Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Mysuru 570015, Karnataka, India.
Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Mysuru 570015, Karnataka, India.
Eur J Pharm Sci. 2018 Sep 15;122:214-229. doi: 10.1016/j.ejps.2018.06.028. Epub 2018 Jun 30.
Respiratory infection is a viral spreading disease and a common issue, particularly in kids. The treatments are available but have so many limitations because the drawback of this disease is more morbidity and mortality in the severely immune compromised. Even, the phyto-constituent antibacterial drug Gingerol was selected to treat respiratory infection but it exhibits low bioavailability profile, less aqueous-solubility issue and most important is rapidly eliminated from the body. To overcome these problems, novel drug delivery (nanoparticle) based phytosome complexed with chitosan approach was implemented. In this research work, the phytosome (GP) was prepared by blending of gingerol with soya lecithin in organic solvent using anti-solvent precipitation technique and it was further loaded in the aqueous solution of chitosan to formulate the phytosome complexed with chitosan (GLPC). To optimize the formulations of gingerol, it was characterized for percentage yield, percentage entrapment efficiency, drug loading and particle size, physical compatibility studies etc. which demonstrated the confirmation of complex of GLPC with soya lecithin and chitosan. The % entrapment efficiency and % drug loading of GLPC was found (86.02 ± 0.18%, 08.26 ± 0.72%) and of GP (84.36 ± 0.42%, 08.05 ± 0.03%), respectively. The average particle size and zeta potential of GLPC and GP were 254.01 ± 0.05 nm (-13.11 mV), and 431.21 ± 0.90 nm (-17.53 mV), respectively which confirm the inhibition of particle aggregation by using chitosan in complex. The in vitro release rate of GP (86.03 ± 0.06%) was slower than GLPC (88.93 ± 0.33%) in pH 7.4 phosphate buffer up to 24 h by diffusion process (Korsmeyer Peppas model). The optimized GLPC and GP were shown irregular particle shapes & spherical and oval structures with smooth surface by SEM analysis. Furthermore, GLPC has shown the potent in vitro antioxidant activity, susceptible antibacterial activity and effective anti-inflammatory activity as compared to GP against stress, microbial infection and inflammation which were causable reason for the respiratory infections. GLPC has improved the significant bioavailability and also correlated the hematological values on rabbit blood against the incubation of microorganisms. Thus, the prepared nanoparticle based approach to deliver the gingerol, has the combined effect of chitosan and phytosome which shown better sustained-release profile and also prolonging the oral absorption rate of gingerol with effective antibacterial activity to treat respiratory infection.
呼吸道感染是一种病毒传播疾病，是一种常见问题，尤其是在儿童中。有治疗方法，但有很多限制，因为这种疾病的缺点是在严重免疫功能低下的患者中发病率和死亡率更高。甚至，选择植物成分姜辣素作为治疗呼吸道感染的抗菌药物，但它表现出低生物利用度、低水溶性问题，最重要的是它会从体内迅速消除。为了克服这些问题，采用了基于新型药物输送（纳米颗粒）的姜黄素与壳聚糖复合的方法。在这项研究工作中，通过在有机溶剂中使用抗溶剂沉淀技术将姜辣素与大豆卵磷脂混合来制备姜黄素磷脂复合物（GP），并将其进一步载入壳聚糖的水溶液中以形成与壳聚糖复合的姜黄素磷脂复合物（GLPC）。为了优化姜黄素的配方，对其进行了产率、包封率、载药量和粒径、物理相容性等方面的特征分析，证明了 GLPC 与大豆卵磷脂和壳聚糖的复合物的确认。GLPC 的包封率和载药量分别为（86.02±0.18%，08.26±0.72%）和（84.36±0.42%，08.05±0.03%），而 GP 的包封率和载药量分别为（84.36±0.42%，08.05±0.03%）。GLPC 和 GP 的平均粒径和 Zeta 电位分别为 254.01±0.05nm（-13.11mV）和 431.21±0.90nm（-17.53mV），证实了壳聚糖在复合物中的存在抑制了颗粒聚集。在 pH 7.4 磷酸盐缓冲液中，GP（86.03±0.06%）的体外释放速率比 GLPC（88.93±0.33%）慢，持续 24 小时，这是通过扩散过程（Korsmeyer Peppas 模型）实现的。通过 SEM 分析，优化后的 GLPC 和 GP 呈现不规则的颗粒形状和球形、椭圆形结构，表面光滑。此外，GLPC 表现出比 GP 更强的体外抗氧化活性、敏感的抗菌活性和有效的抗炎活性，这是导致呼吸道感染的应激、微生物感染和炎症的原因。GLPC 提高了显著的生物利用度，并与兔血中微生物孵育相关的血液学值相关。因此，基于纳米颗粒的方法来输送姜辣素，具有壳聚糖和姜黄素的联合作用，显示出更好的缓释特性，并延长姜辣素的口服吸收速率，具有有效的抗菌活性，可用于治疗呼吸道感染。
