Melasma is a chronic and unsightly dermal pathology responsible for a high demand for aesthetic treatments. It can be caused by excess melanin in the epidermis, commonly exhibiting symmetrically distributed brown or gray macules, with a predilection for the face. It is more common in women than men, usually begins between the ages of 20 and 40, and can lead to considerable embarrassment and distress. The present work aims to evaluate the effectiveness of microneedling associated with drug delivery in the treatment of this dysfunction. This is a narrative bibliographical review whose research was carried out from the descriptors “Melasma”, “microneedling”, “drug delivery system” and “treatment”. The Boolean operator "AND" was used in the PubMed and Scielo databases; including works in Portuguese and English published in the last 10 years, excluding bibliographic reviews. Isolated microneedling can lighten skin spots in patients with recalcitrant melasma. The trauma caused by the procedure should be modest and the use of whitening actives and sunscreen after the procedure becomes mandatory. Despite some proposed theories, the exact mechanism of skin lightening is still not well established. The effect of the technique drug delivery system tends to flexible results. The findings of this review confirm positive results, especially when associated with whitening actives, which considerably increase skin rejuvenation, the treatment of scars and hyperchromia (melasma). New controlled studies are needed to clarify the mechanism of action of microneedling in melasma.