Vignesh Kumar Suresh Kumar, Renuka Devi Ponnuswamy, Harish Saru, Hemananthan Eswaran
Department of Biotechnology, Anna University Regional Campus, Coimbatore, Tamil Nadu, India.
IET Nanobiotechnol. 2017 Feb;11(1):104-112. doi: 10.1049/iet-nbt.2016.0055.
Thymoquinone (TQ), a major bioactive compound of seeds has several therapeutic properties. The main drawback in bringing TQ to therapeutic application is that it has poor stability and bioavailability. Hence a suitable carrier is essential for TQ delivery. Recent studies indicate biodegradable polymers are potentially good carriers of bioactive compounds. In this study, polyethylene glycol (PEG) modified chitosan (Cs) nanocapsules were developed as a carrier for TQ. Aqueous soluble low molecular weight Cs and PEG was selected among different biodegradable polymers based on their biocompatibility and efficacy as a carrier. Optimisation of synthesis of nanocapsules was done based on particle size, PDI, encapsulation efficiency and process yield. A positive zeta potential value of +48 mV, indicating good stability was observed. Scanning electron microscope and atomic-force microscopy analysis revealed spherical shaped and smooth surfaced nanocapsules with size between 100 to 300 nm. The molecular dispersion of the TQ in Cs PEG nanocapsules was studied using X-ray powder diffraction. The Fourier transform infrared spectrum of optimised nanocapsule exhibited functional groups of both polymer and drug, confirming the presence of Cs, PEG and TQ. In vitro drug release studies showed that PEG modified Cs nanocapsules loaded with TQ had a slow and sustained release.
百里醌（TQ）是种子中的一种主要生物活性化合物，具有多种治疗特性。将TQ应用于治疗的主要缺点是其稳定性和生物利用度较差。因此，合适的载体对于TQ的递送至关重要。最近的研究表明，可生物降解聚合物可能是生物活性化合物的良好载体。在本研究中，开发了聚乙二醇（PEG）修饰的壳聚糖（Cs）纳米胶囊作为TQ的载体。基于其生物相容性和作为载体的功效，在不同的可生物降解聚合物中选择了水溶性低分子量Cs和PEG。基于粒径、多分散指数（PDI）、包封率和工艺产率对纳米胶囊的合成进行了优化。观察到+48 mV的正zeta电位值，表明稳定性良好。扫描电子显微镜和原子力显微镜分析显示纳米胶囊呈球形且表面光滑，尺寸在100至300 nm之间。使用X射线粉末衍射研究了TQ在Cs PEG纳米胶囊中的分子分散情况。优化后的纳米胶囊的傅里叶变换红外光谱显示了聚合物和药物的官能团，证实了Cs、PEG和TQ的存在。体外药物释放研究表明，负载TQ的PEG修饰的Cs纳米胶囊具有缓慢且持续的释放特性。
