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用于治疗消化性溃疡的壳聚糖包衣奥美拉唑-姜黄素载药水凝胶珠的设计与优化

Design and Optimization of Omeprazole-Curcumin-Loaded Hydrogel Beads Coated with Chitosan for Treating Peptic Ulcers.

作者信息

Heikal Eman J, Kaoud Rashad M, Gad Shadeed, Mokhtar Hatem I, Aldahish Afaf A, Alzlaiq Wafa Ali, Zaitone Sawsan A, Moustafa Yasser M, Hammady Taha M

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt.

Faculty of Pharmacy, The University of Mashreq, Baghdad 10001, Iraq.

出版信息

Pharmaceuticals (Basel). 2023 May 27;16(6):795. doi: 10.3390/ph16060795.

DOI:10.3390/ph16060795
PMID:37375745
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10305022/
Abstract

This study aimed to formulate a pharmaceutical dosage form containing omeprazole (OMP) and curcumin (CURC) to treat experimental peptic ulcers. OMP and CURC were preliminarily complexed with hydroxypropyl-β-cyclodextrin for enhancing their solubilization. After that, the combined complex (CURC/OMP) was loaded to alginate beads to sustain their release and then coated with chitosan. Finally, we tested the anti-ulcerogenic impact of the best formula versus free OMP or OMP-only-loaded beads. The formulated spherical beads' diameter ranged from a minimum value of 1.5 ± 0.08 mm to 2.6 ± 0.24 mm; the swelling results ranged from 400.00 ± 8.5% to 800.00 ± 6.2%. The entrapment efficiency was in a range from 60.85 ± 1.01% to 87.44 ± 1.88%. The optimized formula (F8) showed a maximum EE% (87.44 ± 1.88%), swelling (800.00 ± 6.2%), and diameter in the range of 2.60 ± 0.24, with a desirability of 0.941. In the first hour following the administration of the free drug complex, 95% of OMP and 98% of CURC were released. This is unacceptable for medications that require a delayed release in the stomach. The initial drug release from hydrogel beads was 23.19% for CURC and 17.19% for OMP after 2 h and 73.09% for CURC and 58.26% for OMP after 12 h; however, after 24 h, 87.81% of CURC and 81.67% of OMP had been released. The OMP/CURC beads showed a more stable particle size (0.52 ± 0.01 mm) after 6 weeks. In conclusion, the OMP/CURC hydrogel beads give stronger anti-ulcer effectiveness compared to free OMP, CURC-only beads, and OMP-only-loaded beads, indicating a prospective application for managing peptic ulcers.

摘要

本研究旨在制备一种含奥美拉唑（OMP）和姜黄素（CURC）的药物剂型，用于治疗实验性消化性溃疡。OMP和CURC预先与羟丙基-β-环糊精络合以提高其溶解度。之后，将复合络合物（CURC/OMP）载入海藻酸钠珠粒以实现其缓释，然后用壳聚糖包衣。最后，我们测试了最佳配方与游离OMP或仅载有OMP的珠粒相比的抗溃疡效果。所制备的球形珠粒直径范围为最小值1.5±0.08毫米至2.6±0.24毫米；溶胀结果范围为400.00±8.5%至800.00±6.2%。包封率范围为60.85±1.01%至87.44±1.88%。优化配方（F8）显示出最大的包封率（87.44±1.88%）、溶胀率（800.00±6.2%），直径在2.60±0.24范围内，可取性为0.941。在给予游离药物复合物后的第一小时，95%的OMP和98%的CURC被释放。对于需要在胃中延迟释放的药物来说，这是不可接受的。水凝胶珠粒在2小时后CURC的初始药物释放率为23.19%，OMP为17.19%；12小时后CURC为73.09%，OMP为58.26%；然而，24小时后，87.81%的CURC和81.67%的OMP已被释放。6周后，OMP/CURC珠粒显示出更稳定的粒径（0.52±0.01毫米）。总之，与游离OMP、仅含CURC的珠粒和仅载有OMP的珠粒相比，OMP/CURC水凝胶珠粒具有更强的抗溃疡效果，表明其在治疗消化性溃疡方面具有潜在应用前景。

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