Abstract

Aim

The present research was aimed to develop thiolated polyacrylic acid (TPA) based microspheres (MSPs) containing famotidine (FX) and clarithromycin (CLX).

Methods

TPA was synthesised from polyacrylic acid and l-cysteine in the presence of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDAC). The prepared TPA was characterised using FT-IR (Fourier transform-infra red), ¹H-NMR (proton nuclear magnetic resonance) spectroscopy, P-XRD (powder X ray diffraction) method, and zeta potential. The analytical tools have supported the formation of TPA. The thiolated microspheres were prepared by emulsion solvent evaporation method using 0.75% w/v polymer concentration and stirring at 400 rpm for 8 hr.

Results

The average particle size and zeta potential of optimised formulation was found to be 25.2 ± 1.87 μm and –26.68 mV, respectively. The entrapment efficiency of the optimised formulation was obtained 67.20% for FX and 70.20% for CLX. The developed microspheres were swelled only in 4 h from 0.5 to 0.9. The in vitro mucoadhesive study and in vitro drug release studies demonstrated that microspheres showed mucoadhesive property. In in vitro drug release studies, the release of FX and CLX were observed to be 58.68% and 60.48%, respectively from microspheres in 8 h. The thiolated microspheres showed higher adhesion time (7.0 ± 0.8 h) in comparison to the plain microspheres (2.6 ± 0.4 h).

Conclusion

The prepared TPA based mucoadhesive microspheres can be utilised as carriers for the treatment of peptic ulcer caused by Helicobacter pylori which will offer enhanced residence time for the rational drug combination in the gastric region.

中文翻译：

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用于法莫替丁和克拉霉素程序化递送的粘膜粘附性胃滞留微粒系统

摘要

目标

本研究旨在开发含有法莫替丁 (FX) 和克拉霉素 (CLX) 的硫醇化聚丙烯酸 (TPA) 基微球 (MSP)。

方法

TPA 是在 1-乙基-3-(3-二甲基氨基丙基) 碳二亚胺盐酸盐 (EDAC) 存在下由聚丙烯酸和l-半胱氨酸合成的。使用 FT-IR（傅里叶变换红外）、¹ H-NMR（质子核磁共振）光谱、P-XRD（粉末 X 射线衍射）方法和 zeta 电位对制备的 TPA 进行了表征。分析工具支持了 TPA 的形成。硫醇化微球通过乳液溶剂蒸发法制备，使用0.75% w/v聚合物浓度并以400  rpm搅拌8小时。

结果

发现优化配方的平均粒径和 zeta 电位分别为 25.2 ± 1.87 μm 和 –26.68 mV。FX 和 CLX 的优化配方的包封率分别为 67.20% 和 70.20%。开发的微球仅在 4 小时内从 0.5 膨胀到 0.9。体外粘膜粘附研究和体外药物释放研究表明微球具有粘膜粘附特性​​。在体外药物释放研究中，观察到 FX 和 CLX 在 8 小时内从微球中的释放量分别为 58.68% 和 60.48%。与普通微球 (2.6 ± 0.4 h) 相比，硫醇化微球显示出更高的粘附时间 (7.0 ± 0.8 h)。

结论

所制备的TPA基黏膜粘附微球可作为治疗幽门螺杆菌引起的消化性溃疡的载体，为合理的药物组合在胃部提供更长的停留时间。