Home>>Biochemical Assay Reagents>>Cremophor EL

Cremophor EL Sale

(Synonyms: 聚氧乙烯蓖麻油EL) 目录号 : GC30024

Cremophor EL (CrEL, Kolliphor EL), a polyethoxylated surfactant, is a formulation vehicle used for various poorly-water soluble drugs, including the anticancer agent paclitaxel (Taxol). Cremophor EL is used in severe anaphylactoid hypersensitivity reactions, hyperlipidaemia, abnormal lipoprotein patterns, aggregation of erythrocytes and peripheral neuropathy.

Cremophor EL Chemical Structure

Cas No.:61791-12-6

规格 价格 库存 购买数量
100mL
¥714.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment:

Cell viability is determined by double fluorescent staining: bis-benzimide labels all cell nuclei, ethidium-homodimer-1 stains only dead cells. For morphological examinations, primary brain endothelial cells with tight barrier properties are used. Cells grown on glass coverslips are treated with Cremophor EL and RH40 for 1 and 24 h. Cremophor EL and RH40 are tested at 0.1 to 50 mg/mL concentrations. Triton X-100 detergent (10 mg/mL) is used in toxicity assays as a reference compound to cause cell death[1].

References:

[1]. Kiss L, et al. Kinetic analysis of the toxicity of pharmaceutical excipients Cremophor EL and RH40 on endothelial and epithelial cells. J Pharm Sci. 2013 Apr;102(4):1173-81.

产品描述

Cremophor EL (CrEL, Kolliphor EL), a polyethoxylated surfactant, is a formulation vehicle used for various poorly-water soluble drugs, including the anticancer agent paclitaxel (Taxol). Cremophor EL is used in severe anaphylactoid hypersensitivity reactions, hyperlipidaemia, abnormal lipoprotein patterns, aggregation of erythrocytes and peripheral neuropathy.

Cremophor EL is a widely used excipient. In the first 10 h, Cremophor EL at 5 mg/mL increases the impedance, then decreases it, and after 20 h of treatment, epithelial cell death is detected. Cremophor EL in concentrations corresponding to clinical doses causes endothelial and epithelial toxicity. Both epithelial viability and monolayer integrity are seriously impaired at 10 to 50 mg/mL concentrations of Cremophor EL at 24-h treatment. Cremophor EL also enhances cell detachment.[1]

Cremophor EL reduces nociception in a dose-dependent manner. At 10.6 g/kg, Cremophor EL causes antinociception similar to that induced by dipyrone (300 mg/kg, by gavage) in the abdominal writhing test, and antinociception similar to that induced by morphine (20 mg/kg, by gavage) in the tail immersion test.

[1] Kiss L, et al. J Pharm Sci. 2013 Apr;102(4):1173-81. [3] Gelderblom H, et al. Eur J Cancer. 2001 Sep;37(13):1590-8.

Chemical Properties

Cas No. 61791-12-6 SDF
别名 聚氧乙烯蓖麻油EL
Canonical SMILES [Cremophor EL]
分子式 分子量
溶解度 Water : 25 mg/mL 储存条件 Store at RT, protect from light
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

Research Update

Cremophor EL: the drawbacks and advantages of vehicle selection for drug formulation

Eur J Cancer 2001 Sep;37(13):1590-8.11527683 10.1016/s0959-8049(01)00171-x

Cremophor EL (CrEL) is a formulation vehicle used for various poorly-water soluble drugs, including the anticancer agent paclitaxel (Taxol). In contrast to earlier reports, CrEL is not an inert vehicle, but exerts a range of biological effects, some of which have important clinical implications. Its use has been associated with severe anaphylactoid hypersensitivity reactions, hyperlipidaemia, abnormal lipoprotein patterns, aggregation of erythrocytes and peripheral neuropathy. The pharmacokinetic behaviour of CrEL is dose-independent, although its clearance is highly influenced by duration of the infusion. This is particularly important since CrEL can affect the disposition of various drugs by changing the unbound drug concentration through micellar encapsulation. In addition, it has been shown that CrEL, as an integral component of paclitaxel chemotherapy, modifies the toxicity profile of certain anticancer agents given concomitantly, by mechanisms other than kinetic interference. A clear understanding of the biological and pharmacological role of CrEL is essential to help oncologists avoid side-effects associated with the use of paclitaxel or other agents using this vehicle. With the present development of various new anticancer agents, it is recommended that alternative formulation approaches should be pursued to allow a better control of the toxicity of the treatment and the pharmacological interactions related to the use of CrEL.

Cremophor EL Nano-Emulsion Monomerizes Chlorophyll a in Water Medium

Biomolecules 2019 Dec 16;9(12):881.31888249 PMC6995590

In this paper, the application of a non-ionic detergent Cremophor EL for monomerization of chlorophyll a in an aqueous medium is studied. The spectrophotometric properties of chlorophyll a encapsulated into the Cremophor EL nano-emulsion system were characterized by electronic absorption, steady-state and time-resolved fluorescence as well as circular dichroism spectroscopy. The results have shown that chlorophyll a dissolves more efficiently in the aqueous medium containing low-level Cremophor (5 wt%) than at an ethanolic solution even in the concentration of 10-4 M. The molecular organization of the chlorophyll a in the Cremophor EL nano-micelles was also investigated by means of Raman spectroscopy. The spectral changes in the frequency of the C=O stretching group were used to distinguish the aggregation state of chlorophyll. It was revealed that chlorophyll a exists dominantly in the monomeric form in the Cremophor EL aqueous solution. The promising aspect of the use of Cremophor EL nano-emulsion as a delivery system is to maintain stable chlorophyll monomer in an aqueous medium. It would open the potential for a new, practical application of chlorophyll a in medicine, as a dietary supplement or studies on molecular organization of chlorophyll a in the well-defined artificial system.

Albumin-bound paclitaxel: a next-generation taxane

Expert Opin Pharmacother 2006 Jun;7(8):1041-53.16722814 10.1517/14656566.7.8.1041

Taxanes are standard treatment for metastatic breast cancer; however, the solvents used as vehicles in these formulations cause severe toxicities. The FDA recently approved a solvent-free formulation of paclitaxel for the treatment of metastatic breast cancer that utilises 130-nanometer albumin-bound (nab) technology (Abraxane; nab-paclitaxel) to circumvent the requirement for solvents. nab-Paclitaxel utilises the natural properties of albumin to reversibly bind paclitaxel, transport it across the endothelial cell and concentrate it in areas of tumour. The proposed mechanism of drug delivery involves, in part, glycoprotein 60-mediated endothelial cell transcytosis of paclitaxel-bound albumin and accumulation in the area of tumour by albumin binding to SPARC (secreted protein, acidic and rich in cysteine). Clinical studies have shown that nab-paclitaxel is significantly more effective than paclitaxel formulated as Cremophor EL (CrEL, Taxol, CrEL-paclitaxel), with almost double the response rate, increased time to disease progression and increased survival in second-line patients. The absence of CrEL from the formulation is associated with decreased neutropenia and rapid improvement of peripheral neuropathy with nab-paclitaxel, compared with CrEL-paclitaxel. For these reasons, nab-paclitaxel can be administered using higher doses of paclitaxel than that achievable with CrEL-paclitaxel, with shorter infusion duration and without the requirement for corticosteroid and antihistamine premedication to reduce the risk of solvent-mediated hypersensitivity reactions. Taken together, these studies have demonstrated that nab technology has increased the therapeutic index of paclitaxel compared with the conventional, solvent-based formulation.

Cremophor EL Alters the Plasma Protein Binding and Pharmacokinetic Profile of Valspodar in Rats

Drug Res (Stuttg) 2017 Oct;67(10):591-595.28628923 10.1055/s-0043-111411

Cremophor EL is a nonionic surfactant widely used in pharmaceutical formulations. Nonetheless, there are several reports on the influence of this excipient on the protein binding, pharmacokinetics, and pharmacodynamics of drugs. Valspodar is an investigational non-immunosuppressive derivative of cyclosporine A, used in clinical trials for treatment of multidrug resistant tumors. The formulation of valspodar (Amdray®) contains Cremophor EL and ethanol as solubilizing agents. The main aim of the current study was to assess the plasma protein binding (in vitro) and the pharmacokinetic profile of valspodar in the cremophor EL-based formulation in comparison to a cremophor EL-free formulation following intravenous (i. v.) administration to rats. Valspodar dissolved in PEG 400/ethanol (diluted in Dextrose 5%) was used as the cremophor EL-free formulation. The in vitro plasma unbound fraction (f u) of valspodar in the Cremophor EL formulation was 2.3-fold higher than the PEG 400/ethanol formulation. Following a single i. v. dose of 5 mg/kg, valspodar in the cremophor EL-based formulation had around 50% lower plasma AUC compared to the PEG 400/ethanol formulation. Moreover, the Cremophor EL formulation had significantly higher volume of distribution and clearance in comparison to the PEG 400-based formulation. The results highlight the significance of excipient-drug interaction that should not be overlooked during the early stages of drug development.

Pharmacology and toxicology of Cremophor EL diluent

Ann Pharmacother 1994 May;28(5 Suppl):S11-4.7915152 10.1177/10600280940280S503