ABSTRACT
The study evaluates the lipolysis rate and extent of type Ⅲ lipid formulations using testosterone undecanoate as a model drug after digestion with in vitro lipolysis model, and studies the digestive regularity with optical microscope and electrical conductivity. The results showed that for testosterone undecanoate type Ⅲ lipid formulations with castor oil as oil phase and Transcutol HP as latent solvent, the lipolysis rate and extent were increased with the increase of oil phase proportion and were decreased with excessive proportion of surfactant, in which can see liquid crystal phase during lipolysis process. The lipolysis rate of type ⅢB lipid preparations with different surfactant were ordered as Labrasol > Tween 80 > Cremophor EL, but the rate of type ⅢA is different in quick digestion phase and slow digestion phase. The lipolysis extent of type Ⅲ lipid formulations with different surfactant were ordered as Cremophor EL > Tween 80 > Labrasol. These may be related to the digestive effect of pancreatic lipase on different surfactants. This study implied that the lipolysis rate and extent of type Ⅲ lipid formulations are greatly influenced by the proportion of oil phase and surfactant, and the surfactant structure. These factors will affect the in vivo digestion and should be taken into account when screening type Ⅲ lipid formulations.
ABSTRACT
Aim To explore the therapeutic effects of main active compounds of panaxadiol ( PD ) in on Alzheimer’s disease ( AD) via network pharmacologi-cal analysis and Mmolecular docking. Methods A to-tal of 107 prescriptions for AD treatment were screened by using network pharmacology, screening for the high-est frequency of ginseng and its target for AD. Use mo-lecular docking technology was used to find components with the highest score for non-receptor tyrosine kinase ( FYN) docking. Then we successfully estimatedestab-lished AD cell model with overexpressinged APP pro-teins in vitro. Next,the cell viability was detected by MTT assay,the cell damage was detected by LDH as-say,the apoptosis and intracellular Ca2+concentration were detected by flow cytometry, and phosphorylated FYN protein expression was detected by Western blot detection of . phosphorylated FYN protein expression. Results Eighteen active components of Gginseng and 29 AD-related targets were screened by the method of network pharmacology. The results of molecular doc-king showed that PD had strong binding effects with FYN. The results showed that PD could increase the survival rate of cells,reduce the release of LDH,reduce apoptosis,and improve AD cells’ intracellular Ca2+o-verload and reduce the expression of FYN-Y416 pro-tein. Conclusion The experimental results of network pharmacology were are verified and the protective effect of PD on AD may be related to inhibition of FYN signa-ling pathway.