结肠靶向磁响应美沙拉胺微球的制备与表征

S. Gaikwad, Preeti K. Suresh
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摘要

背景:磁响应美沙拉胺微球是治疗肠易激病的一种有效的靶向给药策略,从而最大限度地减少剂量和药物诱导毒性。目的:本研究的主要目的是使药物仅在靶部位定位,从而使剂量最小化。结果与讨论:本研究以可生物降解聚合物壳聚糖和果胶为原料,采用溶剂蒸发法制备具有磁性响应的美沙拉胺微球,并对其进行各种药理学和磁学表征,研究聚合物类型对其体外释放的影响,以及微生物激活系统体外释放研究和体外抗炎活性等临床前体外筛选研究。2. 用FTIR光谱进行了化学相容性研究。FTIR光谱研究表明,美沙拉胺与聚合物具有相容性。光谱显示主峰没有变化,从而证实了药物与聚合物之间没有相互作用。3.在pH7磷酸盐缓冲盐水中建立美沙拉胺的校准曲线。4. 采用沉淀法化学合成了以Fe3O4为载体的磁铁矿。本研究以壳聚糖和果胶为聚合物,以不同比例(1:1、1:2和1:3)和两种聚合物的组合制备了3种配方。并对聚合物类型的影响进行了研究。结论:磁响应美沙拉胺微球通过物理途径(利用磁靶向原理在靶器官附近产生储库)和生化途径(利用可生物降解聚合物壳聚糖和果胶进行药物可控释放)的联合作用,仅在靶部位提供局部药物递送。通过在靶器官附近建立一个储存库,可以避免不必要的药物分布到非靶器官。
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Formulation and Characterization of Magnetically Responsive Mesalamine Microspheres for Colon Targeting
Background: Magnetically Responsive Mesalamine Microspheres is an effective strategy for localized drug delivery only at the target site for the treatment of Irritable Bowel Diseases and thereby minimizing the dose and drug induced toxicity. Objective: The main objective of the study is to localize the drug only at the target site thereby minimizing the dose. Result and Discussion: 1. The aim of present study was to formulate Magnetically Responsive Mesalamine Microspheres by solvent evaporation method using biodegradable polymers Chitosan and Pectin and carry out the various pharmaceutical and magnetic characterizations, to study the effect of polymer type on in-vitro drug release and preclinical in-vitro screening studies such as in- vitro release studies using microflora activated system and in-vitro anti-inflammatory activity. 2. Chemical compatibility study was performed using FTIR spectroscopy. FTIR spectroscopy studies indicated that the Mesalamine is compatible with polymers. The spectra showed no changes in the major peaks thus confirming no interactions between drug and polymers. 3. Calibration curves of Mesalamine was constructed in Phosphate Buffer Saline pH7. 4. Magnetite (Fe3O4) (used as magnetic carrier) was chemically synthesized using precipitation method.5. In the present study, 3 formulations were prepared in total by using Chitosan and Pectin as polymer in different ratios (1:1,1:2 and 1:3) of each polymer and combination of two polymers. Also, the effect of polymer type was studied. Conclusion: It can be concluded that the Magnetically Responsive Mesalamine Microspheres offer a localized drug delivery only at the target site by the combined effect of physical approach (utilizing the principle of magnetic targeting with an intention to produce a depot near the target organ) and biochemical approach (using biodegradable polymers chitosan and pectin for drug release in a controlled manner). By producing a depot near the target organ, unwanted distribution of drug to non-target organ can be avoided.
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