Rapid development of nanotechnology provides promising strategies in biomedicine, especially in tumor therapy. In particular, the cellular uptake of nanosystems is not only a basic premise to realize various biomedical applications, but also a fatal factor for determining the final therapeutic effect. Thus, a systematic and comprehensive summary is necessary to overview the recent research progress on the improvement of nanosystem cellular uptake for cancer treatment. According to the process of nanosystems entering the body, they can be classified into three categories. The first segment is to enhance the accumulation and permeation of nanosystems to tumor cells through extracellular microenvironment stimulation. The second segment is to improve cellular internalization from extracellular to intracellular via active targeting. The third segment is to enhance the intracellular retention of therapeutics by subcellular localization. The major factors in the delivery can be utilized to develop multifunctional nanosystems for strengthening the tumor therapy. Ultimately, the key challenges and prospective in the emerging research frontier are thoroughly outlined. This review is expected to provide inspiring ideas, promising strategies and potential pathways for developing advanced anticancer nanosystems in clinical practice.
Keywords: cancer therapy; cellular uptake; efficient enrichment; multifunctional nanosystems; nanotechnology.
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