Amresh Gupta, Agarwal Vipin Kumar, Rao Chandana Venkateswara
Department of Pharmacognosy, Faculty of Pharmacy, Uttar Pradesh University of Medical Sciences, Saifai, Etawah, Uttar Pradesh, India.
Department of Pharmaceutics, Invertis Institute of Pharmacy, Invertis University, NH 24 Lucknow Bareilly Highway, Bareilly, Uttar Pradesh, India.
J Tradit Complement Med. 2017 Jun 3;8(1):164-169. doi: 10.1016/j.jtcme.2017.05.005. eCollection 2018 Jan.
Self microemulsifying formulation is an approach used for enhancing the bioavailability of poorly soluble molecules due to their lipidic nature and small particle size. The objective of the present study was to evaluate the hepatoprotective activity of poorly soluble hydroxy- and polyhydroxy-organic phytomolecules rich leaves extract in modern formulation i.e. "Self microemulsifying System". Different doses of SME (Self microemulsifying) formulation of leaves extract were evaluated for the hepatoprotective activity against carbon tetrachloride induced liver toxicity in rats. The parameters evaluated were (a) biochemical parameters like serum enzymes: aspartate aminotransferase (AST), serum glutamate pyruvate transaminase (ALT), serum alkaline phosphatase (ALP) and total bilirubin (b) liver antioxidant parameters as estimation of Lipid peroxidation (LPO), catalase (CAT), Superoxide dismutase (SOD) activity and concentration of reduced glutathione (GSH). Oral administration of SME formulation provided the significant protection in marker enzyme of treated group at 100 mg/kg, p.o. as AST (P < 0.001), ALT (P < 0.001), ALP (P < 0.001) and total bilirubin (P < 0.001) comparable to the group treated with silymarin. Treatment with SME formulation at the doses of 100 mg/kg, p.o. significantly prevented the rise in levels of LPO significantly (P < 0.001). The GSH, SOD and CAT contents had significantly (P < 0.001) increased in SME formulation treated groups whereas carbon tetrachloride intoxicated group had shown significant decrease in these parameters compared to control group. Formulation at the dose 100 mg/kg, p.o. has shown maximum protection which was almost comparable to those of the normal control and standard. The histological observations further uphold the results for hepatoprotective activity.
自微乳化制剂是一种用于提高难溶性分子生物利用度的方法,这归因于其脂质性质和小粒径。本研究的目的是评估富含难溶性羟基和多羟基有机植物分子的叶提取物在现代制剂即“自微乳化系统”中的肝保护活性。评估了不同剂量的叶提取物自微乳化(SME)制剂对四氯化碳诱导的大鼠肝毒性的肝保护活性。评估的参数包括:(a)生化参数,如血清酶:天冬氨酸转氨酶(AST)、血清谷氨酸丙酮酸转氨酶(ALT)、血清碱性磷酸酶(ALP)和总胆红素;(b)肝脏抗氧化参数,如脂质过氧化(LPO)的测定、过氧化氢酶(CAT)、超氧化物歧化酶(SOD)活性以及还原型谷胱甘肽(GSH)的浓度。口服SME制剂在100 mg/kg口服剂量下对治疗组的标志物酶提供了显著保护,AST(P < 0.001)、ALT(P < 0.001)、ALP(P < 0.001)和总胆红素(P < 0.001),与水飞蓟宾治疗组相当。100 mg/kg口服剂量的SME制剂治疗可显著预防LPO水平的升高(P < 0.001)。SME制剂治疗组的GSH、SOD和CAT含量显著增加(P < 0.001),而与对照组相比,四氯化碳中毒组的这些参数显著降低。100 mg/kg口服剂量的制剂显示出最大保护作用,几乎与正常对照组和标准组相当。组织学观察进一步支持了肝保护活性的结果。