CTG-loaded liposomes as an approach for improving the intestinal absorption of asiaticoside in Centella Total Glucosides

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Abstract

Centella Total Glucosides (CTG),obtained from Centella asiatica (L.), have been shown to possess a multitude of pharmacological activities, however, oral administeration of CTG failed to fulfill their therapeutic potentials due to the low bioavailability. In this study, the author prepared the liposomes encapsulated CTG using the ethanol injection method in order to enhance their intestinal absorption. The average particle size and the polydispersityindex(PDI) of CTG-loaded liposome in a batch are 137.0 nm and 0.283, and the CTG-loaded amounts in CTG-loaded liposomes were 0.177 mg mL−1 and the zeta potential of CTG-loaded lipsomes is −21.2 mV. The TEM images of CTG-loaded lipsomes showed that CTG-loaded liposomes are round and maintain high structural integrity, and their DSC thermograms indicated that CTG might be incorporated into the aqueous phase of DPPC to become more stable. The everted rat gut sac model was used to study the absorption characteristic of CTG-loaded solution in rat intestines. The cumulative absorption amount (Q) and the cumulative absorption percentage (P%) of asiaticoside in the CTG-loaded liposome was significantly higher than that in CTG (P < 0.05), both the steady-state infiltration rate (Jss, μg cm−2 s−1) and the permeability coefficient (Papp, cm s−1) of asiaticoside in CTG-loaded liposomes were significantly higher than those in CTG (P < 0.05), which revealed that the liposomes encapsulated CTG can promote the absorption of asiaticoside in the ileum of the rats by enhancing its transmembrane permeability. The above study will provide the experimental evidence and a reference for the development of the oral dosage forms of Centella total glucosides.

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