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新型聚电解质复合微球的设计与统计优化,以提高伏格列汀的包封效率和释放研究。

Design and Statistical Optimization of Novel Polyelectrolyte Complex Microbeads to Improve Entrapment Efficiency and Release Study of Vildagliptin.

机构信息

Department of Pharmacy, Shri Ram Murti Smarak College Engineering & Technology (Pharmacy), Bareilly, India.

Department of Pharmacy, Dean Academic Pharmacy, Future Group of Institutions, Bareilly, India.

出版信息

Recent Adv Drug Deliv Formul. 2023;17(1):71-85. doi: 10.2174/2667387817666230308113951.

DOI:10.2174/2667387817666230308113951
PMID:36892032
Abstract

BACKGROUND

The current research focused on the improvement of drug entrapment efficiency and release study of hydrophilic drug through polymer complextation.

OBJECTIVE

Ionotropic gelation technique was utilised for the preparation of Polyelectrolyte complex microbeads of Vildagliptin using Sodium alginate and Eudragit RL100 and their performance was optimized by Central composite design.

METHODS

Fourier Transform Infrared Spectroscopy, Scanning Electron Microscope, Differential Scanning Calorimetry, particle size, Drug Entrapment Efficiency, X-ray diffraction and drug release at 10hr were chosen for evaluating formulated microbeads. The impact of independent variables like concentration of sodium alginate and eudragit RL100 was examined over dependent responses.

RESULTS

The interpretation of XRD, SEM, DSC, and FTIR affirmed no drug excipients interference and confirmed formation of polyelectrolyte complex microbeads. For complex microbeads, the maximum and minimum drug release after 10 hours was obtained as 96.23.5% and 89.45%, respectively. The 32 central composite design was further used to obtain response surface graph and the values for the particle size, DEE and Drug release were retained as 0.197, 76.30 % and 92.15%, respectively for the optimize batch.

CONCLUSION

The result suggested the combination of two polymers (Sodium alginate and Eudragit RL100) were suitable for improving the entrapment efficiency of hydrophilic drug (Vildagliptin). The central composite design (CCD) technique is an effective tool for obtaining optimal drug delivery systems of Vildagliptin polyelectrolyte complex microbeads.

摘要

背景

本研究旨在通过聚合物络合作用提高亲水性药物的药物包封效率并进行释放研究。

目的

采用离子凝胶化技术,以海藻酸钠和 Eudragit RL100 为原料,制备维格列汀聚电解质复合微球,并采用中心复合设计对其进行优化。

方法

选择傅里叶变换红外光谱、扫描电子显微镜、差示扫描量热法、粒径、药物包封效率、X 射线衍射和 10 小时药物释放度来评价所制备的微球。考察了独立变量(海藻酸钠和 Eudragit RL100 的浓度)对依赖响应的影响。

结果

XRD、SEM、DSC 和 FTIR 的解释证实了没有药物赋形剂的干扰,并证实了聚电解质复合微球的形成。对于复合微球,在 10 小时后,最大和最小药物释放量分别为 96.23.5%和 89.45%。进一步使用 32 点中心复合设计获得响应面图,优化批的粒径、DEE 和药物释放的数值分别为 0.197、76.30%和 92.15%。

结论

结果表明,两种聚合物(海藻酸钠和 Eudragit RL100)的组合适合提高亲水性药物(维格列汀)的包封效率。中心复合设计(CCD)技术是获得维格列汀聚电解质复合微球最佳药物传递系统的有效工具。

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