文獻：兩親性mPEG-膽固醇共軛物的合成、膠束化及其在姜黃素遞送中的應用

鏈接：http://dspace.nitrkl.ac.in/dspace/handle/2080/3725

作者：普拉丹、艾斯瓦婭·帕特爾、薩比塔

節選：

癌癥是全球*致命的疾病，至今仍未得到根治。眾多研究人員和科學家已經提出了幾種方法來根除癌癥，即聯合*方式和引入多種藥物載體，如脂質體、納米顆粒、膠束等。其中，聚合物膠束作為藥物遞送載體因其穩定性更高、CMC 更低、溶解性更好、粒徑小和生物相容性更好而備受關注。為了將 PEG 基膠束配制成疏水藥物載體，我們通過縮合法合成了兩親性 mPEG-膽固醇共軛物。使用 1H NMR、FTIR、HRMS 光譜分析對合成的聚合物表面活性劑進行了表征。通過紫外可見光和熒光法分析了這些合成表面活性劑的膠束化行為。發現上述體系的 CMC 在微摩爾范圍內。以姜黃素為模型藥物，研究了使用配制的穩定膠束進行疏水藥物的摻入和遞送。與水介質中的姜黃素相比，姜黃素在膠束介質中的穩定性非常高。計算得出的藥物負載效率為 72%，可與其他膠束體系相媲美。通過 XRD 分析證實了藥物的摻入。利用 SEM 技術分析了表面形貌。從 DSC 熱分析圖可以看出，負載姜黃素的膠束的穩定性高于未負載的膠束。藥物釋放曲線證實了藥物的持續釋放，這對癌癥*至關重要。還研究了細胞活力和*癌活性。從獲得的總體結果來看，我們配制的 mPEG-膽固醇膠束體系被發現是一種非常有前途且有效的藥物遞送載體。

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.

西安齊岳生物提供相關產品：

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響應性細胞穿膜肽)

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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