In the present work, we aimed to optimize the preparation technology of dimethyl curcumin niosomes, improve its solubility and assess its stability. The novel anti-androgen dimethyl curcumin niosomes were prepared by ...In the present work, we aimed to optimize the preparation technology of dimethyl curcumin niosomes, improve its solubility and assess its stability. The novel anti-androgen dimethyl curcumin niosomes were prepared by thin-film dispersion-ultrasonic method, and the prescription composition and preparation process were optimized by single-factor investigation method. Certainly, the solubility and quality evaluation of dimethyl curcumin niosomes were also investigated. The average particle size of prepared dimethyl curcumin niosomes was （310.3＋0.9） nm. The highest encapsulation rate was 88.1%± 1.7%, and the drug-loading amount was 4.03%±1.05%. Moreover, the leakage rate was below 2% within 45 d. Collectively, all these findings indicated that the niosomes, as a vector, could significantly improve the solubility and stability of dimethyl curcumin, offering a theoretical basis for dimethyl curcumin as an anticancer drug in medicine application.展开更多
目的采用Box-Behnken响应面法优化白藜芦醇(resveratrol)-辛酸癸酸聚乙二醇甘油酯(Labrasol)/泊洛沙姆407(P407)混合胶束(Res-Labrasol/P407-MM)的处方工艺,并考察其体外特征。方法HPLC法测定白藜芦醇含量。薄膜分散-探头超声法制备Res-...目的采用Box-Behnken响应面法优化白藜芦醇(resveratrol)-辛酸癸酸聚乙二醇甘油酯(Labrasol)/泊洛沙姆407(P407)混合胶束(Res-Labrasol/P407-MM)的处方工艺,并考察其体外特征。方法HPLC法测定白藜芦醇含量。薄膜分散-探头超声法制备Res-Labrasol/P407-MM。在单因素实验结果的基础上,以投药量、水化体积和水化温度为考察因素,胶束样品的质量浓度和药物沉降率为评价指标,采用Box-Behnken响应面法优化处方,并对最优处方制备的胶束进行外观形态、粒径和体外释放行为评价。结果最佳处方工艺为白藜芦醇投药量28 mg,水化体积9 m L,水化温度40℃,在此条件下测得白藜芦醇平均载药量为(11.62±0.20)%、平均包封率为(93.96±1.83)%、胶束平均粒径为(69.00±1.58)nm,平均Zeta电位为(-21.25±0.18)m V。样品质量浓度和沉降率的实测值与预测值偏差较小,RSD<5.5%。结论Box-Behnken响应面法预测性良好,可以用于优化Res-Labrasol/P407-MM的处方工艺。制备的混合胶束包封率高,粒径小,分布均匀,缓释效果明显。展开更多
基金The National Natural Science Foundation of China(Grant No.31271002)Jiangsu Provincial Department of Education Funded Projects(Grant No.14KJB350001)
文摘In the present work, we aimed to optimize the preparation technology of dimethyl curcumin niosomes, improve its solubility and assess its stability. The novel anti-androgen dimethyl curcumin niosomes were prepared by thin-film dispersion-ultrasonic method, and the prescription composition and preparation process were optimized by single-factor investigation method. Certainly, the solubility and quality evaluation of dimethyl curcumin niosomes were also investigated. The average particle size of prepared dimethyl curcumin niosomes was （310.3＋0.9） nm. The highest encapsulation rate was 88.1%± 1.7%, and the drug-loading amount was 4.03%±1.05%. Moreover, the leakage rate was below 2% within 45 d. Collectively, all these findings indicated that the niosomes, as a vector, could significantly improve the solubility and stability of dimethyl curcumin, offering a theoretical basis for dimethyl curcumin as an anticancer drug in medicine application.
文摘目的采用Box-Behnken响应面法优化白藜芦醇(resveratrol)-辛酸癸酸聚乙二醇甘油酯(Labrasol)/泊洛沙姆407(P407)混合胶束(Res-Labrasol/P407-MM)的处方工艺,并考察其体外特征。方法HPLC法测定白藜芦醇含量。薄膜分散-探头超声法制备Res-Labrasol/P407-MM。在单因素实验结果的基础上,以投药量、水化体积和水化温度为考察因素,胶束样品的质量浓度和药物沉降率为评价指标,采用Box-Behnken响应面法优化处方,并对最优处方制备的胶束进行外观形态、粒径和体外释放行为评价。结果最佳处方工艺为白藜芦醇投药量28 mg,水化体积9 m L,水化温度40℃,在此条件下测得白藜芦醇平均载药量为(11.62±0.20)%、平均包封率为(93.96±1.83)%、胶束平均粒径为(69.00±1.58)nm,平均Zeta电位为(-21.25±0.18)m V。样品质量浓度和沉降率的实测值与预测值偏差较小,RSD<5.5%。结论Box-Behnken响应面法预测性良好,可以用于优化Res-Labrasol/P407-MM的处方工艺。制备的混合胶束包封率高,粒径小,分布均匀,缓释效果明显。
