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Objective:To prepare a phase-change lipid nanoparticle modified by tumor homing membrane-penetrating peptide (tLyP-1) and carrying paclitaxel (PTX) engineered by metal polyphenol network (TA-Fe 3+ ), and evaluate the therapeutic effects of tumor targeting, ultrasound/photoacoustic imaging and photothermal combined chemotherapy in vitro. Methods:Phase-change lipid nanoparticles (t-P@TFP) with TA-Fe 3+ engineered PTX mediated by tLyP-1 were prepared by solvent replacement method, thin film hydration method and double emulsification method. Its detection and characterization, in vitro targeting ability, photothermal conversion ability, in vitro photoacoustic and ultrasonic imaging ability, CCK-8 method, cell live and death double staining method and flow cytometry method were used to detect the safety of nanoparticles and the killing effects of different nanoparticles on 4T1 cells. Results:t-P@TFP nanoparticles were successfully prepared. Transmission electron microscopy showed that the nanoparticles were spherical with uniform shape and size, with a particle size of (209.8±1.56)nm and a potential of (-25.9±1.36)mV. Laser confocal scanning microscopy showed that t-P@TFP nanoparticles could gather around 4T1 cells in a targeted manner. It had an efficient photothermal conversion effect, and nanoparticles could quickly become microbubbles after being irradiated by near-infrared laser, which enhanced the in vitro ultrasonic imaging effect; The photoacoustic signal of nanoparticles increased with the increase of concentration. CCK-8 method, double staining of living and dead cells and flow cytometry showed that t-P@TFP combined photothermal chemotherapy had the best anti-tumor effect. Conclusions:t-P@TFP nanoparticles are successfully prepared. The nanoparticles have good targeting ability for photoacoustic and ultrasonic imaging and have good photothermal effect, killing breast cancer cells, which is expected to realize the integration of diagnosis and treatment.
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Anti-tumor antibiotics exhibit great application potential in the anti-tumor therapy. Some drugs have become the first-line medication clinically. However, there are always various problems associated with anti-tumor antibiotics, such as poor solubility and instability as well as severe systemic side effects. It is important to choose suitable delivery carriers for a reasonable delivery system for a good targeting ability, enhanced anti-tumor efficacy and reduced adverse effects of the anti-tumor antibiotics, especially in the smart delivery systems. This review summarizes the carriers and the advances in the delivery systems of anti-tumor antibiotics, including anti-tumor antibiotic drugs currently on the market, in the clinical research stage and in the basic research stage.
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Objective: To prepare voriconazole albumin nanoparticles and evaluate the characteristics of pharmacokinetics and tissue distribution in rats.Methods: Voriconazole albumin nanoparticles were prepared by a new ultra-high pressure microfluidization technology.The physicochemical properties of voriconazole albumin nanoparticles were studied, such as the particle size distribution, zeta potential and particle shape.The release of voriconazole from albumin nanoparticles was investigated in pH7.4 phosphate buffered saline.The concentrations of voriconazole in plasma and the other different tissues were determined after the tail-vein injection of voriconazole albumin nanoparticles in rats.Results: Voriconazole albumin nanoparticles were homogeneous small spheres as seen under a transmission electron microscope.The average particle diameter was (121.9±41.6) nm, the polydispersity index was 0.197, and the zeta potential was (-42.1±0.9) mV.In 0.5% Tween-80 phosphate buffered saline (pH7.4), the in vitro cumulative release of voriconazole albumin nanoparticles reached up to 67.5% in 24 h.AUC0-24 of voriconazole albumin nanoparticles and voriconazole injection was (98.27±1.42) and (105.32±1.45) g/L/h, and MRT0-24 was (4.48±0.38) and (4.86±0.51) h, respectively.Conclusion: Voriconazole albumin nanoparticles can prolong the circulation time, and exhibit promising targeting ability in liver, spleen and brain.
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Objective:To observe the transfection efficacy and targeting efficiency of hepatitis B virus envelope(HBVE) as a gene transfer vector for liver cancer cells.Methods:HBVE was obtained from the supernatant of HepG2.2.15 cells with a PEG8000 system and ?-propiolactone.The pIRS2-EGFP was packed with HBVE to obtain HBVE-GFP and was packed with liposome to obtain Liposome-GFP.HBVE-GFP and Liposome-GFP were used to transfect human hepatoblastoma cell line HepG 2 to study the transfection efficiency.HepG 2,A 549,HeLa and FB cells were transfected with HBVE-GFP to appraise the targeting ability of HBVE-GFP.GFP protein expression was observed under a fluorescent microscope and the ratio of GFP positive cells was determined by flow cytometry.Results:(1) Transfection efficiency:The GFP protein was observed in both the liposome group and the HBVE group under the fluorescent microscope;the fluorescent intensity in the HBVE group was 3-4 times that of liposome group as determined by flow cytometry(P