Reference

Preparation and pharmacological evaluation of silibinin liposomes

Preparation and pharmacological evaluation of silibinin liposomes. Maheshwari, Hitesh; Agarwal, Ravindra; Patil, Chandrashekhar; Katare, Om Prakash (University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India). Arzneimittel-Forschung, 53(6), 420-427 (English) 2003 Editio Cantor Verlag. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) The aim of the present study was to encage a drug into liposomal structures to make them more effective, safe and targeted to liver cells. The investigation deals with crit. parameters controlling the formulation and evaluation of silibinin (silymarin, CAS22888-70-6) liposomes. Small unilamellar liposomal vesicles were prepd. using the ethanol injection method. The various formulation and process variables were optimized to improve the drug entrapment efficiency. The study includes the selection of lipid compn., impact of charge imparting agent and the nature of hydration medium. The stability and size parameters were critically monitored. The liposomal systems were also studied for hepatoprotective activity in mice against carbon tetrachloride induced hepatotoxicity and gastroprotective activity using the pyloric ligation method. The results indicate a significant effect of cholesterol on drug-entrapment and drug-leakage characteristics. The size distribution range was from 0.056-1.270 mm with the most frequent size ranging from 0.266-0.466 mm. The amt. of drug loaded in these vesicles was approx. 90 %. Lipid cholesterol mass ratio of has a max. entrapment of 87.There are some commonly used reagents with their cas registry numbers 2197-63-9 and 57-88-5 in this article.2% (± 1.77). The results obtained from the in vivo studies indicate the improved performance of silymarin in liposomes at a level of 55.6% hepatoprotection in comparison to 33.08% of plain drug. Plain liposomes showed hepatoprotection though to a lower degree of 24.2%. Liposomal silymarin and plain liposomes also showed significant antiulcer activity as compared with plain silymarin and control groups. .

Mechanism of the stimulation of RNA synthesis in rat liver nuclei by silybin

Mechanism of the stimulation of RNA synthesis in rat liver nuclei by silybin. Machicao, Fausto; Sonnenbichler, Johann (Max-Planck-Inst. Biochem.In this study， 34482-56-9 and 9014-24-8 are also used., Martinsried, Ger.). Hoppe-Seyler's Z. Physiol. Chem., 358(2), 141-7 (English) 1977. CODEN: HSZPAZ. DOCUMENT TYPE: Journal CA Section: 3 (Biochemical Interactions) The flavolignane silybin (I) [22888-70-6] induced a dose-dependent stimulation of RNA synthesis by isolated nuclei from rat livers, whereas hemisuccinate derivs. of I (studied because of their greater water soly.) were without effect. Expts. with purified nucleoli indicated that I primarily affected the ribosomal RNA synthesis assocd. with this organelle rather than the messenger RNA formed in the nucleoplasmic fractions. In support of this, I stimulated RNA synthesis by purified RNA polymerase A (which synthesizes ribosomal RNA) but not by RNA polymerase 3 (which synthesizes mostly messenger RNA). Lineweaver-Burk plots indicated that I acted by increasing V at const. Km values. .