Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy and Drug Technology, Heliopolis University, Cairo, Egypt.
Pharmaceutical Nano-Technology Lab., Medical Applications of Laser Department, Niles, Cairo University, Cairo, Egypt.
Int J Nanomedicine. 2019 Jul 11;14:5073-5085. doi: 10.2147/IJN.S210484. eCollection 2019.
To potentiate the anticancer activity of curcumin (CUR) by improving its cell penetration potentials through formulating it into nanostructured lipid carriers (NLCs) and using the prepared NLCs in photodynamic therapy.
A 3×4 factorial design was used to obtain 12 CUR-NLCs using two factors on different levels: (1) the solid lipid type at four levels and (2) the solid to liquid lipid ratio at three levels. Olive oil, Tween 80 and lecithin were chosen as liquid lipid, surfactant and co-surfactant, respectively. CUR-NLCs prepared by high shear hot homogenization method were evaluated by determination of particle size (PS), polydispersity index, zeta potential (ZP), entrapment efficiency percent, drug loading percent and in vitro drug release. Optimization was based on the evaluation results using response surface modeling (RSM). Optimized formulae were tested for their in vitro release pattern and for dark and photo-cytotoxic anticancer activity on breast cancer cell line in comparison to free CUR.
Evaluation tests showed the appropriateness of NLCs prepared from glyceryl monooleate and Geleol™ helped choosing two optimized formulae, PE3 and GE3. PE3 (prepared using glyceryl monooleate) showed enhanced release rates compared to GE3 (prepared from Geleol) and superior cytotoxic anticancer activity compared to both GE3 and free CUR under both light and dark conditions. The small mean PS, spherical shape as well as the negative ZP enhanced the internalization of the NLCs within cells. Modulation and inhibition of P-glycoprotein expression by glyceryl monooleate synergized the cytotoxic activity of CUR.
CUR loading in NLCs enhanced its cell penetration and cytotoxic anticancer properties both in dark and in light conditions.
通过将姜黄素（CUR）制成纳米结构脂质载体（NLC）来提高其细胞穿透潜力，从而增强其抗癌活性，并将制备的 NLC 应用于光动力疗法。
使用 3×4 析因设计，使用两种因素的不同水平获得 12 种 CUR-NLC：（1）固体脂质有 4 个水平，（2）固体与液体脂质的比例有 3 个水平。橄榄油、吐温 80 和卵磷脂分别被选为液体脂质、表面活性剂和助表面活性剂。采用高剪切热熔匀化法制备 CUR-NLC，通过测定粒径（PS）、多分散指数、Zeta 电位（ZP）、包封效率百分率、载药量百分率和体外药物释放来评价 CUR-NLC。基于响应面建模（RSM）的评价结果进行优化。对优化的配方进行体外释放模式测试，并与游离 CUR 进行体外光毒性和抗癌活性测试。
评价试验表明，由甘油单油酸酯和 Geleol™ 制备的 NLC 合适，有助于选择两种优化配方，PE3 和 GE3。与 GE3（由 Geleol 制备）相比，PE3（由甘油单油酸酯制备）显示出增强的释放速率，与 GE3 和游离 CUR 相比，在光照和黑暗条件下均显示出更好的细胞毒性抗癌活性。较小的平均 PS、球形形状以及负 ZP 增强了 NLC 在内化细胞内的内化。甘油单油酸酯对 P-糖蛋白表达的调节和抑制协同增强了 CUR 的细胞毒性。
CUR 负载于 NLC 中，可增强其在黑暗和光照条件下的细胞穿透和抗癌活性。
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