National and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, Yunnan Minzu University, Kunming 650500, China.
National and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, Yunnan Minzu University, Kunming 650500, China.
Int J Biol Macromol. 2022 Sep 30;217:922-930. doi: 10.1016/j.ijbiomac.2022.07.195. Epub 2022 Jul 28.
This study was performed to promote the clinical application of Panax notoginseng saponins (PNS), which present anti-inflammatory and antitumor activities, and provided insights for the preparation of controlled-release dosage forms of traditional Chinese medicine. A series of drug-loaded microspheres with degradable amphiphilic polymer material polyethylene glycol monomethyl ether-polylactic acid (mPEG-PLA) as the carrier was synthesized. The degradation, sustained-release behavior, and biocompatibility of the drug-loaded microspheres were studied through in vitro release, degradation, hemolysis, anticoagulation, and cytotoxicity experiments. The pharmacological activities of the microspheres were studied through anti-inflammatory and antitumor experiments. The results showed that the best carrier material was mPEG-PLA (1:9), with an average particle size of 3.47 ± 0.35 μm, a drug load of 5.50 ± 0.28 %, and an encapsulation efficiency of 38.52 ± 1.93 %. This material could be released stably for approximately 24 days and degrade in approximately 60 days. Moreover, the microspheres had good biocompatibility and anti-inflammatory and antitumor activities.
本研究旨在促进具有抗炎和抗肿瘤活性的三七总皂苷（PNS）的临床应用，并为中药控释剂型的制备提供了思路。采用可降解两亲性聚合物材料聚乙二醇单甲醚-聚乳酸（mPEG-PLA）作为载体，合成了一系列载药微球。通过体外释放、降解、溶血、抗凝和细胞毒性实验研究了载药微球的降解、缓释行为和生物相容性。通过抗炎和抗肿瘤实验研究了微球的药理活性。结果表明，最佳载体材料为 mPEG-PLA（1:9），平均粒径为 3.47±0.35μm，载药量为 5.50±0.28%，包封率为 38.52±1.93%。该材料可稳定释放约 24 天，约 60 天降解。此外，微球具有良好的生物相容性和抗炎、抗肿瘤活性。
