| Summary: | This paper reports the permeation-enhancing properties and safety of different chemical permeation enhancers (CPEs) on the topical delivery of vitamin C (VC) and its derivatives. A literature search using search keywords or phrases was done in PubMed<sup>®</sup>, ScienceDirect, and MEDLINE databases. The calculated Log <i>P</i> (cLog <i>P</i>) values were referenced from PubChem and the dermal LD<sub>50</sub> values were referenced from safety data sheets. Thirteen studies described the permeation-enhancing activity of 18 identified CPEs in the topical delivery of VC. Correlation analysis between ER and cLog <i>P</i> values for porcine (<i>r</i> = 0.114) and rabbit (<i>r</i> = 0.471) showed weak and moderate positive correlation, while mouse (<i>r</i> = −0.135), and reconstructed human epidermis (<i>r</i> = −0.438) had a negative correlation. The majority (<i>n</i> = 17) of the CPEs belonged to Category 5 of the Globally Harmonized System of Classification or low toxicity hazard. CPEs alone or in combination enhanced permeation (ER = 0.198–106.57) of VC in topical formulations. The combination of isopropyl myristate, sorbitan monolaurate, and polyoxyethylene 80 as CPEs for VC resulted in the highest permeation enhancement ratio.
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