Determination of percutaneous absorption characteristics of Panax notoginseng saponins transfersomes by in vitro skin permeation method / 中草药

ABSTRACT

Objective: To establish the key conditions for the determination of percutaneous absorption of Panax notoginseng saponins (PNS) in transfersomes (TFS) by in vitro skin permeation method and clarify its percutaneous absorption characteristics. Methods: The film hydration-dispersion method was used to prepare PNS TFS and liposomes (LPS). Their physico-chemical properties were characterized. The drug content and sample volume of PNS TFS for in vitro skin permeation experiments were screened. The effects of vesicle type (TFS or LPS), size of the TFS, and formulation amount of sodium deoxycholate (DOC) on percutaneous permeation of PNS were investigated. Results: The TFS and LPS were mainly unilamellar vesicles with roundish shape and size of (121.2 ± 4.5) and (113.9 ± 2.9) nm, without gathering property. According to the cumulative permeated quantity (Qn) and steady-state percutaneous permeation rate (J) of the assayed ingredients, the appropriate PNS content in the TFS was 500 mg and sample volume was 0.5 mL. Compared with those of the LPS, the Qn values of each assayed component (ginseng saponin Rg1, ginseng saponin Rb1, ginseng saponin Re, PNS R1) in PNS of the TFS were high, and the J values of the assayed components in TFS were about 2-3 times of those in the LPS. The Qn and J values of the assayed components in the TFS with an average size of 120 nm were obviously higher than those of the assayed components in the TFS with an average size of 250 nm. The Qn and J values of the assayed components in PNS TFS with large amount of DOC were prominently higher than those containing small amount of DOC, and the increase ratios of different assayed components were different. Conclusion: In vitro skin permeation method is suitable for the determination of percutaneous absorption of PNS in TFS. The TFS promote drug percutaneous permeation stronger than the LPS and the promotion increases with an appropriate increase of the amount of DOC and decrease of vesicle size of the TFS.