Prakash Upputuri Ravi Theaj, Azad Mandal Abul Kalam
School of Bio Sciences and Technology, VIT University, Vellore-632014, Tamil Nadu, India.
Iran J Biotechnol. 2017 Dec 29;15(4):277-283. doi: 10.15171/ijb.1322. eCollection 2017.
Green tea polyphenols (GTP) are known to have several health benefits. In spite of these benefits, its application as a therapeutic agent is limited due to some of its limitations such as stability, bioavailability, and biotransformation. To overcome these limitations, liposomal nanoparticles have been used as a carrier of the GTP. Encapsulation of GTP to the liposomal nanoparticles in order to achieve a sustained release of the GTP and to determine the drug release kinetics and the mechanism of the release. GTP encapsulated liposomal nanoparticles were prepared using phosphatidyl choline and cholesterol. The synthesized particles were characterized for their particle size and morphology. release studies were carried out, followed by drug release kinetics, and determining the mechanism of release. , antioxidant assay was determined following 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. Atomic force microscope (AFM) and high resolution scanning electron microscope (HR SEM) images showed spherical particles of the size of 64.5 and 252 nm. An encapsulation efficiency as high as 77.7% was observed with GTP concentration of 5 mg.mL. release studies showed that the loading concentrations of GTP were independent to the cumulative percentage of the drug release. GTP release by varying the pH and temperature showed a direct correlation between the release parameter and the percentage of drug release. The higher the pH and temperature, the higher was the percentage of the drug release. The release data showed a good correlation with Zero order kinetics and the mechanism of the release being anomalous mode. Radical scavenging activity of the released GTP showed a potent scavenging activity. GTP encapsulated liposomal nanoparticles could be used as a delivery vehicle for achieving a sustained release.
绿茶多酚(GTP)具有多种健康益处。尽管有这些益处,但由于其稳定性、生物利用度和生物转化等一些局限性,其作为治疗剂的应用受到限制。为了克服这些局限性,脂质体纳米颗粒已被用作GTP的载体。将GTP包裹到脂质体纳米颗粒中,以实现GTP的持续释放,并确定药物释放动力学和释放机制。使用磷脂酰胆碱和胆固醇制备了包裹GTP的脂质体纳米颗粒。对合成的颗粒进行了粒径和形态表征。进行了释放研究,随后进行了药物释放动力学研究,并确定了释放机制。按照2,2-二苯基-1-苦基肼基(DPPH)法进行了抗氧化测定。原子力显微镜(AFM)和高分辨率扫描电子显微镜(HR SEM)图像显示尺寸为64.5和252 nm的球形颗粒。在GTP浓度为5 mg.mL时,观察到高达77.7%的包封效率。释放研究表明,GTP的负载浓度与药物释放的累积百分比无关。通过改变pH和温度进行的GTP释放显示释放参数与药物释放百分比之间存在直接相关性。pH和温度越高,药物释放百分比越高。释放数据与零级动力学具有良好的相关性,释放机制为异常模式。释放的GTP的自由基清除活性显示出强大的清除活性。包裹GTP的脂质体纳米颗粒可作为实现持续释放的递送载体。