Introduction: Transforming Growth Factor-β (TGF-β) is an important growth factor in the wound healing process. The flavonoid substance in citrus peel is believed could induce TGF-β. In making substance based on natural ingre- dients, nanoparticles can be formed to increase their bioavailability. The aim of this study was to determine the effect of nanotransfersome of Citrus Peel Extract (Citrus aurantifolia Swingle) Towards TGF-β Expression by macrophage in Wound Healing of White Rat’s Labial Mucosa. Methods: The experimental study in vivo had been carried out with the thermal induction of white rat’s labial mucosa which were divided into four groups. Then each group was induced on the 3rd and 7th day. The groups consist of : negative control group (K), positive control group with triam- cinolone acetonide 0,1% (K+7), extract group (PA), nanotransfersome group (PB). Observation of TGF-β expression was carried out by immunohistochemistry staining process and light microscopy with magnification of 1000x. Re- sults: The data analysis using the one way ANOVA showed the highest average number of TGF-β expressions in the nanotransfersome group. Conclusion: Thus, it can be concluded that nanotransfersome of Citrus Peel Extract (Citrus aurantifolia Swingle) could be affected in increasing the number of TGF-β expression during wound healing in white rat’s labial mucosa.