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In vivo pharmacokinetics, biodistribution and antitumor effect of paclitaxel-loaded micelles based on α-tocopherol succinate-modified chitosan.
Drug Deliv. 2016 Oct; 23(8):2651-2660.DD

Abstract

In our previous study, α-tocopherol succinate modified chitosan (CS-TOS) was synthesized and encapsulated paclitaxel (PTX) to form micelles. Preliminary study revealed that the CS-TOS was a potential micellar carrier for PTX. In this study, some further researches were done using Taxol formulation as the control to evaluate the micelle system deeply. In vitro cell experiments demonstrated that the cytotoxic effect of PTX-loaded CS-TOS micelles against MCF-7 cells was comparable with that of Taxol formulation, and the PTX-loaded micelles had excellent cellular uptake ability, which was in a time-dependent manner. The in vivo pharmacokinetic study in rats showed that the micelles prolonged the half-life and increased AUC of PTX than Taxol formulation. From biodistribution study, it was clear that for micelles, the drug concentrations in the liver and spleen were significantly higher than those of Taxol formulation, but much lower in the heart and kidney. Furthermore, the PTX-loaded micelles showed superior antitumor effect, but yielded less toxicity as indicated by the results of antitumor efficacy study and survival study in U14 tumor-bearing mice. These results suggested that CS-TOS micelles could be a potentially useful drug delivery system to improve the performance and safety of PTX.

Authors+Show Affiliations

a College of Chemistry & Chemical Engineering, Harbin Normal University , Harbin , China.b Key Laboratory of Chemical Engineering Process & Technology for High-efficiency Conversion, College of Heilongjiang Province, Heilongjiang University , Harbin , China. c School of Chemistry and Material Science, Heilongjiang University , Harbin , China , and.d School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.d School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.d School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.d School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

26165423

Citation

Liang, Na, et al. "In Vivo Pharmacokinetics, Biodistribution and Antitumor Effect of Paclitaxel-loaded Micelles Based On Α-tocopherol Succinate-modified Chitosan." Drug Delivery, vol. 23, no. 8, 2016, pp. 2651-2660.
Liang N, Sun S, Hong J, et al. In vivo pharmacokinetics, biodistribution and antitumor effect of paclitaxel-loaded micelles based on α-tocopherol succinate-modified chitosan. Drug Deliv. 2016;23(8):2651-2660.
Liang, N., Sun, S., Hong, J., Tian, J., Fang, L., & Cui, F. (2016). In vivo pharmacokinetics, biodistribution and antitumor effect of paclitaxel-loaded micelles based on α-tocopherol succinate-modified chitosan. Drug Delivery, 23(8), 2651-2660.
Liang N, et al. In Vivo Pharmacokinetics, Biodistribution and Antitumor Effect of Paclitaxel-loaded Micelles Based On Α-tocopherol Succinate-modified Chitosan. Drug Deliv. 2016;23(8):2651-2660. PubMed PMID: 26165423.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vivo pharmacokinetics, biodistribution and antitumor effect of paclitaxel-loaded micelles based on α-tocopherol succinate-modified chitosan. AU - Liang,Na, AU - Sun,Shaoping, AU - Hong,Juan, AU - Tian,Jingzhuo, AU - Fang,Liang, AU - Cui,Fude, Y1 - 2015/07/13/ PY - 2015/7/15/pubmed PY - 2017/3/3/medline PY - 2015/7/14/entrez KW - chitosan KW - micelle KW - paclitaxel KW - pharmacokinetics KW - α-Tocopherol succinate SP - 2651 EP - 2660 JF - Drug delivery JO - Drug Deliv VL - 23 IS - 8 N2 - In our previous study, α-tocopherol succinate modified chitosan (CS-TOS) was synthesized and encapsulated paclitaxel (PTX) to form micelles. Preliminary study revealed that the CS-TOS was a potential micellar carrier for PTX. In this study, some further researches were done using Taxol formulation as the control to evaluate the micelle system deeply. In vitro cell experiments demonstrated that the cytotoxic effect of PTX-loaded CS-TOS micelles against MCF-7 cells was comparable with that of Taxol formulation, and the PTX-loaded micelles had excellent cellular uptake ability, which was in a time-dependent manner. The in vivo pharmacokinetic study in rats showed that the micelles prolonged the half-life and increased AUC of PTX than Taxol formulation. From biodistribution study, it was clear that for micelles, the drug concentrations in the liver and spleen were significantly higher than those of Taxol formulation, but much lower in the heart and kidney. Furthermore, the PTX-loaded micelles showed superior antitumor effect, but yielded less toxicity as indicated by the results of antitumor efficacy study and survival study in U14 tumor-bearing mice. These results suggested that CS-TOS micelles could be a potentially useful drug delivery system to improve the performance and safety of PTX. SN - 1521-0464 UR - https://www.unboundmedicine.com/medline/citation/26165423/In_vivo_pharmacokinetics_biodistribution_and_antitumor_effect_of_paclitaxel_loaded_micelles_based_on_α_tocopherol_succinate_modified_chitosan_ L2 - http://www.tandfonline.com/doi/full/10.3109/10717544.2015.1045103 DB - PRIME DP - Unbound Medicine ER -