Khan Md Asad, Zafaryab Md, Mehdi Syed Hassan, Ahmad Irfan, Rizvi M Moshahid A
Genome Biology Lab, Department of Biosciences, Jamia Millia Islamia, New Delhi, 110025, India.
Genome Biology Lab, Department of Biosciences, Jamia Millia Islamia, New Delhi, 110025, India.
Int J Biol Macromol. 2016 Dec;93(Pt A):242-253. doi: 10.1016/j.ijbiomac.2016.08.050. Epub 2016 Aug 24.
In the present study the chitosan nanoparticles (CsNPs) and curcumin loaded chitosan nanoparticles (CLCsNPs) were synthesized by tripolyphosphate (TPP) cross-linking method. The nanoparticles were prepared within a zone of appropriate chitosan and TPP concentrations. The average size of CsNPs and CLCsNPs were approximately 189±11.8nm and 197±16.8nm, exhibited a zeta potential of +76±5.6mV and +71±6.4mV respectively and drug entrapment efficiency was ≈85%. The CLCsNPs and CsNPs were further characterized by different physicochemical methods like transmission electron microscopy (TEM), dynamic light scattering (DLS), HPLC, MALDI-TOF, FT-IR, XRD and UV-vis Spectroscopy. In vitro studies revealed a fast release of ≈35% at pH 5 and ≈25% at pH 7.4 of the drug during the first 3h, followed by controlled release of curcumin over a period of 120h and sustained anti-proliferative activity of the drug in a dose and time dependent manner of CLCsNPs and combination with methyl jasmonate. The higher cytotoxicity effect of CLCsNPs may be due to their higher cellular uptake as compared to curcumin. Chitosan nanoparticles were not only stable but also a nontoxic. Our data suggested that curcumin loaded nanoformulations, therefore, might be promising candidates in cancer therapy.
在本研究中，通过三聚磷酸钠（TPP）交联法合成了壳聚糖纳米颗粒（CsNPs）和载姜黄素壳聚糖纳米颗粒（CLCsNPs）。在合适的壳聚糖和TPP浓度范围内制备纳米颗粒。CsNPs和CLCsNPs的平均粒径分别约为189±11.8nm和197±16.8nm，ζ电位分别为+76±5.6mV和+71±6.4mV，药物包封率约为85%。通过透射电子显微镜（TEM）、动态光散射（DLS）、高效液相色谱（HPLC）、基质辅助激光解吸电离飞行时间质谱（MALDI-TOF）、傅里叶变换红外光谱（FT-IR）、X射线衍射（XRD）和紫外可见光谱等不同的物理化学方法对CLCsNPs和CsNPs进行了进一步表征。体外研究表明，在最初3小时内，药物在pH 5时快速释放约35%，在pH 7.4时释放约25%，随后姜黄素在120小时内持续释放，并且CLCsNPs中的药物以剂量和时间依赖性方式具有持续的抗增殖活性，并与茉莉酸甲酯联合使用。与姜黄素相比，CLCsNPs具有更高的细胞毒性作用可能是由于其更高的细胞摄取率。壳聚糖纳米颗粒不仅稳定而且无毒。因此，我们的数据表明，载姜黄素纳米制剂可能是癌症治疗中有前景的候选药物。
