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用于结肠给药的吲哚美辛电纺纳米纤维:制备与表征

Indomethacin electrospun nanofibers for colonic drug delivery: preparation and characterization.

作者信息

Akhgari Abbas, Heshmati Zohreh, Sharif Makhmalzadeh Behzad

机构信息

Nanotechnology Research Center and School of Pharmacy, Ahvaz Jundishpaur University of Medical Sciences, Ahvaz,Iran.

出版信息

Adv Pharm Bull. 2013;3(1):85-90. doi: 10.5681/apb.2013.014. Epub 2013 Feb 7.

Abstract

PURPOSE

The objective of this study was to prepare a suitable form of nanofiber for indomethacin using polymers Eudragit RS100 (ERS) and Eudragit S100 (ES) and to evaluate the effect of some variables on the characteristics of resulted electrospunnanofibers.

METHODS

Electrospinning process was used for preparation of nanofibers. Different solutions of combinations of ERS, ES and indomethacin in various solvents and different ratios were prepared. The spinning solutions were loaded in 10 mL syringes. The feeding rate was fixed by a syringe pump at 2.0 mL/h and a high voltage supply at range 10-18 kV was applied for electrospinning. Electrospunnanofibers were collected and evaluated by scanning electron microscopy, differential scanning calorimetry and FTIR for possible interaction between materials used in nanofibers. The effect of solvent and viscosity on the characteristics of nanofibers also was investigated.

RESULTS

Fiber formation was successful using a solvent ethanol and mixture of ERS and ES. Increase in viscosity of ethanolic solutions of ERS followed by addition of ES in the solution led to preparation of smooth fibers with larger diameters and less amounts of beads. DSC analysis of fibers certified that indomethacin is evenly distributed in the nanofibers in an amorphous state. FTIR analysis did not indicate significant interaction between drug and polymer.

CONCLUSION

It was shown that drug-loaded ERS and ES nanofibers could be prepared by exact selection of range of variables such as type of solvent, drug: polymer ratio and solution viscosity and the optimized formulations could be useful for colonic drug delivery.

摘要

目的

本研究的目的是使用聚合物Eudragit RS100(ERS)和Eudragit S100(ES)制备适合吲哚美辛的纳米纤维形式,并评估一些变量对所得电纺纳米纤维特性的影响。

方法

采用电纺丝工艺制备纳米纤维。制备了ERS、ES和吲哚美辛在各种溶剂中的不同比例组合的不同溶液。将纺丝溶液装入10 mL注射器中。通过注射泵将进料速率固定为2.0 mL/h,并施加10 - 18 kV范围内的高压电源进行电纺丝。收集电纺纳米纤维,并通过扫描电子显微镜、差示扫描量热法和傅里叶变换红外光谱法评估纳米纤维中所用材料之间可能的相互作用。还研究了溶剂和粘度对纳米纤维特性的影响。

结果

使用溶剂乙醇以及ERS和ES的混合物成功形成了纤维。在ERS的乙醇溶液中增加粘度,随后在溶液中加入ES,导致制备出直径更大且珠粒数量更少的光滑纤维。纤维的差示扫描量热分析证明吲哚美辛以无定形状态均匀分布在纳米纤维中。傅里叶变换红外光谱分析未表明药物与聚合物之间有显著相互作用。

结论

结果表明,通过精确选择溶剂类型、药物:聚合物比例和溶液粘度等变量范围,可以制备载药的ERS和ES纳米纤维,优化后的制剂可用于结肠给药。

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