Camptothecin derivatives have an obvious inhibitory effect on keloid fibroblasts proliferation. In order to improve the utilization rate of drug and provide a transdermal drug treat method, a non-alcoholic hyaluronic acid O/W type nanoemulsion without any chemical enhancers was made to encapsulate 10,11-methylenedioxycamptothecin (MD-CPT). We used transmission electron microscopy (TEM) and laser particle size instrument to survey the HA-GMS nanoemulsion morphology observation, and measured the particle size of (177.32±27.11) nm, the zetaelectric potential of -15.6±1.7, the PdI of 0.55±0.01 and the encapsulation efficiency of (77.85±1.29)%. Determination by MTT method was used to research the effect of biomaterial HA-GMS on HSF cells and HUVECs cells, and the relative cell viability range from 75%～95%, having good biocompatibility, and for keloid fibroblasts culture, growth inhibition rate was 28.2%.The transdermal effect of HA-GMS nanoemulsion carrying MD-CPT was obviously better than that of the control group (CPT MD-CPT ethanol solution), treating for 4 h, the cumulative drug permeation was (660.72±20.54) μg/cm² and (102.73±13.81) μg/cm² respectively, the HA-GMS nanoemulsion significantly increased the efficiency of MD-CPT through skin, which may provide a good drug delivery approach.