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硝苯地平载药聚乳酸/聚乙二醇微胶囊的制备及释药行为。

Preparation and Drug Release Behavior of Nifedipine-Loaded Poly(lactic acid)/Polyethylene Glycol Microcapsules.

机构信息

Convergence Institute of Biomedical Engineering and Biomaterials, Seoul National University of Science and Technology, Seoul, 01811, Republic of Korea.

Department of Biomedical Engineering, Daelim University, Anyang, 13916, Republic of Korea.

出版信息

J Nanosci Nanotechnol. 2021 Jul 1;21(7):3735-3741. doi: 10.1166/jnn.2021.19168.

Abstract

Nifedipine (NF)-loaded poly(lactic acid) (PLA) and PLA/polyethylene glycol (PLA/PEG) microcapsules are synthesized using a high-speed agitator and a syringe pump with an oil-in-water emulsion-solvent evaporation technique to evaluate the effect of PLA/PEG ratio on morphology and drug release behavior of the capsules. Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimeter (DSC), and X-ray diffraction (XRD) results indicate that PEG reacts successfully with PLA due to the ether bond between PEG and PLA. The drug release rate of PLA and PLA/PEG capsules increases dramatically from 0 to 5 min and then reaches a plateau within 15 to 20 min. Due to the high specific surface area, the amount of NF released is raised by reducing the PLA concentration from 5 wt% to 2 wt%. Unlike PLA capsules, the drug release rate of PLA/PEG capsules increases due to the size effect by varying the PLA/PEG ratio from 10/0 to 6/4. Larger PLA/PEG capsules are attributed to higher amounts of encapsulated NF. The capsules show no evidence of cytotoxicity, suggesting that the PLA and PLA/PEG drug carriers are clinically safe.

摘要

硝苯地平(NF)负载的聚乳酸(PLA)和 PLA/聚乙二醇(PLA/PEG)微胶囊是使用高速搅拌器和注射器泵通过油包水乳液-溶剂蒸发技术合成的,以评估 PLA/PEG 比例对胶囊形态和药物释放行为的影响。傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)和 X 射线衍射(XRD)结果表明,由于 PEG 和 PLA 之间的醚键,PEG 与 PLA 成功反应。PLA 和 PLA/PEG 胶囊的药物释放率从 0 到 5 分钟急剧增加,然后在 15 到 20 分钟内达到平台期。由于比表面积高,通过将 PLA 浓度从 5wt%降低至 2wt%,NF 的释放量增加。与 PLA 胶囊不同,通过改变 PLA/PEG 比例从 10/0 至 6/4,PLA/PEG 胶囊的药物释放率因尺寸效应而增加。较大的 PLA/PEG 胶囊归因于包裹的 NF 量较高。这些胶囊没有显示出细胞毒性的证据,表明 PLA 和 PLA/PEG 药物载体在临床上是安全的。

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