Silymarin-albumin nanoplex: Preparation and its potential application as an antioxidant in nervous system in vitro and in vivo

• Published in: International journal of pharmaceutics 2019-12, Vol.572, p.118824-118824, Article 118824
• Main Authors: Sohrabi, Mohammad Javad, Dehpour, Ahmad-Reza, Attar, Farnoosh, Hasan, Anwarul, Mohammad-Sadeghi, Nahid, Meratan, Ali Akbar, Aziz, Falah Mohammad, Salihi, Abbas, Shekha, Mudhir Sabir, Akhtari, Keivan, Shahpasand, Koorosh, Hojjati, Seyed Mohammad Masood, Sharifi, Majid, Saboury, Ali Akbar, Rezayat, Seyed Mahdi, Mousavi, Seyyedeh Elaheh, Falahati, Mojtaba
• Format: Article
• Language: English
• Subjects: Albumin; Animals; Antioxidant; Antioxidants - administration & dosage; Antioxidants - pharmacology; Apoptosis - drug effects; Cell Line, Tumor; Cell Survival - drug effects; Humans; In vitro; In vivo; Lipopolysaccharides - toxicity; Male; Nanoplex; Neuroblastoma - pathology; Oxidative Stress - drug effects; Particle Size; Rats; Rats, Wistar; Reactive Oxygen Species - metabolism; Serum Albumin, Human - chemistry; Silymarin; Silymarin - administration & dosage; Silymarin - pharmacology
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2019.118824

[Display omitted] In this study, we formulated silymarin-HSA nanoplex and assayed its ability to reduce LPS-induced toxicity in vitro and in vivo. Silymarin molecules were encapsulated into HSA nanoplex and the loading efficiency and characterization of fabricated nanoplex were performed by using HPLC, TEM, SEM, DLS, FTIR analysis, and theoretical studies. Afterwards, their protective effect against LPS (20 µg/ml) -induced toxicity in SH-SY5Y cells was investigated by MTT, ROS, and apoptosis assays. For in vivo experiments, rats were pre-treated with either silymarin or silymarin -HSA nanoplex (200 mg/kg) orally for 3 days and at third day received LPS by IP at a dose of 0.5 mg/kg, 150 min before scarification followed by SOD and CAT activity assay. The formulation of silymarin-HSA nanoplex showed a spherical shape with an average diameter between 50 nm and 150 nm, hydrodynamic radius of 188.3 nm, zeta potential of −26.6 mV, and a drug loading of 97.3%. In LPS-treated cells, pretreatments with silymarin-HSA noncomplex recovered the cell viability and decreased the ROS level and corresponding apoptosis more significantly than free silymarin. In rats, it was also depicted that, silymarin-HSA noncomplex can increase the SOD and CAT activity in brain tissue at LPS-triggered oxidative stress model more significantly than the free counterpart. Therefore, nanoformulation of silymarin improved its capability to reduce LPS-induced oxidative stress by restoring cell viability and elevation of SOD and CAT activity in vitro and in vivo, respectively. In conclusion, formulation of silymarin may hold a great promise in the development of antioxidant agents.