文献:两亲性mPEG-胆固醇共轭物的合成、胶束化及其在姜黄素递送中的应用
链接:http://dspace.nitrkl.ac.in/dspace/handle/2080/3725
作者:普拉丹、艾斯瓦娅·帕特尔、萨比塔
节选:
癌症是全球*致命的疾病,至今仍未得到根治。众多研究人员和科学家已经提出了几种方法来根除癌症,即联合*方式和引入多种药物载体,如脂质体、纳米颗粒、胶束等。其中,聚合物胶束作为药物递送载体因其稳定性更高、CMC 更低、溶解性更好、粒径小和生物相容性更好而备受关注。为了将 PEG 基胶束配制成疏水药物载体,我们通过缩合法合成了两亲性 mPEG-胆固醇共轭物。使用 1H NMR、FTIR、HRMS 光谱分析对合成的聚合物表面活性剂进行了表征。通过紫外可见光和荧光法分析了这些合成表面活性剂的胶束化行为。发现上述体系的 CMC 在微摩尔范围内。以姜黄素为模型药物,研究了使用配制的稳定胶束进行疏水药物的掺入和递送。与水介质中的姜黄素相比,姜黄素在胶束介质中的稳定性非常高。计算得出的药物负载效率为 72%,可与其他胶束体系相媲美。通过 XRD 分析证实了药物的掺入。利用 SEM 技术分析了表面形貌。从 DSC 热分析图可以看出,负载姜黄素的胶束的稳定性高于未负载的胶束。药物释放曲线证实了药物的持续释放,这对癌症*至关重要。还研究了细胞活力和*癌活性。从获得的总体结果来看,我们配制的 mPEG-胆固醇胶束体系被发现是一种非常有前途且有效的药物递送载体。
Cancer is a deadliest illness worldwide which is still not conquered. Several approaches have been made by various researchers and scientists to eradicate it by combined therapeutic modalities and introduction of number of drug carriers like liposomes, nanoparticles, micelles etc. Among them polymeric micelles as a drug delivery carrier has gained much more attention because of its greater stability, lower CMC, solubility, small size and biocompatibility. In an attempt to formulate PEG-based micelle as hydrophobic drug carrier, we have synthesized amphiphilic mPEG-Cholesterol conjugates by condensation method. The synthesized polymeric surfactants were characterised using 1H NMR, FTIR, HRMS spectral analysis. Micellization behaviour of these synthesized surfactants were analysed by UV-Vis and fluorescence method. The CMC of the above systems are found to be in the micro-molar range. Incorporation and delivery of hydrophobic drug using the formulated stable micelles was studied using curcumin as a model drug. The stability of curcumin was found to be very high in the micellar medium compared to the curcumin in aqueous medium. Drug loading efficiency was calculated and found to be 72% which can be comparable to the other micellar system. From the XRD analysis, the drug incorporation was confirmed. Surface morphology was analysed by using SEM technique. From the DSC thermograms, the stability of the curcumin loaded micelle was found to be higher than the unloaded micelle. Drug release profile confirmed a sustained release of drug which is vital for the cancer therapy. The cell viability and anticancer activity was also studied. From the overall results obtained, our formulated mPEG-Cholesterol micellar system found to be very promising and effective as drug delivery vehicles.
西安齐岳生物提供相关产品:
Pentacosadiynoic acid-MPEG
DMPE-PEG-Mal
DSPE-PEG-SEARYL-EB1(二硬脂酰基磷脂酰乙醇胺-聚乙二醇-PH响应性细胞穿膜肽)
DSPE-PEG-TMS
DMPE-PEG-Biotin
mPEG-Unsaturated Fatty Acid
DSPE-Biotin
DSPE-PEG-Estrogen
Angiopep-2 PEG
DSPE(Sodium salt)-PEG-NH2
DSPE-PEG-IA
Angiopep-2-PEG-DSPE
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