用于前列腺癌靶向的白藜芦醇固体脂质纳米颗粒的开发、评价、药代动力学和生物分布估计。

IF 3 4区医学 Q2 CHEMISTRY, APPLIED

Journal of microencapsulation Pub Date : 2022-09-01 DOI:10.1080/02652048.2022.2135785

Alok Nath Sharma, Prabhat Kumar Upadhyay, Hitesh Kumar Dewangan

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引用次数: 13

摘要

背景与目的:本研究旨在利用固体脂质纳米颗粒(RSV- sln)延长反式白藜芦醇(RSV)的体循环和生物半衰期(t1/2)，以提高其抗癌潜力。方法:采用溶剂乳化蒸发法制备RSV-SLN，对其进行粒径、PDI、zeta电位、体外释放、体外细胞毒性、细胞内化、溶血和红细胞膜完整性、血小板聚集等评价和大鼠药代动力学研究。此外，还需要评估癌细胞对RSV-SLN的积累情况，以证明其靶向能力。结果:制备的SLN粒径为126.85±12.09 nm, Zeta电位为-24.23±3.27 mV, Zeta电位为74.67±4.76%。48小时后释放，血液相容。细胞内化图像显示SLN在PC3前列腺细胞的细胞质和细胞核内延伸。RSV-SLN具有较高的t1/2(8.22±1.36 h)和7.19±0.69 h MRT(平均停留时间)和较低的清除率(286.42±13.64 mL/min/kg)。发现RSV- sln在前列腺细胞中的生物分布非常高，积累量是RSV溶液的7.56倍。结论:所制备的RSV-SLN可作为化疗药物大体循环输送的潜在载体，具有肿瘤部位靶向性。

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Development, evaluation, pharmacokinetic and biodistribution estimation of resveratrol-loaded solid lipid nanoparticles for prostate cancer targeting.

Background and aim: The study was to extend systemic circulation and biological half-life (t_1/2) of trans-resveratrol (RSV) using solid lipid nanoparticles (RSV-SLN) to improve its anti-cancer potential.

Methods: RSV-SLN was prepared by solvent emulsification evaporation technique and proceeded for evaluation like particle size, PDI, zeta potential, in vitro release, in vitro cytotoxicity, cellular internalisation, haemolysis and erythrocyte membrane integrity, platelet aggregation and pharmacokinetic studies in rats. Moreover, cancer cells accumulation of RSV-SLN also needs to be evaluated for proving their targeting ability.

Result: Prepared SLN showed 126.85 ± 12.09 nm particle size, -24.23 ± 3.27 mV Zeta potential and 74.67 ± 4.76%. release at 48 h and haemocompatible. The cellular internalisation image showed the SLN reach in a cytoplasm and nucleus of PC3 prostate cells. RSV-SLN exhibited high t_1/2 (8.22 ± 1.36 h) and 7.19 ± 0.69 h MRT (Mean residence time) and lower clearance i.e. 286.42 ± 13.64 mL/min/kg. The bio-distribution of RSV-SLN was found to be extremely high in prostate cells and accumulate 7.56 times greater than that of RSV solution.

Conclusion: The developed RSV-SLN can be applied as potential carrier for delivery of drug of chemotherapeutics at an extend systemic circulation and targeting efficiency at tumour site.

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来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

审稿时长

3 months

期刊介绍： The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.