Vitamin A or retinol is a proven cosmetic ingredient for the treatment of photoaged skin. It has been incorporated in various product forms which are used in daily skin care regimens. Retinol as an oil form can offer unique aesthetics and physicochemical characteristics. The relative polarity between skin, retinol, and emollient ratios allows for controlled biodelivery of retinol. Retinol induced-bioactivity could be enhanced, and its irritation potential could be mitigated by controlling its delivery rate to skin. Thus, an optimized retinol oil formulation enabling a controlled release of retinol drives better efficacy and lower irritation. An advanced retinol oil was developed through evaluation of the relationship between its composition versus its bioactivity and irritation potential by using clinically correlated standardized biomarker gene expression analysis. This retinol oil composition delivered superior bioactivity with a low irritation potential profile in comparison with other marketed retinol oil-based products. When used as part of a retinol-based skin care regimen, this retinol oil composition delivered twice the bioactivity of retinol in vitro. Moreover, a single center, open-label, clinical trial was conducted to evaluate its overall effectiveness as a daily treatment for photoaged skin. 35 healthy female subjects were enrolled with moderate photodamage of the face and moderate to severe facial fine wrinkles in the periocular area. This advanced retinol oil composition was well tolerated and resulted in significant and sustained improvements versus baseline in the appearance of fine lines and wrinkles and other antiaging parameters evaluated. Thus, this anti-aging retinol oil, supported with scientific testing and clinical assessments, constitutes a novel, unique, and superior retinol form that delivers improvements in facial wrinkles as early as 1 week, as well as sustained improvements in cutaneous skin parameters that address the needs of subjects with signs of skin aging and photodamage.