ABSTRACT
OBJECTIVE: To prepare and optimize the conditions of Sodium Aescinat micro-emulsion for injection. METHODS: Sodium Aescinat O/W micro-emulsion (soybean phospholipids + HS15/glycerin/medium chain triglycerides/water) was formulated guided by the pseudo-titration ternary phase diagram. RESULTS: Stable Sodium Aescinat micro-emulsion was obtained with medium chain triglycerides as oil, soybean phospholipids + HS15 (1:2) as emulsifier, glycerin as co-emulsifier, and a ratio of emulsifier and co-emulsifier (Km) between 2.00-3.75. CONCLUSION: Stable Sodium Aescinat micro-emulsion can be prepared with conditions described in this study.
Subject(s)
Emulsions/chemistry , Saponins/chemistry , Triterpenes/chemistry , Chemistry, Pharmaceutical , Glycerol , Phospholipids , Triglycerides , WaterABSTRACT
Improving efficacy of inflammation treatment by increasing drug delivery to the inflammatory sites is a challenging endeavor. N-formyl-methionyl-leucyl-phenylalanine (fMLP), the first discovered leukocyte chemotaxis peptide, is composed of formyl methionine, leucine and phenylalanine. It conjugates with formyl peptide receptors on the target cells with high receptor expression on the surface such as macrophages. With this in mind, we developed a novel fMLP-modified liposome (fMLP-LIP) for enhancing drug delivery to the inflammatory sites and resolving the systemic reaction issue with conventional anti-inflammatory drugs. Being a more stable and cheaper liposomal component than phospholipids, cholesterol (CHO) has been thoroughly investigated as an alternative anchor. In this study, fMLP was covalently conjugated with CHO with polyethylene glycol link to prepare the liposomes, cellular uptake of liposomes by differentiated human U937 cells was examined and cellular uptake experiment in vitro was employed to optimize fMLP-LIP prescription and investigate the uptake mechanism. An in vivo inflammatory model was established to evaluate the targeting performance of fMLP-LIP to inflammatory site. The in vitro and in vivo findings indicate that the fMLP ligands playing an important role in increasing drug delivery to inflammatory sites and fMLP-LIP as a promising anti-inflammatory drug carrier.
Subject(s)
Cholesterol/administration & dosage , Cholesterol/chemistry , Inflammation/drug therapy , Liposomes/administration & dosage , Liposomes/chemistry , N-Formylmethionine Leucyl-Phenylalanine/administration & dosage , N-Formylmethionine Leucyl-Phenylalanine/chemistry , Anti-Inflammatory Agents/administration & dosage , Anti-Inflammatory Agents/chemistry , Cell Differentiation/drug effects , Cell Line, Tumor , Chemistry, Pharmaceutical/methods , Drug Delivery Systems/methods , Humans , U937 CellsABSTRACT
OBJECTIVE: To establish a method of TLC identification for Dida commonly used in Tibetan medicine from different species. METHOD: With silica gel G as the stationary phase, and chloroform-methanol (40: 1) as mobile phase, oleanolic acid from different species of Dida was separated and identified. RESULT: Oleanolic acid was detected in 70 kinds of Dida derived from the Gentianaceae Swertia, Halenia, Gentianopsis, Lomatogonium, and Saxifragaceae saxifrage, except for the saxifrage, there are some differences among different genera or subjection. CONCLUSION: This TLC method can be used for identification of oleanolic acid in Dida from different species except saxifrage.
