Since 5‐ALA exists as a charged zwitterion and HA is rich of negative charges under physiological pH, we propose to utilize cationic CDG2 in combination with HA to encapsulate 5‐ALA with an aid of electrostatic interaction for efficient transdermal delivery and photodynamic therapy in attempt not only to ablate local melanoma, but also to exert immunostimulatory effect to regress the distant metastasis. Here, TGFBI is linked to melanoma.