水滑石-PLGA复合纳米粒子用于丹参素的负载和递送,RSC Advances

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水滑石-PLGA复合纳米粒子用于丹参素的负载和递送
RSC Advances ( IF 3.9 ) Pub Date : 2020-6-9 , DOI: 10.1039/d0ra01593h
Lihui Pu ₁ , Haiyan Yu ₁ , Juan Du ₁ , Yanyan Zhang ₁ , Sihao Chen ₁

Affiliation

作为丹参水溶性成分中的主要药效成分之一（丹参）、丹参素（DSS）适用于治疗心血管疾病。然而，水溶性低、半衰期短等缺点会降低其生物利用度，限制其临床应用。因此，可以将其整合到载药聚合物微球中，有效提高药物的生物利用度。在这项研究中，DSS 首先嵌入到水滑石 (LDH) 层中。然后，将具有优异生物相容性和生物降解性的聚乳酸（PLGA）涂覆在表面上。PLGA/DSS-LDH复合纳米粒子是使用双乳液（w/o/w）溶剂蒸发法制备的。XRD和FTIR研究表明，药物DSS成功包埋在LDH层中，LDH的载药量达到32.6%。PLGA/DSS-LDH的体外药物释放特性。PLGA/DSS-LDH复合纳米粒子不仅表现出高包封效率，而且具有缓释特性。溶血试验表明，PLGA/DSS-LDH复合纳米粒子对溶血的诱导无效，表明PLGA/LDH复合纳米粒子可以为药剂学提供有效的控释药物体系。

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Hydrotalcite–PLGA composite nanoparticles for loading and delivery of danshensu

As one of the main pharmacodynamic components present in the water-soluble components of Salvia miltiorrhiza (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 in vitro 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.

更新日期：2020-06-09

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