Poly(maleic anhydride-alt-1-octadecene)-based bioadhesive nanovehicles improve oral bioavailability of poor water-soluble gefitinib.

Guanru Wang, Yaru Xie, Xindi Qian, Xinyue Zhang, Yanqiang Shan, Minghui Zhang, Jie Li, Zhiwen Zhang, Yaping Li

Drug development and industrial pharmacy 2022 Mar

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The poor water solubility and inadequate oral bioavailability of gefitinib (Gef) remain a critical issue to achieve the therapeutic outcomes. Herein, we designed a poly(maleic anhydride-alt-1-octadecene) (PMA/C18) based lipid nanovehicle (PLN) to improve the intestinal absorption and oral bioavailability of poorly water-soluble Gef. PLN was nanometer-sized particles, and Gef was dispersed in the PLN formulation as amorphous or molecular state. At 4 h of oral administration, the tissue concentration of Gef in duodenum, jejunum, and ileum was profoundly enhanced 3.37-, 8.94-, and 8.09-fold by PLN when comparing to the counterpart lipid nanovehicle. Moreover, the oral bioavailability of Gef was significantly enhanced 2.48-fold by the PLN formulation when comparing to the free drug suspension. Therefore, this study provides an encouraging bioadhesive delivery platform to improve the oral delivery of poorly water-soluble drugs.

Citation

Guanru Wang, Yaru Xie, Xindi Qian, Xinyue Zhang, Yanqiang Shan, Minghui Zhang, Jie Li, Zhiwen Zhang, Yaping Li. Poly(maleic anhydride-alt-1-octadecene)-based bioadhesive nanovehicles improve oral bioavailability of poor water-soluble gefitinib. Drug development and industrial pharmacy. 2022 Mar;48(3):109-116