Omer Ahmed M, Ahmed Maha S, El-Subruiti Gehan M, Khalifa Randa E, Eltaweil Abdelazeem S
Polymer Materials Research Department, Advanced Technology and New Materials Research Institute (ATNMRI), City of Scientific Research and Technological Applications (SRTA-City), New Borg El-Arab City, Alexandria 21934, Egypt.
Chemistry Department, Faculty of Science, Alexandria University, P.O. Box 426 Ibrahimia, Alexandria 21321, Egypt.
Pharmaceutics. 2021 Mar 5;13(3):338. doi: 10.3390/pharmaceutics13030338.
To develop an effective pH-sensitive drug carrier, alginate (Alg), carboxymethyl chitosan (CMCs), and aminated chitosan (AmCs) derivatives were employed in this study. A simple ionic gelation technique was employed to formulate Alg-CMCs@AmCs dual polyelectrolyte complexes (PECs) microcapsules as a pH-sensitive carrier for efficient encapsulation and release of diclofenac sodium (DS) drug. The developed microcapsules were characterized by Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analyzer (TGA), and scanning electron microscope (SEM). The results clarified that formation of dual PECs significantly protected Alg microcapsules from rapid disintegration at colon conditions (pH 7.4), and greatly reduced their porosity. In addition, the dual PECs microcapsules can effectively encapsulate 95.4% of DS-drug compared to 86.3 and 68.6% for Alg and Alg-CMCs microcapsules, respectively. Higher DS-release values were achieved in simulated colonic fluid [SCF; pH 7.4] compared to those obtained in simulated gastric fluid [SGF; pH 1.2]. Moreover, the drug burst release was prevented and a sustained DS-release was achieved as the AmCs concentration increased. The results confirmed also that the developed microcapsules were biodegradable in the presence of the lysozyme enzyme. These findings emphasize that the formulated pH-sensitive microcapsules could be applied for the delivery of diclofenac sodium.
为开发一种有效的pH敏感药物载体，本研究采用了海藻酸钠（Alg）、羧甲基壳聚糖（CMCs）和胺化壳聚糖（AmCs）衍生物。采用简单的离子凝胶技术制备了Alg-CMCs@AmCs双聚电解质复合物（PEC）微胶囊，作为一种pH敏感载体，用于高效包封和释放双氯芬酸钠（DS）药物。通过傅里叶变换红外光谱（FT-IR）、热重分析仪（TGA）和扫描电子显微镜（SEM）对所制备的微胶囊进行了表征。结果表明，双PEC的形成显著保护了Alg微胶囊在结肠条件（pH 7.4）下不快速崩解，并大大降低了其孔隙率。此外，双PEC微胶囊能有效包封95.4%的DS药物，而Alg和Alg-CMCs微胶囊分别为86.3%和68.6%。与在模拟胃液[SGF；pH 1.2]中获得的值相比，在模拟结肠液[SCF；pH 7.4]中获得了更高的DS释放值。此外，随着AmCs浓度的增加，药物的突释得到了抑制，并实现了DS的持续释放。结果还证实，所制备的微胶囊在溶菌酶存在下可生物降解。这些发现强调，所制备的pH敏感微胶囊可用于双氯芬酸钠的递送。
