The dissolving microneedles have gradually become a popular way of transdermal delivery. This paper mainly introduces all the application areas of dissolving microneedles loaded with small molecule compounds, which are divided into functional categories, treatment, diagnosis and popular cosmetology on the market nowadays.Combining with the specific microneedles preparation examples, the research progress is described by analysing of the small molecule compounds loaded in dissolving microneedle are superior to traditional pharmaceutical preparations from the properties of different compounds in various application fields. It is concluded that compounds loaded in dissolving microneedles should possess the characteristics, such as high activity , high stability, the use of traditional skin preparations can not achieve the desired effect, high additional value and combining with the characteristics of the microneedles, which provides reference for other scholars to further study the small molecule compounds loaded in dissolving microneedles. Finally, the current problems of dissolving microneedles have been put forward and the future trend of dissolving microneedles is forecasted.