Abstract—Theranostics is the direction in modern biomedicine aimed at developing drugs that combine the capabilities of diagnosis and therapy of tumors in one agent. Upconversion nanophosphors (UCNPs) are inorganic crystalline materials that can be used to create a nanoplatform providing diagnostic and therapeutic modalities. They have been proposed as luminescent markers for optical imaging of biological tissue due to their anti-Stokes luminescence, lack of photodegradation and low toxicity. In this article, UCNPs as a theranostic agent for both optical imaging and delivery of anticancer drugs have been offered. To obtain biocompatible nanocomplexes, UCNP surface with a core/shell structure of NaYF₄:Yb³⁺Tm³⁺/NaYF₄ was modified with polylactic acid in the presence of various stabilizers (dextran, polyvinyl alcohol, and poly-N-vinylpyrrolidone). To give the therapeutic modality to the nanocomplex, the antitumor antibiotic doxorubicin was loaded into the polymer shell. The loading efficiency was up to 0.1 mg per 1 mg UCNPs. The toxicity and the intracellular accumulation of nanocomplexes were evaluated in vitro. It was concluded that the modification of UCNPs with polylactic acid provides the transport of doxorubicin, allowing the combination of diagnostic and therapeutic modalities in one agent.

摘要—Theranostics是现代生物医学的方向，旨在开发将一种肿瘤的诊断和治疗功能结合在一起的药物。上转换纳米磷光体（UCNP）是无机晶体材料，可用于创建提供诊断和治疗方式的纳米平台。由于它们的抗斯托克斯（Stokes）发光，缺乏光降解和低毒性，它们已被建议作为生物组织光学成像的发光标记。在本文中，已提供了作为光学成像和抗癌药物传递治疗试剂的UCNP。为了获得生物相容的纳米复合物，UCNP表面应具有NaYF ₄的核/壳结构：Yb ³⁺ Tm ³⁺ / NaYF ₄在各种稳定剂（右旋糖酐，聚乙烯醇和聚N-乙烯基吡咯烷酮）的存在下，用聚乳酸对苯甲酸进行改性。为了给纳米复合物提供治疗手段，将抗肿瘤抗生素阿霉素加载到聚合物壳中。每1毫克UCNP的负载效率高达0.1毫克。在体外评估了纳米复合物的毒性和细胞内积累。结论是，用聚乳酸修饰UCNPs可提供阿霉素的转运，从而允许在一种药物中组合诊断和治疗方式。