Research On The Compound Liposome-in-gel Of Sinomenine Hydrochloride And Paeonol:preparation,characterization,in Vitro And Ex Vivo Release

In this paper,UV Dual Wavelength Method for the content determination of sinomenine hydrochloride and paeonol was established.The liposomes-in-gel of sinomenine hydrochloride and paeonol was prepared,and its appearance,morphology,potential and particle size distribution,liposomal encapsulation efficiency,IR spectrum,viscosity and p H value were characterized,respectively.Then the precision,repeatability and recovery of the samples were investigated,which provides the basis for the formulation design,the determination of process conditions and the establishment of analysis method in vivo.The compound liposomes containing sinomenine hydrochloride and paeonol were prepared by ethanol injection method with soybean phospholipid and cholesterol as raw materials.And the compound liposomes-in-gel formulation was prepared after natural swelling with hyaluronic acid.The release rates of the compound liposomes-in-gel and its control groups diffused in PBS media at the temperature of 37 ℃ in vitro and ex vivo were measured by ultraviolet dual wavelength spectrophotometry,respectively.The distribution of sinomenine hydrochloride and paeonol compound in viscera organs and tissues were investigated preliminarily.The results showed that the entrapment efficiency of compound liposomes was higher than that of single drug,which was 68.13% for sinomenine hydrochloride liposomes,69.3% for sinomenine hydrochloride in compound liposomes,61.72% for paeonol liposomes and 67.11% for paeonol in compound liposomes.Diffusion and transdermal release experiments showed that the release rate of compound preparation was higher than that of single drug preparation under the same temperature and diffusion medium,indicating that sinomenine hydrochloride combined with paeonol promoted drug loading and release rate.The antioxidative capacity of compound drugs for hydrogen peroxide and DPPH was determined,which provides a basis for further study of the antioxidant and anti-inflammatory ability of sinomenine hydrochloride and paeonol compound.The results of the drug distribution of tissue and viscera organs after two weeks drug administration by skin coating on the back of mice showed that the drugs were distributed in the brain,liver,spleen and joints.The contents of the brain and spleen were the largest.The joints and skin were the second,and the liver was the least.It indicated that the liposomes-in-gel could be permeated through the skin slowly and was mild and non-irritating,which was expected to be applied in the clinical practice of transdermal drug delivery for arthritis in the future.