Preparation of sinomenine hydrochloride loaded nano flexible liposomes and their characteristics / 中草药

ABSTRACT

Objective: To study the preparation of sinomenine hydrochloride (SH) loaded nano flexible liposomes and investigate the mechanism of the flexible liposomes for enhanced in vitro transdermal drug delivery. Methods: The SH loaded nano flexible liposomes were prepared by film dispersion method, and the effects of concentration of phosphatidylcholine (PSC), cholesterol (CH), and propyleneglycol (PG) on the entrapment efficiency of SH were also investigated. The SH content was determined by HPLC. The physical property was evaluated by the atomic force microscope (AFM), transmission electron microscope (TEM) and photon correlation spectrometer (PCS). The side-by-side diffusion cells were used to evaluate transdermal delivery of SH by nano flexible liposomes. At the end of the transdermal experiment, the treated skin was carefully observed by scanning electron microscopy (SEM). Results: The SH loaded nano flexible liposomes were prepared by film dispersion method with the PSC (3%), CH (0.02%), and PG (25%); The SH entrapment efficiency was (66±2.3)%. The prepared nano flexible liposomes had a closed spherical or elliptical shape showed by AFM images, the TEM images appeared as multi-lamellar vesicles. The calculated mean size was (170±26) nm, the zeta potential values of -(43±3.4) mV. The SH loaded nano flexible liposomes caused the structure of stratum corneum (SC) layer disturbed and disordered the intercorneocyte domain wider, this increased the skin permeability of drug. Conclusion: The SH loaded nano flexible liposomes are obviously resulted in a remarkable enhancement of the SH transdermal drug delivery, which could act as a new nanodimensional vehicle for transdermal delivery of SH.