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Poloxamer-Based Thermoreversible Gel for Topical Delivery of Emodin: Influence of P407 and P188 on Solubility of Emodin and Its Application in Cellular Activity Screening

机译:基于泊洛沙姆的大黄素局部传递热可逆凝胶:P407和P188对大黄素溶解度的影响及其在细胞活性筛选中的应用

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Emodin is a component in a Chinese herb, Rheum officinale Baill, traditionally used for diabetes and anticancer. Its poor solubility is one of the major challenges to pharmaceutical scientists. We previously reported on thermoreversible gel formulations based on poloxamer for the topical delivery of emodin. The present study was to understand the effect of poloxamer type on emodin solubility and its application in cellular activity screening. Various gel formulations composed of poloxamer 407 (P407), poloxamer 188 (P188) and PEG400 were prepared and evaluated. Major evaluation parameters were the gelation temperature (Tgel) and solubility of emodin. The emodin solubility increased with increasing poloxamer concentration and the Tgel was modulated by the proper combination of P407. In particular, this study showed that the amount of P407 in thermoreversible poloxamer gel (PG) was the dominant factor in enhancing solubility and P188 was effective at fixing gelation temperature in the desired range. A thermoreversible emodin PG was selected as the proper composition with the liquid state at room temperature and gel state at body temperature. The gel showed the solubility enhancement of emodin at least 100-fold compared to 10% ethanol or water. The thermoreversible formulation was applied for in vitro cellular activity screening in the human dermal fibroblast cell line and DLD-1 colon cancer cell line after dilution with cell culture media. The thermoreversible gel formulation remained as a clear solution in the microplate, which allowed reliable cellular activity screening. In contrast, emodin solution in ethanol or DMSO showed precipitation at the corresponding emodin concentration, complicating data interpretation. In conclusion, the gel formulation is proposed as a useful prototype topical formulation for testing emodin in vivo as well as in vitro.
机译:大黄素是中草药大黄(Rheum officinale Baill)中的一种成分,传统上用于糖尿病和抗癌。其溶解性差是药物科学家面临的主要挑战之一。我们先前曾报道过基于泊洛沙姆的可逆性凝胶制剂可用于大黄素的局部给药。本研究旨在了解泊洛沙姆类型对大黄素溶解度的影响及其在细胞活性筛选中的应用。制备并评估了由泊洛沙姆407(P407),泊洛沙姆188(P188)和PEG400组成的各种凝胶制剂。主要评估参数是大黄素的胶凝温度(Tgel)和溶解度。大黄素的溶解度随泊洛沙姆浓度的增加而增加,Tgel受P407适当组合的调节。特别地,该研究表明,热可逆泊洛沙姆凝胶(PG)中P407的含量是提高溶解度的主要因素,而P188可有效地将凝胶温度固定在所需范围内。选择热可逆大黄素PG作为合适的组合物,其室温下为液态,体温下为凝胶态。与10%的乙醇或水相比,该凝胶显示大黄素的溶解度提高了至少100倍。用细胞培养基稀释后,将热可逆制剂用于人皮肤成纤维细胞系和DLD-1结肠癌细胞系中的体外细胞活性筛选。热可逆凝胶制剂以澄清溶液形式保留在微孔板中,可进行可靠的细胞活性筛选。相反,大黄素在乙醇或DMSO中的溶液在相应的大黄素浓度下显示出沉淀,使数据解释复杂化。总之,该凝胶制剂被建议作为一种有用的原型局部制剂,用于体内和体外测试大黄素。

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