Abstract: OBJECTIVE To describe the recent development of novel drug delivery systems and preparation techniques in photodynamic therapy (PDT). METHODS The novel drug delivery systems of liposome,nanoparticles, micelles, surface modification,and the preparation techniques of microneedle arrays, electroporation, self-luminescence and upconversion used in PDT were reviewed. RESULTS The novel drug delivery systems and preparation techniques mentioned above had particular advantage on overcoming the shortage of most existing photosensitizers,such as hydrophobic, aggregate easily under physiological condition,and low accumulation selectivity to diseased tissues. CONCLUSION The novel drug delivery systems and preparation techniques above were very important to the bright future of PDT since they offered the best hope for extending the reach of photosensitive drug to regions deep in the body with a relative target.