Department of Pharmaceutical Sciences, Pharmaceutics Research Projects Laboratory, Dr. Hari Singh Gour Central University, Sagar, India.
Department of Materials Engineering, Indian Institute of Science, Bangalore, India.
J Microencapsul. 2021 May;38(3):151-163. doi: 10.1080/02652048.2020.1851787. Epub 2021 Jan 28.
The present research was aimed to develop thiolated polyacrylic acid (TPA) based microspheres (MSPs) containing famotidine (FX) and clarithromycin (CLX).
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), H-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 400rpm for 8 hr.
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 mucoadhesive study and drug release studies demonstrated that microspheres showed mucoadhesive property. In 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).
The prepared TPA based mucoadhesive microspheres can be utilised as carriers for the treatment of peptic ulcer caused by which will offer enhanced residence time for the rational drug combination in the gastric region.
本研究旨在开发载有法莫替丁（FX）和克拉霉素（CLX）的巯基化聚丙烯酸（TPA）微球（MSP）。
在 1-乙基-3-（3-二甲基氨基丙基）碳二亚胺盐酸盐（EDAC）的存在下，由聚丙烯酸和 L-半胱氨酸合成 TPA。使用傅里叶变换红外光谱（FT-IR）、质子核磁共振波谱（ 1 H-NMR）、粉末 X 射线衍射（P-XRD）方法和 ζ 电位对制备的 TPA 进行了表征。这些分析工具支持了 TPA 的形成。采用乳化溶剂蒸发法制备巯基微球，聚合物浓度为 0.75%w/v，搅拌 8 小时，转速为 400rpm。
优化配方的平均粒径和 ζ 电位分别为 25.2±1.87μm 和-26.68mV。优化配方的包封效率分别为 FX 的 67.20%和 CLX 的 70.20%。所开发的微球仅在 4 小时内从 0.5 膨胀到 0.9。黏膜粘附研究和药物释放研究表明，微球具有黏膜粘附性。在药物释放研究中，观察到微球在 8 小时内释放 FX 和 CLX 分别为 58.68%和 60.48%。与普通微球（2.6±0.4h）相比，巯基化微球的粘附时间更长（7.0±0.8h）。
所制备的基于 TPA 的黏附性微球可用作治疗由引起的消化性溃疡的载体，可使胃区合理药物组合的停留时间延长。
