Preparation of Injectable Sinomenine-loaded Microemulsion-based Thermosensitive Gel
In order to overcome the shortcomings of sinomenine(1),such as poor water-solubility,short half-life,low oral bioavailability,the oil-in-water(O/W)1-loaded microemulsion(1-ME)was prepared successfully by aqueous titration method via drawing pseudo-ternary phase diagrams.The prepared 1-ME with excellent stability was light yellow homogeneous and transparent with obvious Tyndall phenomenon,and the particle size was 150～180 nm,which met the particle size requirements of microemulsions.Then,1-ME was further compounded with poloxamer(P407,P1 88)hydrogel to obtain the injectable 1-ME-based thermosensitive hydrogels.Furthermore,the formulation of 1-ME-based thermosensitive hydrogels was optimized with the sol-gel transition temperature(Tsol-gel)as the evaluation index.The optimized formulation was as follows:the mass ratio of P407 to P188 was 17∶4,and the mass ratio of Poloxamer hydrogel to 1-ME was 8∶2.The Tsol-gel of 1-ME-based thermosensitive hydrogels was(35.2±1.33)℃,which was match to the normal physiological temperature.Finally,the in vitro release performances revealed that the cumulative release rate of 1-ME-based thermosensitive hydrogels at 48 h was(66.7±6.2)％,which showed a satisfactory long-acting and sustained-release effect in comparison with 1-ME.In conclusion,the prepared 1-ME-based thermosensitive hydrogels was expected to be used as a novel drug delivery system of intra-articular injection for the rheumatoid arthritis treatment.
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