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- W3209743184 endingPage "1741" @default.
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- W3209743184 abstract "Critical adverse effects and frequent administration, three times per day, limit the use of flutamide (FLT) as a chemotherapeutic agent in the treatment of prostate cancer. Therefore, our research aimed to develop new cholesterol-based nanovesicles for delivering FLT to malignant cells in an endeavor to maximize its therapeutic efficacy and minimize undesired adverse effects. Draper-Lin small composite design was used to optimize the critical quality attributes of FLT-loaded niosomes and ensure the desired product quality. The influence of the selected four independent variables on mean particle size (Y1), zeta potential (Y2), drug entrapment efficiency (Y3), and the cumulative drug release after 24 h (Y4) was examined. The optimized nanovesicles were assessed for their in vitro cytotoxicity, ex-vivo absorption via freshly excised rabbit intestine as well as in vivo pharmacokinetics on male rats. TEM confirmed nanovescicles' spherical shape with bilayer structure. Values of dependent variables were 748.6 nm, -48.60 mV, 72.8% and 72.2% for Y1, Y2, Y3 and Y4, respectively. The optimized FLT-loaded niosomes exerted high cytotoxic efficacy against human prostate cancer cell line (PC-3) with an IC50 value of 0.64 ± 0.04 µg/mL whilst, it was 1.88 ± 0.16 µg/mL for free FLT. Moreover, the IC50 values on breast cancer cell line (MCF-7) were 0.27 ± 0.07 µg/mL and 4.07 ± 0.74 µg/mL for FLT-loaded niosomes and free FLT, respectively. The permeation of the optimized FLT-loaded niosomes through the rabbit intestine showed an enhancement ratio of about 1.5 times that of the free FLT suspension. In vivo pharmacokinetic study displayed an improvement in oral bioavailability of the optimized niosomal formulation with AUC and Cmax values of 741.583 ± 33.557 μg/mL × min and 6.950 ± 0.45 μg/mL compared to 364.536 ± 45.215 μg/mL × min and 2.650 ± 0.55 μg/mL for the oral FLT suspension. With these promising findings, we conclude that encapsulation of FLT in cholesterol-loaded nanovesicles enhanced its anticancer activity and oral bioavailability which endorse its use in the management of prostate cancer." @default.
- W3209743184 created "2021-11-08" @default.
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- W3209743184 date "2021-10-20" @default.
- W3209743184 modified "2023-09-30" @default.
- W3209743184 title "Cholesterol-Based Nanovesicles Enhance the In Vitro Cytotoxicity, Ex Vivo Intestinal Absorption, and In Vivo Bioavailability of Flutamide" @default.
- W3209743184 cites W1526743142 @default.
- W3209743184 cites W1966356719 @default.
- W3209743184 cites W1982887154 @default.
- W3209743184 cites W1987659508 @default.
- W3209743184 cites W1990137419 @default.
- W3209743184 cites W1990591974 @default.
- W3209743184 cites W1996219622 @default.
- W3209743184 cites W1996328211 @default.
- W3209743184 cites W2009300512 @default.
- W3209743184 cites W2013164488 @default.
- W3209743184 cites W2014325374 @default.
- W3209743184 cites W2019155896 @default.
- W3209743184 cites W2025061511 @default.
- W3209743184 cites W2026438690 @default.
- W3209743184 cites W2027913641 @default.
- W3209743184 cites W2028080874 @default.
- W3209743184 cites W2033547005 @default.
- W3209743184 cites W2038755095 @default.
- W3209743184 cites W2052129346 @default.
- W3209743184 cites W2053892140 @default.
- W3209743184 cites W2061078558 @default.
- W3209743184 cites W2061318069 @default.
- W3209743184 cites W2066432116 @default.
- W3209743184 cites W2081054963 @default.
- W3209743184 cites W2082511916 @default.
- W3209743184 cites W2084774646 @default.
- W3209743184 cites W2088550778 @default.
- W3209743184 cites W2090325980 @default.
- W3209743184 cites W2091254406 @default.
- W3209743184 cites W2098898775 @default.
- W3209743184 cites W2107946534 @default.
- W3209743184 cites W2114918609 @default.
- W3209743184 cites W2132528779 @default.
- W3209743184 cites W2140502432 @default.
- W3209743184 cites W2143298757 @default.
- W3209743184 cites W2144749910 @default.
- W3209743184 cites W2151467658 @default.
- W3209743184 cites W2158013415 @default.
- W3209743184 cites W2161530911 @default.
- W3209743184 cites W2162542854 @default.
- W3209743184 cites W2164043478 @default.
- W3209743184 cites W2167202145 @default.
- W3209743184 cites W2185007110 @default.
- W3209743184 cites W2207293016 @default.
- W3209743184 cites W2211575893 @default.
- W3209743184 cites W2235934048 @default.
- W3209743184 cites W2282102978 @default.
- W3209743184 cites W2295348757 @default.
- W3209743184 cites W2405475559 @default.
- W3209743184 cites W2435028564 @default.
- W3209743184 cites W2497385737 @default.
- W3209743184 cites W2515639740 @default.
- W3209743184 cites W2559878933 @default.
- W3209743184 cites W2580339592 @default.
- W3209743184 cites W2622199854 @default.
- W3209743184 cites W2788888547 @default.
- W3209743184 cites W2889000313 @default.
- W3209743184 cites W2902444563 @default.
- W3209743184 cites W2927115307 @default.
- W3209743184 cites W2999417355 @default.
- W3209743184 cites W3005731266 @default.
- W3209743184 cites W3027956142 @default.
- W3209743184 cites W3043376060 @default.
- W3209743184 cites W3096295208 @default.
- W3209743184 cites W3105117320 @default.
- W3209743184 cites W3118921680 @default.
- W3209743184 cites W3122028754 @default.
- W3209743184 cites W3136136801 @default.
- W3209743184 cites W3165052303 @default.
- W3209743184 cites W4253538779 @default.
- W3209743184 cites W757337304 @default.
- W3209743184 cites W950508456 @default.
- W3209743184 doi "https://doi.org/10.3390/pharmaceutics13111741" @default.
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- W3209743184 hasPublicationYear "2021" @default.
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