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5-aminolaevulinic acid peptide prodrugs enhance photosensitization for photodynamic therapy

Photodynamic therapy (PDT) using 5-aminolaevulinic acid (ALA) has been widely used for treatment of cutaneous tumours, mainly basal cell carcinoma. However, ALA is relatively hydrophilic with poor stability at physiological pH, which limit its efficacy. In this study, we investigated more lipophilic, ALA-peptide derivatives for improving ALA PDT. We demonstrated that these new derivatives can greatly increase its cellular uptake leading to higher intracellular porphyrin concentrations and a higher PDT effect compared to same ALA dose. The derivatives are comparable in efficacy with a clinically approved derivative of ALA (5-aminolaevulinic hexyl ester) but significantly less toxic and more stable.