Novel Natrosol/Pectin-co-poly (acrylate) based pH-responsive polymeric carrier system for controlled delivery of Tapentadol Hydrochloride

用于控制输送盐酸他喷他多的新型 Natrosol/果胶-共聚(丙烯酸酯)型 pH 响应性聚合物载体系统

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作者:Nadiah Zafar, Asif Mahmood, Sehar Ilyas, Hira Ijaz, Rai Muhammad Sarfraz, Wael A Mahdi, Mounir M Salem-Bekhit, Mohamed A Ibrahim, Yacine Benguerba, Barbara Ernst

Conclusion

The developed IPNs were found to be an excellent system for the controlled delivery of Tapentadol Hydrochloride.

Methods

Novel Tapentadol Hydrochloride-loaded Natrosol-Pectin based IPNs were formulated by using the free radical polymerization technique. Co-polymerization of Acrylic Acid (AA) with Natrosol and Pectin was performed by using Methylene bisacrylamide (MBA). Ammonium persulfate (APS) was used as the initiator of crosslinking process. The impact of ingredients i.e. Natrosol, Pectin, MBA, and Acrylic Acid on the gel fraction, porosity, swelling (%), drug loading, and drug release was investigated. FTIR, DSC, TGA, SEM and EDX studies were conducted to confirm the grafting of polymers and to evaluate the thermal stability and surface morphology of the developed IPNs.

Results

Swelling studies exhibited an increase in swelling percentage from 84.27 to 91.17% upon increasing polymer (Natrosol and Pectin) contents. An increase in MBA contents resulted in a decrease in swelling from 85 to 67.63%. Moreover, the swelling was also observed to increase with higher AA contents. Significant drug release was noted at higher pH instead of gastric pH value. Oral toxicological studies revealed the nontoxic and biocompatible nature of Natrosol-Pectin IPNs. Interpretation &

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