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Docetaxel-loaded pluronic p123 polymeric micelles: in vitro and in vivo evaluation.

Liu Z, Liu D, Wang L, Zhang J, Zhang N - Int J Mol Sci (2011)

Bottom Line: In this work, novel docetaxel (DTX) -loaded Tween 80-free Pluronic P123 (P123) micelles with improved therapeutic effect were developed.The DTX-micelles were spherical with a mean particle size of 50.7 nm and size distribution from 22 to 84 nm, which suggested that they should be able to selectively accumulate in solid tumors by means of EPR effect, with a zeta potential of -12.45 ± 3.24 mV.These results suggested that P123 micelles might be considered as an effective DTX delivery system.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Science, Shandong University, 44 Wenhua Xi Road, Ji'nan 250012, Shandong, China.

ABSTRACT
In this work, novel docetaxel (DTX) -loaded Tween 80-free Pluronic P123 (P123) micelles with improved therapeutic effect were developed. The freeze-dried DTX-loaded P123 micelles (DTX-micelles) were analyzed by HPLC, TEM and DLS to determine the DTX loading, micelle morphology, size, respectively. The in vitro cytotoxic activity of DTX-micelles in HepG2, A549 and malignant melanoma B16 cells were evaluated by MTT assay. The corresponding in vivo antitumor efficacy was assessed in Kunming mice bearing B16 tumor after intravenous administration. The DTX-loading and efficiency into the micelles were 2.12 ± 0.09% and 86.34 ± 3.32%, respectively. The DTX-micelles were spherical with a mean particle size of 50.7 nm and size distribution from 22 to 84 nm, which suggested that they should be able to selectively accumulate in solid tumors by means of EPR effect, with a zeta potential of -12.45 ± 3.24 mV. The in vitro release behavior of DTX from DTX-micelles followed the Weibull equation. Compared with Duopafei(®), DTX-micelles showed higher cytotoxicity against HepG2 (P < 0.01), A549 (P < 0.05) and B16 (P < 0.01) cells. In addition, DTX-micelles exhibited remarkable antitumor activity and reduced toxicity on B16 tumor in vivo. The tumor inhibition rates (TIR) of DTX-micelles was 91.6% versus 76.3% of Duopafei(®) (P < 0.01). These results suggested that P123 micelles might be considered as an effective DTX delivery system.

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The in vivo antitumor effect of DTX-micelles. (A) the changes of tumor volumes of the tested groups; (B) the typical photographs of excised sarcomas from the tested groups; (C) the weights of excised tumor mass; (D) the variation of relative body weight of the mice with time. * P < 0.05, ** P < 0.01 versus Duopafei®.
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f4-ijms-12-01684: The in vivo antitumor effect of DTX-micelles. (A) the changes of tumor volumes of the tested groups; (B) the typical photographs of excised sarcomas from the tested groups; (C) the weights of excised tumor mass; (D) the variation of relative body weight of the mice with time. * P < 0.05, ** P < 0.01 versus Duopafei®.

Mentions: The in vivo antitumor effect of DTX-micelles was assessed by intravenous administration using Kunming mice bearing B16 tumor as the model animals. The treatments were injected via the tail vein once a week for three weeks. Figure 4A shows changes of tumor volumes. It was found that the tumor volumes of DTX-micelles group were smaller than those of Duopafei® group, indicating that DTX-micelles might more effectively inhibit tumor growth. It should be noted that the difference in tumor volumes among the groups of DTX-micelles and blank micelles as well as saline was highly significant (P < 0.01). Figure 4B shows typical photographs of excised sarcomas from the tested groups, which provide a direct visual representation of the tumor-suppression effect.


Docetaxel-loaded pluronic p123 polymeric micelles: in vitro and in vivo evaluation.

Liu Z, Liu D, Wang L, Zhang J, Zhang N - Int J Mol Sci (2011)

The in vivo antitumor effect of DTX-micelles. (A) the changes of tumor volumes of the tested groups; (B) the typical photographs of excised sarcomas from the tested groups; (C) the weights of excised tumor mass; (D) the variation of relative body weight of the mice with time. * P < 0.05, ** P < 0.01 versus Duopafei®.
© Copyright Policy - open-access
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC3111627&req=5

f4-ijms-12-01684: The in vivo antitumor effect of DTX-micelles. (A) the changes of tumor volumes of the tested groups; (B) the typical photographs of excised sarcomas from the tested groups; (C) the weights of excised tumor mass; (D) the variation of relative body weight of the mice with time. * P < 0.05, ** P < 0.01 versus Duopafei®.
Mentions: The in vivo antitumor effect of DTX-micelles was assessed by intravenous administration using Kunming mice bearing B16 tumor as the model animals. The treatments were injected via the tail vein once a week for three weeks. Figure 4A shows changes of tumor volumes. It was found that the tumor volumes of DTX-micelles group were smaller than those of Duopafei® group, indicating that DTX-micelles might more effectively inhibit tumor growth. It should be noted that the difference in tumor volumes among the groups of DTX-micelles and blank micelles as well as saline was highly significant (P < 0.01). Figure 4B shows typical photographs of excised sarcomas from the tested groups, which provide a direct visual representation of the tumor-suppression effect.

Bottom Line: In this work, novel docetaxel (DTX) -loaded Tween 80-free Pluronic P123 (P123) micelles with improved therapeutic effect were developed.The DTX-micelles were spherical with a mean particle size of 50.7 nm and size distribution from 22 to 84 nm, which suggested that they should be able to selectively accumulate in solid tumors by means of EPR effect, with a zeta potential of -12.45 ± 3.24 mV.These results suggested that P123 micelles might be considered as an effective DTX delivery system.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Science, Shandong University, 44 Wenhua Xi Road, Ji'nan 250012, Shandong, China.

ABSTRACT
In this work, novel docetaxel (DTX) -loaded Tween 80-free Pluronic P123 (P123) micelles with improved therapeutic effect were developed. The freeze-dried DTX-loaded P123 micelles (DTX-micelles) were analyzed by HPLC, TEM and DLS to determine the DTX loading, micelle morphology, size, respectively. The in vitro cytotoxic activity of DTX-micelles in HepG2, A549 and malignant melanoma B16 cells were evaluated by MTT assay. The corresponding in vivo antitumor efficacy was assessed in Kunming mice bearing B16 tumor after intravenous administration. The DTX-loading and efficiency into the micelles were 2.12 ± 0.09% and 86.34 ± 3.32%, respectively. The DTX-micelles were spherical with a mean particle size of 50.7 nm and size distribution from 22 to 84 nm, which suggested that they should be able to selectively accumulate in solid tumors by means of EPR effect, with a zeta potential of -12.45 ± 3.24 mV. The in vitro release behavior of DTX from DTX-micelles followed the Weibull equation. Compared with Duopafei(®), DTX-micelles showed higher cytotoxicity against HepG2 (P < 0.01), A549 (P < 0.05) and B16 (P < 0.01) cells. In addition, DTX-micelles exhibited remarkable antitumor activity and reduced toxicity on B16 tumor in vivo. The tumor inhibition rates (TIR) of DTX-micelles was 91.6% versus 76.3% of Duopafei(®) (P < 0.01). These results suggested that P123 micelles might be considered as an effective DTX delivery system.

Show MeSH
Related in: MedlinePlus