RESUMEN
3-succinyl-30-stearyl glycyrrhetinic acid (Suc-GLAOSt) was synthesized as a targeting molecule, and incorporated in ordinary to liposomes (LP) to prepare a liposome surface-modified with glycyrrhetinic acid (LP-GLA), which could bind to the hepatocyte through the specific binding site of glycyrrhetinic acid (GLA) on the surface of rat cellular membrane. The maximal molar ratio of Suc-GLAOSt to total lipids in LP-GLA was 1:10. Calcein loaded liposome (Cal-LP) and calcein loaded LP-GLA (Cal-LP-GLA) were prepared by an ethanol injection method. The average diameter of Cal-LP and Cal-LP-GLA was 65 nm +/- 16 nm and 68 nm +/- 21 nm, respectively. The characteristics of cellular uptake of the two types of liposome were investigated through cellular uptake and competitive inhibition experiments. The uptake of Cal-LP-GLA by rat hepatocytes was markedly higher (3.3-fold) than that of Cal-LP (P < 0.01). The uptake of Cal-LP-GLA was inhibited, but the uptake of Cal-LP was not influenced by adding extraneous GLA. LP-GLA may be internalized by hepatocytes via the specific binding site, and can be used as a novel and promising carrier for targeting drug delivery to hepatocytes.
Asunto(s)
Ácido Glicirretínico/farmacocinética , Hepatocitos/metabolismo , Animales , Células Cultivadas , Relación Dosis-Respuesta a Droga , Portadores de Fármacos , Fluoresceínas/química , Ácido Glicirretínico/administración & dosificación , Indicadores y Reactivos , Cinética , Liposomas , Espectroscopía de Resonancia Magnética , Masculino , Microscopía Electrónica de Transmisión , Tamaño de la Partícula , Ratas , Ratas Wistar , Propiedades de SuperficieRESUMEN
OBJECTIVE: To optimize formulation of tanshinone II(A)-loaded PLGA nanoparticles and compare the difference of two methods in preparation and quality of nanoparticles. METHOD: The two methods were nanoprecipitation method and emulsion-evaporation method. Single factor experiments and central composite design and response surface method were used to optimize the formulation of nanoparticles. The nanoparticles were characterized at size, morphology, entrapment efficiency, drug loading, drug recovery rate, crystallinity and drug release in vitro. RESULT: The mean diameters were 225 nm and 183 nm, the entrapment efficiency were 95.49% and 87.99%, the drug loading were 2.03% and 0.16%, and the drug recovery rates were 38.42% and 17.59% respectively for nanoprecipitation method and emulsion-evaporation method. CONCLUSION: Nanoprecipitation method was better than emulsion-evaporation method for preparation of tanshinone II(A)-loaded PLGA nanoparticles.
Asunto(s)
Ácido Láctico/química , Nanopartículas/química , Fenantrenos/aislamiento & purificación , Ácido Poliglicólico/química , Polímeros/química , Salvia miltiorrhiza/química , Tecnología Farmacéutica/métodos , Abietanos , Precipitación Química , Cristalización , Emulsiones , Tamaño de la Partícula , Fenantrenos/química , Raíces de Plantas/química , Plantas Medicinales/química , Copolímero de Ácido Poliláctico-Ácido Poliglicólico , Control de Calidad , VolatilizaciónRESUMEN
OBJECTIVE: Study the characteristics of absorption and separation of traditional Chinese medicine compound prescription using macroporous resin. METHOD: Study the techniquecs and characteristics of absorption and separation of a sample by macroporous resin, which is composed of coptis root, rhubarb and common anemarrhena rhizome, containing alkaloid, anthraquinone and saponin. RESULT: It is proved by qualitative and quantitative researches studies that after absorbed and separated by optimized technics process, most prime effective components or section fractions in traditional Chinese medicine compound prescription can be reserved maintained. CONCLUSION: If the techniquecs of separation is properly designed, the same kind of macropore resin can absorbd and separate various effective components or section in traditional Chinese medicine compound prescription which have with different chemical structures efficiently.