• Proceedings of the Korean Society of Toxicology Conference
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• 2001.05a
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• pp.130-130
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• 2001

The commercially available paclitaxel product, Taxol$\circledR$ is currently formulated in a vehicle containing approximately a 1:1 v/v mixture of polyoxyethylated castor oil (Cremophor EL) and ethanol. Cremophor EL, a commonly used surfactant for lipophilic compounds, has been associated with many issues, such as adverse effects particularly following rapid administration, stability with the possibility for drug precipitation upon dilution, and filtering requirements.(omitted)

• Maxillofacial Plastic and Reconstructive Surgery
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• v.28 no.3
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• pp.193-201
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• 2006

Squamous cell carcinoma(SCC) of head and neck(SCCHN) is the sixth most common human malignant tumor. However, despite advances in prevention and treatment of SCC, the five-year survival rates for patients remain still low. To improve the outcome for patients with SCCHN, novel treatment strategies are needed. Overexpression of the epidermal growth factor(EGF) and activation of its receptor(EGFR) are associated with progressive growth of SCCHN. Vascular endothelial growth factor(VEGF) signaling molecules are related with neoangiogenesis and vascular metastasis of SCC. In this study, we determined the therapeutic effect of AEE788(Novartis Pharma AG, Basel, Switzerland), which is a dual inhibitor of EGFR/ErbB2 and VEGFR tyrosine kinases, on human oral SCC. At first, we screened the expression of EGFR, c-ErbB2(HER-2) and VEGFR-2 in a series of human oral SCC cell lines. And then we evaluated the effects of AEE788 on the phosphorylation of EGFR and VEGFR-2 in a oral SCC cell line expressing EGFR/HER-2 and VEGFR-2. We also evaluated the effects of AEE788 alone, or with paclitaxel(Taxol) on the oral SCC cell growth and apoptosis. As a result, all oral SCC cells expressed EGFR and VEGFR-2. Treatment of oral SCC cells with AEE788 led to dose-dependent inhibition of EGFR and VEGFR-2 phosphorylation, growth inhibition, and induction of apoptosis. Moreover, AEE788 sensitizes the cells to paclitaxel-mediated toxicity and apoptosis. These data mean EGFR and VEGFR-2 can be reliable targets for molecular therapy of oral SCC, and therefore warrant clinical use of EGFR/VEGFR inhibition in the treatment of patients with recurrent or metastatic oral SCC.

• Bulletin of the Korean Chemical Society
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• v.34 no.6
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• pp.1800-1808
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• 2013

Dual-responsive amphiphilic block copolymers were synthesized by combining enzymatic ring-opening polymerization (eROP) of ${\varepsilon}$-caprolactone (CL) and ATRP of N,N-dimethylamino-2-ethyl methacrylate (DMAEMA). The obtained block copolymers were characterized by gel permeation chromatography (GPC), $^1H$ NMR and FTIR-IR. The critical micelle concentration (CMC) of copolymer was determined by fluorescence spectra, it can be found that with hydrophilic block (PDMAEMA) increasing, CMC value of the polymer sample increased accordingly, and the CMC value was 0.012 mg/mL, 0.025 mg/mL and 0.037 mg/mL for $PCL_{50}$-b-$PDMAEMA_{68}$, $PCL_{50}$-b-$PDMAEMA_{89}$, $PCL_{50}$-b-$PDMAEMA_{112}$, $PCL_{50}$-b-$PDMAEMA_{89}$ was chosen as drug carrier to study in vitro release profile of anti-cancer drug (taxol). The temperature and pH dependence of the values of hydrodynamic diameter (Dh) of micelles, and self-assembly of the resulting block copolymers in water were evaluated by dynamic light scattering (DLS). The result showed that with the temperature increasing and pH decreasing, the Dh decreased. Drug-loaded nanoparticles were fabricated using paclitaxel as model. Transmission electron microscopy (TEM) and atomic force microscopy (AFM) had been explored to study the morphology of the hollow micelles and the nanoparticles, revealing well-dispersed spheres with the average diameters both around 80 nm. In vitro release kinetics of paclitaxel from the nanoparticles was also investigated in different conditions (pH and temperature, etc.), revealing that the drug release was triggered by temperature changes upon the lower critical solution temperature (LCST) at pH 7.4, and at $37^{\circ}C$ by an increase of pH.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.13
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• pp.5169-5173
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• 2015

To determine the efficacy of postoperative adjuvant chemotherapy with paclitaxel plus cisplatin (Taxol + DDP, TP therapy) for stage IIA esophageal squamous cell carcinoma (ESCC) and to investigate the expression of RUNX3 in lymph node metastasis-negative esophageal cancer and its relationship with medical prognosis, a retrospective summary of clinical treatment of 143 cases of stage IIA esophageal squamous cell carcinoma patients was made. The patients were divided into two groups, a surgery alone control group (52 patients) and a chemotherapy group that received postoperative TP therapy (91 patients). The disease-free and 5 year survival rates were compared between the groups and a multivariate analysis of prognostic factors was performed. The same analysis was performed for cases classified as RUNX3 positive and negative, with post-operative specimens assessed by immunohistochemistry. Although the disease-free and 5 year survival rates in control and chemotherapy groups did not significantly differ and there was no significance in RUNX3 negative cases, postoperative adjuvant chemotherapy in the chemotherapy group was shown to improve disease-free and 5 year survival rate compared to the control group in RUNX3 positive cases. On Cox regression multivariate analysis, postoperative adjuvant chemotherapy (P<0.01) was an independent prognostic factor for RUNX3 positive cases, suggesting that postoperative TP may be effective as adjuvant chemotherapy for stage IIA esophageal cancer patients with RUNX3 positive lesions.

• Journal of Gastric Cancer
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• v.5 no.4 s.20
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• pp.252-259
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• 2005

To clarify the clinicopathologic features of small-cell carcinomas (SCC) of the stomach, we reviewed three cases of surgically treated SCC. The first case was a pure SCC, with severe pancreatic invasion and peritoneal seeding. A gastro-jejunostomy was performed. Postoperative chemotherapy was performed with CDDP and VP-16 (8 cycles) but showed disease progression (PD); a consecutive chemotherapy with CDDP and irinotencan (2 cycles) also showed PD. A third line with CDDP, VP16, ifosfamide, and mesna was followed by a 4th line (CDDP and Taxol). The male patient died with liver metastasis and peritoneal seeding 14 months after the operation. The second case was a SCC mixed with a poorly differentiated adenocarcinoma. Profound lymphadenopathy and liver metastasis were found. Two cycles of preoperative chemotherapy with TS-1 and CDDP were performed, which showed nearly complete remission for lymphadenopathy and partial response for the primary tumor site and liver metastatic lesion. A total gastrectomy and extended lymphadenectomy was performed. There were no viable cancer cells in 35 retrieved lymph nodes. Postoperative chemotherapy using the same regimen was performed for 4 cycles. Enlarged liver metastasis was found at the follow-up CT scan, so a posterior segmentectomy of liver was performed. After liver surgery, the chemotherapy regimen was changed to irinotecan and cisplatin. This male patient has been in good health for the f4 months since gastric surgery. The third case was a pure SCC, and a subtotal gastrectomy was performed curatively. That male patient received 5 cycles of TS-1 and is still in good health 14 months after operation.