Targeted Delivery of Cisplatin-Derived Nanoprecursors via a Biomimetic Yeast Microcapsule for Tumor Therapy by the Oral Route.

摘要: Targeted therapy via the patient-friendly oral route remains holy grail of chemotherapy for cancer. Herein we report a yeast-derived platform targeted delivery cisplatin (CDDP) that is one most effective drugs various types cancers. Methods: The optimal conditions were first established to fabricate yeast microcapsules (YCs) with desirable loading capability. Then, CDDP-derived precursor nanoparticles (PreCDDP) prepared and packaged into YC produce orally deliverable PreCDDP/YC. physiochemical properties, in vitro drug release profiles, antitumor activity, targeting capability, vivo pharmacokinetics, efficacy YC-based biomimetic system examined. Results: YCs obtained under optimized condition showed efficiency quantum dots used as model nanocargo. In experiments demonstrated rapid endocytosis prolonged retention macrophages. By electrostatic force-mediated self-deposition, PreCDDP was efficiently loaded YC. PreCDDP/YC potent cytotoxicity different tumor cells, indicating maintained its activity after intracellular release. As compared CDDP PreCDDP, administered displayed significantly higher bioavailability. Post delivery, could accumulate A549 human lung carcinoma xenografts mice, achieving by monocyte/macrophage-mediated translocation lymphatic system. Through this effect, xenograft-bearing which comparable free intravenous injection. Orally CDDP, however, did not afford effects. Furthermore, treatment better safety than or route. Conclusions: This approach can serve an strategy develop chemotherapies based on derivatives.