In vitro and in vivo anticancer effect of pH-responsive paclitaxel-loaded niosomes.
In vitro and in vivo anticancer effect of pH-responsive paclitaxel-loaded niosomes.
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pH响应性紫杉醇载药囊泡的体外和体内抗癌作用。
DOI：
10.1007/s10856-021-06623-6
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发表时间：
2021-12-04
期刊：
影响因子：
--
通讯作者：
Baino F
中科院分区：
文献类型：
--
作者：
Barani M;Hajinezhad MR;Sargazi S;Rahdar A;Shahraki S;Lohrasbi-Nejad A;Baino F
在这项研究中，开发了以麦角甾醇修饰的紫杉醇（PTX）负载ph响应niosomes。对该制剂进行了粒径、形态、包封效率（EE）及pH值为5.2和7.4时的体外释放度表征。使用MCF7、Hela和HUVEC细胞系评估游离PTX和niosome/PTX的体外疗效。为了评价niosomal PTX在大鼠体内的作用，与游离PTX相比，动物腹腔注射2.5 mg/kg和5 mg/kg niosomal PTX两周。结果表明，该纳米粒粒径为纳米级，呈球形，EE含量为77%，在pH 5.2和pH 7.4条件下具有pH响应释放。与游离PTX相比，我们发现用niosomal PTX治疗癌细胞48小时后，ic50明显降低，对宫颈癌和乳腺癌衍生的人类癌症也有很高的疗效。此外，niosomal PTX诱导这些细胞系发生了明显的形态学变化。与对照组相比，体内给药2.5 mg/kg的游离PTX显著增加了大鼠的血清生化指标和肝脏脂质过氧化。乳状体PTX给予大鼠的情况不同：5 mg/kg剂量的乳状体PTX显著提高了大鼠的血清生化指标，但2.5 mg/kg剂量的乳状体PTX组的毒性作用低于相同剂量的游离PTX组。总之，我们的研究结果证明了将PTX包埋在niosomal制剂中以提高其治疗效果的概念。
In this study, paclitaxel (PTX)-loaded pH-responsive niosomes modified with ergosterol were developed. This new formulation was characterized in terms of size, morphology, encapsulation efficiency (EE), and in vitro release at pH 5.2 and 7.4. The in vitro efficacy of free PTX and niosome/PTX was assessed using MCF7, Hela, and HUVEC cell lines. In order to evaluate the in vivo efficacy of niosomal PTX in rats as compared to free PTX, the animals were intraperitoneally administered with 2.5 mg/kg and 5 mg/kg niosomal PTX for two weeks. Results showed that the pH-responsive niosomes had a nanometric size, spherical morphology, 77% EE, and pH-responsive release in pH 5.2 and 7.4. Compared with free PTX, we found markedly lower IC50s when cancer cells were treated for 48 h with niosomal PTX, which also showed high efficacy against human cancers derived from cervix and breast tumors. Moreover, niosomal PTX induced evident morphological changes in these cell lines. In vivo administration of free PTX at the dose of 2.5 mg/kg significantly increased serum biochemical parameters and liver lipid peroxidation in rats compared to the control rats. The situation was different when niosomal PTX was administered to the rats: the 5 mg/kg dosage of niosomal PTX significantly increased serum biochemical parameters, but the group treated with the 2.5 mg/kg dose of niosomal PTX showed fewer toxic effects than the group treated with free PTX at the same dosage. Overall, our results provide proof of concept for encapsulating PTX in niosomal formulation to enhance its therapeutic efficacy.
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DOI：
10.2147/dddt.s142337
发表时间：
2017
期刊：
Drug design, development and therapy
影响因子：
--
作者：
Jurj A;Braicu C;Pop LA;Tomuleasa C;Gherman CD;Berindan-Neagoe I
通讯作者：
Berindan-Neagoe I
影响因子：
10.8
作者：
Kyriakides, TR;Cheung, CY;Hoffman, AS
通讯作者：
Hoffman, AS
影响因子：
3.4
作者：
Hafez, IM;Cullis, PR
通讯作者：
Cullis, PR
影响因子：
9.9
作者：
Chowdhury P;Nagesh PKB;Hatami E;Wagh S;Dan N;Tripathi MK;Khan S;Hafeez BB;Meibohm B;Chauhan SC;Jaggi M;Yallapu MM
通讯作者：
Yallapu MM
影响因子：
3.8
作者：
Bayindir, Zerrin Sezgin;Yuksel, Nilufer
通讯作者：
Yuksel, Nilufer