Docetaxel-conjugated monomethoxy-poly(ethylene glycol)-b-poly(lactide) (mPEG-PLA) polymeric micelles to enhance the therapeutic efficacy in oral squamous cell carcinoma

RSC Advances ◽  
2016 ◽  
Vol 6 (49) ◽  
pp. 42819-42826 ◽  
Author(s):  
Liang Shi ◽  
Xiao-Bin Song ◽  
Yong Wang ◽  
Ke-Tao Wang ◽  
Ping Liu ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Oral Squamous Cell Carcinoma ◽  
Ethylene Glycol ◽  
Cell Carcinoma ◽  
Therapeutic Efficacy ◽  
Polymeric Micelles ◽  
Poly Ethylene Glycol ◽  
Ester Linkage ◽  
Poly Ethylene ◽  
Polymer Block

In this study, docetaxel (DTX) was successfully conjugated to the monomethoxy-poly(ethylene glycol)-b-poly(lactide) (mPEG-PLA) polymer block via an ester linkage (DTX-PM).

Tissue Distribution and Systemic Toxicity Evaluation of Raloxifene Targeted Polymeric Micelles of Poly (Styrene-Maleic Acid)-Poly (Amide- Ether-Ester-Imide)-Poly (Ethylene Glycol) Loaded With Docetaxel in Breast Cancer Bearing Mice

2019 ◽  
Vol 14 (3) ◽  
pp. 280-291 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Farshid Hassanzadeh ◽  
Batool Hashemi-Beni ◽  
Mohsen Minaiyan ◽  
Saeedeh Enteshari
Keyword(s):  
Side Effects ◽  
Antitumor Activity ◽  
Ethylene Glycol ◽  
Tissue Distribution ◽  
Tumor Cells ◽  
Maleic Acid ◽  
Polymeric Micelles ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Ether Ester

Background: Due to the low water solubility of Docetaxel (DTX), it is formulated with ethanol and Tween 80 with lots of side effects. For this reason, special attention has been paid to formulate it in new drug nano-carriers. Objective: The goal of this study was to evaluate the safety, antitumor activity and tissue distribution of the novel synthesized Raloxifene (RA) targeted polymeric micelles. Methods: DTX-loaded RA-targeted polymeric micelles composed of poly(styrene-maleic acid)- poly(amide-ether-ester-imide)-poly(ethylene glycol) (SMA-PAEE-PEG) were prepared and their antitumor activity was studied in MC4-L2 tumor-bearing mice compared with non-targeted micelles and free DTX. Safety of the micelles was studied by Hematoxylin and Eosin (H&E) staining of tumors and major organs of the mice. The drug accumulation in the tumor and major organs was measured by HPLC method. Results: The results showed better tumor growth inhibition and increased survival of mice treated with DTX-loaded in targeted micelles compared to the non-targeted micelles and free DTX. Histopathological studies, H&E staining of tumors and immunohistochemical examination showed the potential of DTX-loaded RA-targeted micelles to inhibit tumor cells proliferation. The higher accumulation of the DTX in the tumor tissue after injection of the micelles compared to the free DTX may indicate the higher uptake of the targeted micelles by the G-Protein-Coupled Estrogen Receptors (GPER). Conclusion: The results indicate that RA-conjugated polymeric micelles may be a strong and effective drug delivery system for DTX therapy and uptake of the drug into tumor cells, and overcome the disadvantages and side effects of conventional DTX.

Effects of denaturing acid on the self-association behaviour of poly(ethylene glycol)-block-poly(γ-benzyl l-glutamate)-graft-poly(ethylene glycol) copolymer in ethanol

2011 ◽  
Vol 65 (4) ◽  
Author(s):  
Guo-Quan Zhu ◽  
Qiao-Chun Gao ◽  
Fa-Gang Wang ◽  
Guo-Chang Li ◽  
Ping Wang
Keyword(s):  
Ethylene Glycol ◽  
Polymeric Micelles ◽  
The Self ◽  
Mixed System ◽  
Resonance Spectroscopy ◽  
Poly Ethylene Glycol ◽  
Transmission Electron ◽  
Self Association ◽  
Ester Exchange Reaction ◽  
Poly Ethylene

AbstractPoly(ethylene glycol)-block-poly(γ-benzyl l-glutamate)-graft-poly(ethylene glycol) (PEG-b-PBLG-g-PEG) copolymer was synthesised by the ester exchange reaction of PEG-block-PBLG copolymer with mPEG. The self-association behaviour of PEG-b-PBLG-g-PEG in mixtures of ethanol, chloroform, and trifluoroacetic acid as denaturing acid was investigated by transmission electron microscopy, nuclear magnetic resonance spectroscopy, FT-IR spectroscopy, dynamic light scattering, and viscometry. It was revealed that the increase in denaturing acid content in the mixed system not only promoted the critical micelle concentration but also changed the morphology of the polymeric micelles from elliptical to spherical.

Therapeutic Efficacy Evaluation of Curcumin on Human Oral Squamous Cell Carcinoma Xenograft Using Multimodalities of Molecular Imaging

2010 ◽  
Vol 38 (02) ◽  
pp. 343-358 ◽  
Author(s):  
Yu-Chuan Lin ◽  
Hong-Wen Chen ◽  
Yu-Cheng Kuo ◽  
Ya-Fang Chang ◽  
Yi-Jang Lee ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Animal Model ◽  
Molecular Imaging ◽  
Oral Squamous Cell Carcinoma ◽  
Cell Carcinoma ◽  
Squamous Cell ◽  
Therapeutic Efficacy ◽  
Therapeutic Effects ◽  
Significant Difference

Oral squamous cell carcinoma (OSCC) is the most common malignancy of the oral cavity; however the treatment approaches are still unsatisfactory. We used a luciferase-transfected animal model to evaluate the therapeutic effects of curcumin. Human oral squamous cell carcinoma SAS cell line was stably transfected with luc gene, named SAS/luc cells. For the in vivo study, they were inoculated subcutaneously to 6-week-old male NOD/SCID mice which were separated into four groups for intraperitoneal injection (i.p.) of curcumin: control, daily with 35 mg/kg, 70 mg/kg every 2 days, and 100 mg/kg every 3 days. We applied SAS/luc bearing animal model and bioluminescent imaging (BLI) to study the inhibition effect of curcumin on tumor growth. The cytotoxic effect of curcumin on SAS/luc cells was mainly at G2/M phase and a significant dose dependent increase of the apoptotic SAS/luc cells as represented by sub-G1 phase was shown. Therapeutic efficacy evaluated by both caliper assay and BLI showed a significant difference between curcumin-treated mice and the controls (p < 0.01). The significant inhibition effects of curcumin on the proliferation and the growth of human OSCC are observed both in vitro and in vivo. No significant body weight change (i.e. within 20%) was observed in all SAS/luc-bearing mice with or without curcumin treatment. This SAS/luc human OSCC bearing animal model combined with multimodalities of molecular imaging permits a sensitive and non-invasive approach to evaluate the therapeutic efficacy in vivo.

Factors influencing aggregation behavior of poly(γ-benzyl l-glutamate)-graft-poly(ethylene glycol) copolymer in mixed solvents

2010 ◽  
Vol 64 (5) ◽  
Author(s):  
Guo-Quan Zhu ◽  
Fa-Gang Wang ◽  
Yu-Ying Liu ◽  
Qiao-Chun Gao
Keyword(s):  
Ethylene Glycol ◽  
Polymeric Micelles ◽  
Mixed Solvents ◽  
Particle Diameter ◽  
Solution Concentration ◽  
Aggregation Behavior ◽  
Average Particle ◽  
Poly Ethylene Glycol ◽  
Preparation Conditions ◽  
Poly Ethylene

AbstractPoly(γ-benzyl l-glutamate)-graft-poly(ethylene glycol) (PBLG-graft-PEG) copolymer was synthesized by the ester exchange reaction of PBLG homopolymer with mPEG. Aggregation behavior of the PBLG-graft-PEG copolymer in mixtures of ethanol and chloroform was investigated by transmission electron microscopy (TEM), dynamic light scattering (DLS), and viscometry. Effects of the polymer solution concentration, grafting degree, test temperature, and chloroform content on the morphology, average particle diameter, and critical micelle concentration (CMC) of the micelles formed by the PBLG-graft-PEG copolymer in the mixed solvents were mainly studied. It was revealed that the PBLG-graft-PEG copolymer can self-assemble into polymeric micelles with a core-shell structure in various shapes depending on the preparation conditions.

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