Bhatt Himanshu, Rompicharla Sri Vishnu Kiran, Komanduri Neeraja, Aashma Shah, Paradkar Sateja, Ghosh Balaram, Biswas Swati
Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Shameerpet, Hyderabad, Telangana 500078, India.
Curr Drug Deliv. 2018;15(9):1271-1283. doi: 10.2174/1567201815666180503120113.
Solid lipid nanoparticles (SLNs) represent an affordable, easily scalable, stable and biocompatible drug delivery system with a high drug to lipid ratio which also improves solubility of poorly soluble drugs.
SLNs were developed by using glyceryl monostearate as the single lipid in the presence of surfactant Poloxamer 188 and evaluated the efficiency of SLNs to load the therapeutic cargo, curcumin (CUR).
The nano-formulation was optimized by Quality by Design approach to understand the effect of various process parameters on various quality attributes, including drug loadability, particle size and polydispersity. The nanoparticles were characterized using Differential scanning calorimetry (DSC), Fourier Transform Infra-red Spectroscopy (FT-IR) and X-Ray Diffraction (XRD) analysis. These novel SLNs were evaluated for in-vitro anticancer activity using breast adenocarcinoma cells (MDA-MB-231).
The optimized formulation had a particle size of 226.802±3.92 nm with low polydispersity index of 0.244±0.018. The % encapsulation of CUR into SLNs was found to be 67.88±2.08 %. DSC, FT-IR and XRD confirmed that the CUR was encapsulated stably into the lipid matrix, thereby improving the solubility of the drug. CUR-SLN showed sustained drug release in comparison to the free CUR solution. CUR-SLNs exhibited higher cellular uptake in human breast adenocarcinoma cells compared to free CUR at both 1 and 4 h time points. CUR-SLNs demonstrated decreased cell viability (43.97±1.53%) compared to free CUR (59.33±0.95%) at a concentration of 50 µg/mL after 24 h treatment. Furthermore, the treatment of MDA-MB-231 cells with CUR-SLNs for 24 h induced significantly higher apoptosis (37.28±5.3%) in cells compared to the free CUR (21.06±0.97%).
The results provide a strong rationale for further exploration of the newly developed CUR-SLN to be utilized as a potent chemotherapeutic agent in cancer therapy.
固体脂质纳米粒（SLNs）是一种经济实惠、易于扩大规模、稳定且具有生物相容性的药物递送系统，药物与脂质比例高，还能提高难溶性药物的溶解度。
以单硬脂酸甘油酯为单一脂质，在表面活性剂泊洛沙姆188存在的情况下制备SLNs，并评估其负载治疗药物姜黄素（CUR）的效率。
采用质量源于设计方法对纳米制剂进行优化，以了解各种工艺参数对包括载药量、粒径和多分散性在内的各种质量属性的影响。使用差示扫描量热法（DSC）、傅里叶变换红外光谱法（FT-IR）和X射线衍射（XRD）分析对纳米颗粒进行表征。使用乳腺腺癌细胞（MDA-MB-231）对这些新型SLNs的体外抗癌活性进行评估。
优化后的制剂粒径为226.802±3.92 nm，多分散指数低，为0.244±0.018。发现CUR在SLNs中的包封率为67.88±2.08%。DSC、FT-IR和XRD证实CUR稳定地包封在脂质基质中，从而提高了药物的溶解度。与游离CUR溶液相比，CUR-SLN表现出持续的药物释放。在1小时和4小时时间点，CUR-SLNs在人乳腺腺癌细胞中的细胞摄取均高于游离CUR。在50 μg/mL浓度下处理24小时后，CUR-SLNs的细胞活力（43.97±1.53%）低于游离CUR（59.33±0.95%）。此外，与游离CUR（21.06±0.97%）相比，用CUR-SLNs处理MDA-MB-231细胞24小时可显著诱导更高的细胞凋亡（37.28±5.3%）。
这些结果为进一步探索新开发的CUR-SLN作为癌症治疗中的有效化疗药物提供了有力依据。
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