高效紫杉醇微乳液载体PMBN的制备及生物相容性

Q3 Biochemistry, Genetics and Molecular Biology
Mahmoud Gharbavi, A. Sharafi, P. Fath, Saeed Oruji, H. Pakzad, H. Manjili
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引用次数: 8

摘要

简介:紫杉醇(PTX)是一种有效的化疗药物,广泛用于治疗多种类型的癌症。然而,由于水溶性差,生物利用度低,其使用受到限制。提高药物疗效和耐受性的主要方法之一取决于用于药物的载体。在目前的研究中,基于聚[2-甲基丙烯酰氧基乙基磷酰胆碱(MPC)-甲基丙烯酸正丁酯(BMA)-对硝基苯氧基羰基-甲基丙烯酸聚乙二醇(ME-ONP)](PMBN)作为PTX载体提高其半衰期和生物利用度的能力,研究了微乳液(ME)。此外,还对ME体系的物理化学性质进行了评价。材料和方法:分别以PMBN、吐温80、三乙酸甘油和甘油为药物载体、表面活性剂、油相和共表面活性剂。使用红细胞溶血试验对溶血活性进行表征,以评估ME的血液相容性。此外,进行了PMBN-PTX-ME和PTX对MCF-7、4T1和HFF-2细胞系的体外细胞毒性作用。PI和Annexin-V染料用于细胞凋亡。结果:评估了ME的电导率,结果显示432至589µS/cm。在体外,药物释放研究表明,PTX在不同pH水平下具有控制释放的作用。ME的折射率(RI)和%透射率分别保持在1.43至1.53和89%至98%的范围内。MTT法测定不含PTX的PMBN-ME对HFF-2、MCF-7和4T-1细胞系没有显著毒性。基于细胞凋亡测定,用PMBN处理的细胞系大致保持存活。结论:基于PMBN的ME是一种很有前途的PTX给药系统。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and Biocompatibility of Microemulsion-Based PMBN as an Efficient System for Paclitaxel Delivery
Introduction: Paclitaxel (PTX), an effective chemotherapeutic drug, is widely used to treat several types of cancers.  However, its use is limited due to poor water solubility resulted in poor bioavailability. One of the main ways to increase the efficacy and endurance of medications depends on the carrier that used for it. In the current study, the microemulsions (ME) were investigated based on Poly [2-methacryloyloxyethyl phosphorylcholine (MPC)-co-n-butyl methacrylate (BMA)-co-p-nitrophenyl-oxycrabonyl poly ethylene glycol-methacrylate (ME-ONP)] (PMBN) ability as a carrier for PTX to increase the half-life and its bioavailability. Also, the physicochemical properties of the ME system were evaluated. Materials and Methods: PMBN, tween 80, triacetin, and glycerol were used as the drug carrier, surfactant, oil phase, and co-surfactant, respectively. The hemolytic activity was characterized using the RBC hemolysis assay to evaluate the blood compatibility of the MEs. In addition, the in vitro cytotoxic effect of PMBN-PTX-ME and PTX on MCF-7, 4T1, and HFF-2 cell lines was performed. PI and Annexin-V dyes were used for cell apoptosis. Results: The conductivity of ME evaluated and the results showed 432 to 589 µS/cm. In vitro, the drug release study revealed that PTX has controlled release at different pH levels. Refractive Index (RI) and % transmittance of the MEs remained ranging from 1.43 to 1.53, and 89% to 98%, respectively. The MTT assay determined that PMBN-ME without PTX had no significant toxicity on HFF-2, MCF-7, and 4T-1 cell lines. Based on the apoptosis assay, treated cell lines with PMBN approximately remained alive. Conclusions: The results revealed that ME-based on PMBN would be a promising drug delivery system for PTX drug delivery.
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来源期刊
Journal of Applied Biotechnology Reports
Journal of Applied Biotechnology Reports Biochemistry, Genetics and Molecular Biology-Biotechnology
CiteScore
1.90
自引率
0.00%
发文量
0
期刊介绍: The Journal of Applied Biotechnology Reports (JABR) publishes papers describing experimental work relating to all fundamental issues of biotechnology including: Cell Biology, Genetics, Microbiology, Immunology, Molecular Biology, Biochemistry, Embryology, Immunogenetics, Cell and Tissue Culture, Molecular Ecology, Genetic Engineering and Biological Engineering, Bioremediation and Biodegradation, Bioinformatics, Biotechnology Regulations, Pharmacogenomics, Gene Therapy, Plant, Animal, Microbial and Environmental Biotechnology, Nanobiotechnology, Medical Biotechnology, Biosafety, Biosecurity, Bioenergy, Biomass, Biomaterials and Biobased Chemicals and Enzymes. Journal of Applied Biotechnology Reports promotes a special emphasis on: -Improvement methods in biotechnology -Optimization process for high production in fermentor systems -Protein and enzyme engineering -Antibody engineering and monoclonal antibody -Molecular farming -Bioremediation -Immobilizing methods -biocatalysis
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