School of Pharmaceutical Sciences, Guru Ghasidas Central University, Bilaspur- 495 009 (C.G.), India.
Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda-151 001 Punjab, India.
Curr Drug Deliv. 2021;18(3):369-380. doi: 10.2174/1567201817666200903171124.
To design D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit Seed Starch Nanoparticles (JFSSNPs) for site-specific delivery.
Liver cancer is the third leading cause of death in the world and the fifth most often diagnosed cancer. It is a major global threat to public health. Treatment of liver cancer with conventional method bears several side effects, thus to undertake these side effects as a formulation challenge, it is necessary to develop novel target-specific drug delivery system for the effective and better localization of drug into the proximity of target with restricting the movement of the drug in normal tissues.
To optimize and characterize the developed D-Mannose conjugated 5-Fluorouracil (5- FU) loaded Jackfruit Seed Starch Nanoparticles (JFSSNPs) for effective treatment of liver cancer.
5-FU loaded JFSSNPs were prepared and optimized formulations having higher encapsulation efficiency were conjugated with D-Mannose. These formulations were characterized for size, morphology, zeta potential, X-Ray Diffraction, and Differential Scanning Calorimetry. The potential of NPs was studied using in vitro cytotoxicity assay, in vivo kinetic studies, and bio-distribution studies.
5-Fluorouracil loaded NPs had a particle size between 336 to 802 nm with drug entrapment efficiency between 64.2 to 82.3%. In XRD analysis, 5-FU peak was diminished in the diffractogram, which could be attributed to the successful incorporation of the drug in amorphous form. DSC study suggests there was no physical interaction between 5-FU and Polymer. NPs showed sustained in vitro 5-FU release up to 2 hours. In vivo, mannose conjugated NPs prolonged the plasma level of 5-FU and assisted in the selective accumulation of 5-FU in the liver (vs. other organs spleen, kidney, lungs, and heart) compared to unconjugated one and plain drug.
In vivo, bio-distribution, and plasma profile studies resulted in a significantly higher concentration of 5-Fluorouracil liver, suggesting that these carriers are efficient, viable, and targeted carrier of 5-FU treatment of liver cancer.
设计 D-甘露糖偶联 5-氟尿嘧啶（5-FU）负载的菠萝蜜种子淀粉纳米粒（JFSSNPs）用于靶向递药。
肝癌是全球第三大死亡原因，也是第五大常见癌症。它是对全球公众健康的重大威胁。传统方法治疗肝癌存在多种副作用，因此，为了克服这些副作用，有必要开发新型的靶向药物传递系统，使药物有效且更好地定位于靶部位，并限制药物在正常组织中的移动。
优化并表征所开发的 D-甘露糖偶联 5-氟尿嘧啶（5-FU）负载的菠萝蜜种子淀粉纳米粒（JFSSNPs），以有效治疗肝癌。
制备 5-FU 负载的 JFSSNPs，并优化具有更高包封效率的制剂与 D-甘露糖偶联。对这些制剂进行粒径、形态、Zeta 电位、X 射线衍射和差示扫描量热法进行表征。通过体外细胞毒性试验、体内动力学研究和生物分布研究研究 NPs 的潜力。
负载 5-FU 的 NPs 的粒径在 336 至 802nm 之间，药物包封效率在 64.2%至 82.3%之间。在 XRD 分析中，5-FU 峰在衍射图中减弱，这可能归因于药物以无定形形式的成功掺入。DSC 研究表明，5-FU 和聚合物之间没有物理相互作用。NPs 表现出持续的体外 5-FU 释放长达 2 小时。在体内，甘露糖偶联的 NPs 延长了 5-FU 的血浆水平，并有助于 5-FU 在肝脏（与其他器官脾脏、肾脏、肺和心脏相比）的选择性积累，而不是未偶联的和普通药物。
体内生物分布和血浆谱研究导致肝脏 5-氟尿嘧啶浓度显著升高，表明这些载体是治疗肝癌的高效、可行和靶向 5-FU 载体。
