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Effect of method of preparation and process variables on controlled release of insoluble drug from chitosan microspheres

机译：制备方法和工艺变量对壳聚糖微球不溶性药物控制释放的影响

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An inexpensive and simple method was adopted for the preparation of chitosan microspheres, crosslinked with glutaraldehyde (GA), for the controlled release of an insoluble drug-ibuprofen, which is a commonly used NSAID (non-steroidal anti-inflammatory drug). The chitosan microspheres were prepared by different methods and varying the process conditions such as rate of stirring, concentration of crosslinking agent, and drug:polymer ratio in order to optimize these process variables on microsphere size, size distribution, degree of swelling, drug entrapment efficiency, and release rates. The absence of any chemical interaction between drug, polymer, and the crosslinking agent was confirmed by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and thermogravimetric analyses (TGA) techniques. The microspheres were characterized by optical microscopy, which indicated that the particles were in the size range of 30-200mm and scanning electron microscopy (SEM) studies revealed a smooth surface and spherical shape of microspheres. The microsphere size/size distributions were increased with the decreased stirring rates as well as GAconcentration in the suspension medium. Decreasing the concentration of crosslinker increased the swelling ratio whereas extended crosslinking exhibited lowered entrapment efficiency. The in vitro drug release was controlled and extended up to 10 hr.
机译：采用一种廉价而简单的方法来制备与戊二醛（GA）交联的壳聚糖微球，以控制释放不溶性药物布洛芬，这是一种常用的NSAID（非甾体类抗炎药）。壳聚糖微球是通过不同的方法制备的，并且通过改变工艺条件（例如搅拌速率，交联剂的浓度以及药物与聚合物的比例）来制备，以优化这些工艺变量的微球尺寸，尺寸分布，溶胀度，药物截留效率以及发布率。药物，聚合物和交联剂之间不存在任何化学相互作用，这通过傅立叶变换红外（FTIR）光谱，差示扫描量热法（DSC）和热重分析（TGA）技术得以证实。通过光学显微镜对微球进行了表征，这表明颗粒的尺寸范围为30-200mm，而扫描电子显微镜（SEM）研究表明微球具有光滑的表面和球形。随着降低的搅拌速率以及悬浮介质中GA的浓度，微球尺寸/尺寸分布增加。交联剂浓度的降低增加了溶胀率，而延长的交联则降低了包封率。控制体外药物释放并延长至10小时。

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