Over the last decades enhanced emphasis has been made on the environmental aspects of chemical processes, the preference being given to ―green‖ technologies and materials. Chitosan is considered one of the most promising biopolymer due to its unique characteristics which include biocompatibility, biodegradability, non-toxicity and solubility in aqueous media, thus making it very promising for medical, biochemical and ecological applications [1]. The presence of reactive amine groups in chitosan structure allows for linkage to acidic fragments of other molecules facilitating its solubility and enhancing the efficiency of the resulting composites. Metallophthalocyanines (MPc) are gaining continuously increasing attention in biomedicine especially as photosensitizers for photodynamic therapy (PDT) from a tumor-centered approach [2]. MPc conjugated to naturally occurring polymers doped with noble metal nanoparticles are even more effective as anticancer compounds [3]. Considering all these, the purpose of the research was synthesis and investigation of biopolymer materials based on chitosan conjugated with zinc(II) tetrasulfophthalocyanine, thioacetic acid and gold nanoparticles. UV-Vis spectrophotometric investigation of the solutions of chitosan conjugated with zinc(II) tetrasulfophthalocyanine and thioacetic acid demonstrated the presence of absorption bands in 680-720 nm range. The maximums of the bands shift towards longer wavelengths upon aggregating with gold nanoparticles, which is beneficial for photodynamic therapy. The results of molecular toxicity study test have shown satisfactory results, making the resulting composites convenient candidates for medical use.