiencies were obtained as ۶۹.۶ and ۷۴.۰% for DXL-Span۲۰ and DXL-Span۸۰, respectively; with an in-vitro sustained release patterns. Cytotoxicity assays were performed against MDA-MB-۲۳۱, Calu-۶, and AsPC-۱ cell lines, and the results indicated that DXL loading into nano-niosomes led to decrement in values of half-maximal inhibitory concentration (IC۵۰) at least ۲.۵ times and at most ۶.۵ 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-Span۸۰ compared to DXL-Span۲۰.  Conclusion: Carrying DXL by the nano-niosomes led to enhanced cytotoxicity (and lower IC۵۰ values) and higher efficacy with enhanced pharmacokinetic parameters.

Docetaxel, Taxane, Taxotere®, Niosome, Sorbitan monolaurate, Drug delivery systems