Abstract：
UNASSIGNED: This study aimed to develop, optimize and evaluate glyceryl monooleate (GMO) based cubosomes as a drug delivery system containing cisplatin for treatment of human lung carcinoma.
UNASSIGNED: The significance of this research was to successfully incorporate slightly water soluble and potent anticancer drug (cisplatin) into cubosomes, which provide slow and sustained release of drug for longer period of time.
UNASSIGNED: The delivery system was developed through top-down approach by melting GMO and poloxamer 407 (P407) at 70 °C and then drop-wise addition of warm deionized water (70 °C) containing cisplatin. The formulation then exposed to probe sonicator for about 2 min. A randomized regular two level full factorial design with help of Design Expert was used for optimization of blank cubosomal formulations. Cisplatin loaded cubosomes were then subjected to physico-chemical characterization.
UNASSIGNED: The characterization of the formulation revealed that it had a sufficient surface charge of -9.56 ± 1.33 mV, 168.25 ± 5.73 nm particle size, and 60.64 ± 0.11% encapsulation efficiency. The in vitro release of cisplatin from the cubosomes at pH 7.4 was observed to be sustained, with 94.5% of the drug being released in 30 h. In contrast, 99% of cisplatin was released from the drug solution in just 1.5 h. In vitro cytotoxicity assay was conducted on the human lung carcinoma NCI-H226 cell line, the cytotoxicity of cisplatin-loaded cubosomes was relative to that of pure cisplatin solution, while blank (without cisplatin) cubosomes were nontoxic.
UNASSIGNED: The obtained results demonstrated the successful development of cubosomes for sustained delivery of cisplatin.
Cubosomes were prepared, optimized, and evaluated for cisplatin delivery.A randomized regular two level full factorial design was constructed to optimize blank cubosomes.Blank cubosomes consisted of GMO as the lipid and P407 as an emulsifying agent.In vitro release studies demonstrated sustained release of cisplatin from cubosomes at pH 7.4.Cytotoxicity assay on human lung carcinoma cell line NCI-H226 showed similar cytotoxicity between cisplatin-loaded cubosomes and pure cisplatin solution while blank cubosomes exhibited no toxicity.
UNASSIGNED: The significance of this research was to successfully incorporate slightly water soluble and potent anticancer drug (cisplatin) into cubosomes, which provide slow and sustained release of drug for longer period of time.
UNASSIGNED: The delivery system was developed through top-down approach by melting GMO and poloxamer 407 (P407) at 70 °C and then drop-wise addition of warm deionized water (70 °C) containing cisplatin. The formulation then exposed to probe sonicator for about 2 min. A randomized regular two level full factorial design with help of Design Expert was used for optimization of blank cubosomal formulations. Cisplatin loaded cubosomes were then subjected to physico-chemical characterization.
UNASSIGNED: The characterization of the formulation revealed that it had a sufficient surface charge of -9.56 ± 1.33 mV, 168.25 ± 5.73 nm particle size, and 60.64 ± 0.11% encapsulation efficiency. The in vitro release of cisplatin from the cubosomes at pH 7.4 was observed to be sustained, with 94.5% of the drug being released in 30 h. In contrast, 99% of cisplatin was released from the drug solution in just 1.5 h. In vitro cytotoxicity assay was conducted on the human lung carcinoma NCI-H226 cell line, the cytotoxicity of cisplatin-loaded cubosomes was relative to that of pure cisplatin solution, while blank (without cisplatin) cubosomes were nontoxic.
UNASSIGNED: The obtained results demonstrated the successful development of cubosomes for sustained delivery of cisplatin.
Cubosomes were prepared, optimized, and evaluated for cisplatin delivery.A randomized regular two level full factorial design was constructed to optimize blank cubosomes.Blank cubosomes consisted of GMO as the lipid and P407 as an emulsifying agent.In vitro release studies demonstrated sustained release of cisplatin from cubosomes at pH 7.4.Cytotoxicity assay on human lung carcinoma cell line NCI-H226 showed similar cytotoxicity between cisplatin-loaded cubosomes and pure cisplatin solution while blank cubosomes exhibited no toxicity.
摘要：
目的本研究旨在发展，优化和评估基于单油酸甘油酯（GMO）的立方体作为含顺铂的药物递送系统用于治疗人肺癌。这项研究的意义是成功地将微水溶性和有效的抗癌药物（顺铂）掺入到立方体中，这提供了更长时间的缓慢和持续的药物释放。方法通过自顶向下的方法,通过在70°C下熔化GMO和泊洛沙姆407(P407),然后逐滴添加含有顺铂的温去离子水(70°C)来开发递送系统。然后将制剂暴露于探针超声波仪约2分钟。在DesignExpert的帮助下，使用随机规则的两级全因子设计来优化空白立方体配方。然后对负载顺铂的立方体进行物理化学表征。结果该制剂的表征表明，它具有-9.56±1.33mV的足够表面电荷，168.25±5.73nm粒径，和60.64±0.11%的封装效率。观察到在pH7.4下，顺铂从立方体中的体外释放是持续的，94.5%的药物在30小时内释放。相比之下,99%的顺铂在仅1.5小时内从药物溶液中释放。对人肺癌NCI-H226细胞系进行体外细胞毒性测定，负载顺铂的立方体的细胞毒性相对于纯顺铂溶液，而空白（不含顺铂）立方体是无毒的。结论获得的结果表明成功开发了用于持续递送顺铂的立方体。
准备好了立方体,优化,并评估顺铂的给药情况。构建了随机规则的两级全因子设计，以优化空白立方体。空白立方体由作为脂质的GMO和作为乳化剂的P407组成。体外释放研究表明，顺铂在pH7.4时从立方体中持续释放。对人肺癌细胞系NCI-H226的细胞毒性测定显示，负载顺铂的立方体和纯顺铂溶液之间具有相似的细胞毒性，而空白立方体没有毒性。
准备好了立方体,优化,并评估顺铂的给药情况。构建了随机规则的两级全因子设计，以优化空白立方体。空白立方体由作为脂质的GMO和作为乳化剂的P407组成。体外释放研究表明，顺铂在pH7.4时从立方体中持续释放。对人肺癌细胞系NCI-H226的细胞毒性测定显示，负载顺铂的立方体和纯顺铂溶液之间具有相似的细胞毒性，而空白立方体没有毒性。
