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Development and in vitro/in vivo evaluation of a novel targeted polymeric micelle for delivery of paclitaxel.
Int J Biol Macromol. 2015 Sep; 80:29-40.IJ

Abstract

In this study a novel receptor-targeted micelle delivery system based on tocopherol succinate-chitosan-polyethylene glycol-folic acid (TS-CS-PEG-FA) was synthesized and loaded with paclitaxel (PTX). Physicochemical properties of the micelles such as critical micelle concentration, micelle size, entrapment efficiency, stability, release properties, cellular uptake and in vitro cytotoxicity were investigated in detail. Furthermore, the pharmacokinetics and tissue distributions of PTX-loaded micelles were evaluated in Balb/c mice and compared with Anzatax(®) (PTX in Cremophor EL(®)). Particle sizes and zeta potentials of the micelles were in the range of 162.3-277.1 nm and 18.5-28.3 mV, respectively. The drug entrapment efficiencies of the micelles were within 53.6-82.5% (w/w). Cytotoxicity assay demonstrated increased cytotoxic activity of PTX-loaded TS-CS-PEG-FA micelles compared to free PTX. The Vd and t1/2β of PTX-loaded TS-CS-PEG-FA were increased by 2.76- and 2.05-fold, respectively, while the plasma AUC of the micelles was only 0.76-fold lower than those of Anzatax(®) As demonstrated by tissue distribution, the PTX/TS-CS-PEG-FA micelles increased accumulation of PTX in tumor tissue. Therefore, the targeted chitosan derived micelle offered a stable and effective delivery system for PTX cancer chemotherapy.

Authors+Show Affiliations

Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, Iran.Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, Iran. Electronic address: rezazade@pharm.mui.ac.ir.Department of Medical Chemistry, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, Iran.Department of Biotechnology, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, Iran.Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, Iran.Department of Pharmacology, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, Iran.Department of Medical Chemistry, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, Iran.Faculty of Pharmacy, University of Manitoba, Winnipeg, Manitoba, Canada.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26093319

Citation

Emami, Jaber, et al. "Development and in Vitro/in Vivo Evaluation of a Novel Targeted Polymeric Micelle for Delivery of Paclitaxel." International Journal of Biological Macromolecules, vol. 80, 2015, pp. 29-40.
Emami J, Rezazadeh M, Hasanzadeh F, et al. Development and in vitro/in vivo evaluation of a novel targeted polymeric micelle for delivery of paclitaxel. Int J Biol Macromol. 2015;80:29-40.
Emami, J., Rezazadeh, M., Hasanzadeh, F., Sadeghi, H., Mostafavi, A., Minaiyan, M., Rostami, M., & Davies, N. (2015). Development and in vitro/in vivo evaluation of a novel targeted polymeric micelle for delivery of paclitaxel. International Journal of Biological Macromolecules, 80, 29-40. https://doi.org/10.1016/j.ijbiomac.2015.05.062
Emami J, et al. Development and in Vitro/in Vivo Evaluation of a Novel Targeted Polymeric Micelle for Delivery of Paclitaxel. Int J Biol Macromol. 2015;80:29-40. PubMed PMID: 26093319.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development and in vitro/in vivo evaluation of a novel targeted polymeric micelle for delivery of paclitaxel. AU - Emami,Jaber, AU - Rezazadeh,Mahboubeh, AU - Hasanzadeh,Farshid, AU - Sadeghi,Hojjat, AU - Mostafavi,Abolfazl, AU - Minaiyan,Mohsen, AU - Rostami,Mahboubeh, AU - Davies,Neal, Y1 - 2015/06/18/ PY - 2015/01/30/received PY - 2015/05/20/revised PY - 2015/05/22/accepted PY - 2015/6/21/entrez PY - 2015/6/21/pubmed PY - 2016/6/15/medline KW - Paclitaxel KW - Pharmacokinetics KW - Polymeric micelle SP - 29 EP - 40 JF - International journal of biological macromolecules JO - Int. J. Biol. Macromol. VL - 80 N2 - In this study a novel receptor-targeted micelle delivery system based on tocopherol succinate-chitosan-polyethylene glycol-folic acid (TS-CS-PEG-FA) was synthesized and loaded with paclitaxel (PTX). Physicochemical properties of the micelles such as critical micelle concentration, micelle size, entrapment efficiency, stability, release properties, cellular uptake and in vitro cytotoxicity were investigated in detail. Furthermore, the pharmacokinetics and tissue distributions of PTX-loaded micelles were evaluated in Balb/c mice and compared with Anzatax(®) (PTX in Cremophor EL(®)). Particle sizes and zeta potentials of the micelles were in the range of 162.3-277.1 nm and 18.5-28.3 mV, respectively. The drug entrapment efficiencies of the micelles were within 53.6-82.5% (w/w). Cytotoxicity assay demonstrated increased cytotoxic activity of PTX-loaded TS-CS-PEG-FA micelles compared to free PTX. The Vd and t1/2β of PTX-loaded TS-CS-PEG-FA were increased by 2.76- and 2.05-fold, respectively, while the plasma AUC of the micelles was only 0.76-fold lower than those of Anzatax(®) As demonstrated by tissue distribution, the PTX/TS-CS-PEG-FA micelles increased accumulation of PTX in tumor tissue. Therefore, the targeted chitosan derived micelle offered a stable and effective delivery system for PTX cancer chemotherapy. SN - 1879-0003 UR - https://www.unboundmedicine.com/medline/citation/26093319/Development_and_in_vitro/in_vivo_evaluation_of_a_novel_targeted_polymeric_micelle_for_delivery_of_paclitaxel_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0141-8130(15)00423-7 DB - PRIME DP - Unbound Medicine ER -