目的:通过喷雾干燥制备微球的重复性和放大生产存在重大挑战。在这项研究中,以聚乳酸-羟基乙酸共聚物(PLGA)为缓释载体,采用新型静态混合法制备了醋酸曲安奈德(TAA)可生物降解微球。
方法:使用静态混合技术制备负载TAA的微球(TAA-MS)。PLGA浓度,聚乙烯醇浓度(PVA),油/水的相比,和水/固化的相比在颗粒尺寸方面进行了优化,载药量(DL),和TAA-MS的封装效率(EE)。使用扫描电子显微镜(SEM)检查TAA-MS的形态,通过X射线衍射(XRD)对其理化性质进行了评价,差示扫描量热法(DSC),傅里叶变换红外光谱(FT-IR)。在37°C的pH7.4的介质中,使用水浴振动法将TAA-MS的体外释放与纯药物(TAA)的体外释放进行了比较。
结果:制备TAA-MS的制剂组成和制备条件优化为:PLGA浓度为1%,油(二氯甲烷)/水(PVA溶液)的相比为1:3,水(PVA溶液)/固化的相比为1:2。优化的TAA-MS显示球形颗粒,尺寸范围为30-70μm,DL和EE值分别为27.09%和98.67%,分别。此外,载药微球表现出显著的,持续释放,20%的药物在28天内释放。XRD结果表明,微球中TAA的晶型已部分转化为无定形。DSC和FT-IR结果表明,TAA和PLGA之间发生了一些相互作用,表明该药物被有效地包封到PLGA微球中。
结论:通过静态混合技术成功制备了负载TAA的PLGA微球,具有增强的EE和持续释放的方式。
OBJECTIVE: Reproducibility and scale-up production of microspheres through spray drying present significant challenges. In this study, biodegradable microspheres of Triamcinolone Acetonide Acetate (TAA) were prepared using a novel static mixing method by employing poly( lactic-co-glycolic acid) (PLGA) as the sustained-release carrier.
METHODS: TAA-loaded microspheres (TAA-MSs) were prepared using a static mixing technique. The PLGA concentration, polyvinyl alcohol concentration (PVA), phase ratio of oil/water, and phase ratio of water/solidification were optimized in terms of the particle size, drug loading (DL), and encapsulation efficiency (EE) of TAA-MSs. The morphology of TAA-MSs was examined using Scanning Electron Microscopy (SEM), while the physicochemical properties were evaluated through X-ray diffraction (XRD), Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared Spectroscopy (FT-IR). The in vitro release of TAA-MSs was compared to that of the pure drug (TAA) using a water-bath vibration method in the medium of pH 7.4 at 37°C.
RESULTS: The formulation composition and preparation condition for the preparation of TAA-MSs were optimized as follows: the PLGA concentration was 1%, the phase ratio of oil(dichloromethane) /water (PVA solution) was 1:3, the phase ratio of water (PVA solution)/solidification was 1:2. The optimized TAA-MSs displayed spherical particles with a size range of 30-70 μm, and DL and EE values of 27.09% and 98.67%, respectively. Moreover, the drug-loaded microspheres exhibited a significant, sustained release, with 20% of the drug released over a period of 28 days. The XRD result indicated that the crystalline form of TAA in microspheres had been partly converted into the amorphous form. DSC and FT-IR results revealed that some interactions between TAA and PLGA occurred, indicating that the drug was effectively encapsulated into PLGA microspheres.
CONCLUSIONS: TAA-loaded PLGA microspheres have been successfully prepared via the static mixing technique with enhanced EE and sustained-release manner.