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用于负载和递送丹参素的水滑石-PLGA复合纳米颗粒

Hydrotalcite-PLGA composite nanoparticles for loading and delivery of danshensu.

作者信息

Pu Lihui, Yu Haiyan, Du Juan, Zhang Yanyan, Chen Sihao

机构信息

College of Chemistry and Chemical Engineering, Shanghai University of Engineering Science Shanghai 201620 People's Republic of China

出版信息

RSC Adv. 2020 Jun 9;10(37):22010-22018. doi: 10.1039/d0ra01593h. eCollection 2020 Jun 8.

Abstract

As one of the main pharmacodynamic components present in the water-soluble components of (Danshen), danshensu (DSS) is applicable to treating cardiovascular diseases. Nevertheless, such drawbacks as low water solubility and short half-life could reduce its bioavailability and restrict its clinical applicability. Therefore, it can be integrated into drug-carrying polymer microspheres, which is effective in improving the bioavailability of drugs. In this study, DSS was first embedded in a hydrotalcite (LDH) layer. Then, polylactic acid (PLGA) with excellent biocompatibility and biodegradability was coated on the surface. PLGA/DSS-LDH composite nanoparticles were prepared using the double emulsion (w/o/w) solvent evaporation method. As revealed by XRD and FTIR studies, success was achieved in embedding the drug DSS in the LDH layer, with the drug loading capacity of the LDH reaching 32.6%. A study was conducted on the encapsulation efficiency, surface morphology and drug release characteristics of PLGA/DSS-LDH. PLGA/DSS-LDH composite nanoparticles exhibited not only a high encapsulation efficiency but also a sustained release profile. The hemolysis assays demonstrated that the PLGA/DSS-LDH composite nanoparticles were ineffective in the induction of hemolysis, suggesting that PLGA/LDH composite nanoparticles can provide an effective controlled release drug system for pharmaceutics.

摘要

作为丹参水溶性成分中的主要药效成分之一,丹参素(DSS)适用于治疗心血管疾病。然而,其低水溶性和短半衰期等缺点会降低其生物利用度并限制其临床应用。因此,可将其整合到载药聚合物微球中,这对提高药物的生物利用度有效。在本研究中,首先将DSS嵌入水滑石(LDH)层中。然后,在其表面包覆具有优异生物相容性和生物降解性的聚乳酸(PLGA)。采用双乳液(w/o/w)溶剂蒸发法制备了PLGA/DSS-LDH复合纳米粒子。XRD和FTIR研究表明,成功地将药物DSS嵌入LDH层中,LDH的载药量达到32.6%。对PLGA/DSS-LDH的包封率、表面形态和药物释放特性进行了研究。PLGA/DSS-LDH复合纳米粒子不仅表现出高包封率,而且具有缓释特性。溶血试验表明,PLGA/DSS-LDH复合纳米粒子诱导溶血无效,这表明PLGA/LDH复合纳米粒子可为药剂学提供有效的控释药物系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a66/9054529/2f745a20f8a4/d0ra01593h-f1.jpg

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