Evaluation of hybrid liposomes-encapsulated silymarin regarding physical stability and in vivo performance

• Published in: International journal of pharmaceutics 2006-08, Vol.319 (1), p.121-129
• Main Authors: El-Samaligy, Mohamed S., Afifi, Nagia N., Mahmoud, Enas A.
• Format: Article
• Language: English
• Subjects: Administration, Buccal; Alanine Transaminase - blood; Amines - chemistry; Animals; Antioxidants - administration & dosage; Antioxidants - chemistry; Antioxidants - pharmacology; Antioxidants - therapeutic use; Aspartate Aminotransferases - blood; Biological and medical sciences; Carbon Tetrachloride; Chemical and Drug Induced Liver Injury; Chemistry, Pharmaceutical; Cholesterol - chemistry; Drug Stability; Drug Storage; Evaluation Studies as Topic; General pharmacology; Hepatoprotective activity; Hybrid liposomes; Liposomes; Liver - drug effects; Liver - metabolism; Liver - pathology; Liver Diseases - enzymology; Liver Diseases - prevention & control; Medical sciences; Oxidative Stress - drug effects; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Phosphatidylcholines - chemistry; Polysorbates - chemistry; Rats; Silybum marianum; Silymarin; Silymarin - administration & dosage; Silymarin - chemistry; Silymarin - pharmacology; Silymarin - therapeutic use; Stability; Temperature
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2006.04.023

Silymarin, a known standardized extract obtained from seeds of Silybum marianum is used in treatment of liver diseases of varying origins. Aiming at improving its poor bioavailability from oral products, silymarin hybrid liposomes are introduced in this work for buccal administration after investigating their stability and in vivo hepatoprotective efficiency. Silymarin loaded hybrid liposomes composed of lecithin (L), cholesterol (Ch), stearyl amine (SA) and Tween 20 (T20) in molar ratio of (9:1:1:0.5) were prepared. Their stability upon storage was studied at 4 °C and at ambient conditions. Stored samples were analyzed for percent encapsulation, drug release, particle size, turbidity measurement and visual changes. Characterization of the blend between phospholipid and silymarin was done using FT-IR and DSC which indicated a possible interaction. The stabilized formula of silymarin hybrid liposomes was evaluated upon buccal administration regarding its hepatoprtective activity against carbon tetrachloride-induced oxidative stress in albino rats. The degree of protection was measured using biochemical parameters like serum glutamic oxalacetate transaminase (SGOT) and serum glutamic pyruvate transaminase (SGPT). The introduced silymarin hybrid liposomes produced a significant decrease in both transaminase levels when challenged with CCl 4 (intraperitonially) in comparison with orally administered silymarin suspension. This improvement was also confirmed histopathologically.