通过设计辅助开发D-α-生育酚聚乙二醇1000琥珀酸-吉非替尼负载阳离子脂质体的质量。

IF 3 Q2 PHARMACOLOGY & PHARMACY Therapeutic delivery Pub Date : 2023-12-01 Epub Date: 2023-11-29 DOI:10.4155/tde-2023-0075

Lopamudra Mishra, Shuvadip Bhowmik, Rajveer Singh, Preeti Patel, Ghanshyam Das Gupta, Balak Das Kurmi

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引用次数: 0

摘要

目的:研制吉非替尼负载D-α-生育酚聚乙二醇1000琥珀酸酯(TPGS)包被阳离子脂质体(GEF-TPGS-LIPO+)，并采用质量设计(QbD)方法对其潜在的抗癌作用进行优化。方法/材料:采用Box-Behnken设计(BBD)，采用系统的实验设计对配方变量进行筛选和优化。结果:GEF-TPGS-LIPO+的囊泡大小为210±4.82 nm，多分散性指数为0.271±0.002,zeta电位为22.2±0.84 mV，包封效率为82.3±1.95。MTT结果显示，A549肺癌细胞的细胞毒性增强，细胞内药物摄取增加，活性氧和NF-κB的表达水平最高和最低。结论:阳离子脂质体可能与癌细胞相互作用，对A549细胞具有潜在的抗癌作用。

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Quality by design-assisted development of D-α-tocopherol polyethylene glycol 1000 succinate-incorporated gefitinib-loaded cationic liposome(s).

Aim: Gefitinib-loaded D-α-tocopherol polyethylene glycol 1000 succinate (TPGS)-coated cationic liposomes (GEF-TPGS-LIPO⁺) were developed and optimized by the quality by design (QbD) approach for its potential anticancer effect. Methods/materials: Box-Behnken design (BBD) a systematic design of experiments was added to screen and optimize the formulation variables. Results: GEF-TPGS-LIPO⁺ shows vesicle size (210 ± 4.82 nm), polydispersity index (0.271 ± 0.002), zeta potential (22.2 ± 0.84 mV) and entrapment efficiency (82.3 ± 1.95). MTT result shows the enhanced cytotoxicity and higher intracellular drug uptake with highest and lowest levels of the reactive oxygen species and NF-κB expressions on A549 lung cancer cells, determined by fluorescence-activated cell sorting flow cytometry. Conclusion: Potential anticancer effect on A549 cells might be found due to cationic liposomal interaction with cancer cells.

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来源期刊

Therapeutic delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.50

自引率

0.00%

发文量

期刊介绍： Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.