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首页> 外文期刊>Bulletin of the Korean Chemical Society >Development of SS-AG20-loaded Polymeric Microparticles by Oil-in-Water (o/w) Emulsion Solvent Evaporation and Spray Drying Methods for Sustained Drug Delivery
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Development of SS-AG20-loaded Polymeric Microparticles by Oil-in-Water (o/w) Emulsion Solvent Evaporation and Spray Drying Methods for Sustained Drug Delivery

机译：水包油（o / w）乳化溶剂蒸发和喷雾干燥法开发载有SS-AG20的聚合物微粒以实现持续药物输送

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Controlled drug delivery systems employing microparticles offer lots of advantages over conventional drug dosage formulations. Microencapsulation technique have been conducted with biodegradable polymers such as poly(lactic-co-glycolic acid) (PLGA) and poly(lactic acid) (PLA) for its adjustable biodegradability and biocompatibility. In this study, we evaluated two techniques, oil-in-water (o/w) emulsion solvent evaporation and spray drying, for preparation of polymeric microparticles encapsulating a newly synthesized drug, SSAG20, for the long-term drug delivery of this low-molecular-weight drug with a very short half-life. Drugloaded microparticles prepared by the solvent evaporation method showed a smoother morphology; however, relatively poor encapsulation efficiency and drastic initial burst were discovered as drawbacks. Spray-dried drug-loaded microparticles had an imperfect surface with pores and distorted portions so that its initial burst was critical (70.05-87.16%) when the preparation was carried out with a 5% polymeric solution. By increasing the concentration of the polymer, the morphology was refined and undesirable initial burst was circumvented (burst was reduced to 35.93-74.85%) while retaining high encapsulation efficiency. Moreover, by encapsulating the drug with various biodegradable polymers using the spray drying method, gradual and sustained drug release, for up to 2 weeks, was achieved.
机译：与常规药物剂量制剂相比，采用微粒的受控药物递送系统具有许多优势。微囊化技术已经用可生物降解的聚合物如聚乳酸-乙醇酸共聚物（PLGA）和聚乳酸（PLA）进行，以具有可调节的生物降解性和生物相容性。在这项研究中，我们评估了水包油（o / w）乳剂溶剂蒸发和喷雾干燥这两种技术，用于制备封装有新合成药物SSAG20的聚合物微粒，以长期用于这种低剂量的药物。分子量很短的半衰期药物。通过溶剂蒸发法制得的载药微粒具有较光滑的形态。然而，发现相对较差的封装效率和剧烈的初始破裂是缺点。喷雾干燥的载有药物的微粒的表面不完美，具有毛孔和扭曲的部分，因此当使用5％的聚合物溶液进行制备时，其初始破裂至关重要（70.05-87.16％）。通过增加聚合物的浓度，可以改善形态，并避免了不良的初始破裂（破裂减少到35.93-74.85％），同时保持了高封装效率。此外，通过使用喷雾干燥法将药物与各种可生物降解的聚合物一起包封，可以实现长达2周的逐渐且持续的药物释放。

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