+ Site Statistics
References:
52,654,530
Abstracts:
29,560,856
PMIDs:
28,072,755
+ Search Articles
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ PDF Full Text
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Translate
+ Recently Requested

Enhanced antitumor efficacy and decreased toxicity by self-associated docetaxel in phospholipid-based micelles



Enhanced antitumor efficacy and decreased toxicity by self-associated docetaxel in phospholipid-based micelles



International Journal of Pharmaceutics 434(1-2): 413-419



To overcome the poor aqueous solubility of docetaxel (DTX) and the side effects of the emulsifier in the marketed formulation, we have developed a DTX-loaded micelle using a nontoxic and biodegradable amphiphilic diblock copolymer, methoxy polyethylene glycol-distearoylphosphatidylethanolamine (mPEG(2000)-DSPE). The prepared micelles exhibited a core-shell structure, and DTX was successfully encapsulated in the core with an encapsulation efficiency of 97.31 ± 2.95% and a drug loading efficiency of 3.14 ± 0.13%. The micelles were spherical with a hydrodynamic diameter of approximately 20 nm, which could meet the requirement for in vivo administration, and were expected to enhance the drug's antitumor efficacy and to decrease its toxicity. To evaluate the DTX-loaded micelles, we chose a well marketed formulation, Taxotere(®), as the control. The prepared DTX micelle had a similar antiproliferative effect to Taxotere(®) in vitro but a significantly better antitumor efficacy than Taxotere(®) in vivo, which may be caused by passive targeting of the tumor by the micelles. In addition, the safety evaluation revealed that the DTX micelle was a qualified drug for use in vivo. Based on the experimental results, we propose that mPEG(2000)-DSPE micelle is a potent carrier for DTX.

(PDF emailed within 0-6 h: $19.90)

Accession: 052982137

Download citation: RISBibTeXText

PMID: 22698861

DOI: 10.1016/j.ijpharm.2012.06.014


Related references

Polysialic acid and pluronic F127 mixed polymeric micelles of docetaxel as new approach for enhanced antitumor efficacy. Drug Development and Industrial Pharmacy 43(11): 1827-1835, 2017

The antitumor efficacy of docetaxel is enhanced by encapsulation in novel amphiphilic polymer cholesterol-coupled tocopheryl polyethylene glycol 1000 succinate micelles. Drug Delivery and Translational Research 7(5): 642-653, 2017

Pharmacokinetics, Organ Toxicity and Antitumor Activity of Docetaxel Loaded in Folate Targeted Cholesterol Based Micelles. Current Drug Delivery 13(4): 545-556, 2015

Enhanced Antitumor Efficacy and Reduced Toxicity of Docetaxel Loaded Estradiol Functionalized Stealth Polymeric Nanoparticles. Molecular Pharmaceutics 12(11): 3871-3884, 2016

Folate-conjugated beta-cyclodextrin-based polymeric micelles with enhanced doxorubicin antitumor efficacy. Colloids and Surfaces. B, Biointerfaces 122: 260-269, 2015

Phytantriol Based "Stealth" Lyotropic Liquid Crystalline Nanoparticles for Improved Antitumor Efficacy and Reduced Toxicity of Docetaxel. Pharmaceutical Research 32(10): 3282-3292, 2016

Poly(2-ethyl-2-oxazoline)-doxorubicin conjugate-based dual endosomal pH-sensitive micelles with enhanced antitumor efficacy. Bioconjugate Chemistry 26(1): 110-119, 2015

Mixed Micelles as Nano Polymer Therapeutics of Docetaxel: Increased In vitro Cytotoxicity and Decreased In vivo Toxicity. Current Drug Delivery 15(4): 564-575, 2017

Comparison of hyaluronic acid-based micelles and polyethylene glycol-based micelles on reversal of multidrug resistance and enhanced anticancer efficacy in vitro and in vivo. Drug Delivery 25(1): 330-340, 2018

Enhanced antitumor efficacy by paclitaxel-loaded pluronic P123/F127 mixed micelles against non-small cell lung cancer based on passive tumor targeting and modulation of drug resistance. European Journal of Pharmaceutics and Biopharmaceutics 75(3): 341-353, 2010

Enhanced tolerance and antitumor efficacy by docetaxel-loaded albumin nanoparticles. Drug Delivery 23(8): 2686-2696, 2015

Enhanced in vivo antitumor efficacy of fenretinide encapsulated in polymeric micelles. International Journal of Pharmaceutics 373(1-2): 100-106, 2009

Enhanced antitumor efficacy, biodistribution and penetration of docetaxel-loaded biodegradable nanoparticles. International Journal of Pharmaceutics 430(1-2): 350-358, 2012

Enhanced antitumor efficacy of folate targeted nanoparticles co-loaded with docetaxel and curcumin. Biomedicine & PharmacoTherapy 75(): 26-32, 2016

cRGD/TAT Dual-Ligand Reversibly Cross-Linked Micelles Loaded with Docetaxel Penetrate Deeply into Tumor Tissue and Show High Antitumor Efficacy in Vivo. Acs Applied Materials & Interfaces 9(41): 35651-35663, 2017