Development of quercetin-loaded electrospun nanofibers through shellac coating on gelatin: Characterization, colon-targeted delivery, and anticancer activity

Quercetin possesses multiple biological activities. To achieve efficient colon-specific release of quercetin, new composite nanofibers were developed by coating pH-responsive shellac on hydrophilic gelatin through coaxial electrospinning. These composite nanofibers contained bead-like structures. The encapsulation efficiency (87.6–98.5 %) and loading capacity (1.4–4.1 %) varied with increasing the initial quercetin addition amount (2.5–7.5 %). FTIR, XRD, and TGA results showed that the quercetin was successfully encapsulated in composite nanofibers in an amorphous state, with interactions occurring among quercetin, gelatin, and shellac.

Highlights

Composite nanofibers containing quercetin were fabricated using shellac and gelatin.

These nanofibers had a pH-responsive surface wettability.

These nanofibers could deliver efficiently quercetin to the colon.

The composite nanofibers achieved the sustained release of quercetin in the colon.

Nanofibers showed enhanced anticancer effects against HCT-116 cells.

Composite nanofibers had pH-responsive surface wettability due to the shellac coating. In vitro digestion experiments showed that these composite nanofibers were highly stable in the upper gastrointestinal tract, with quercetin release ranging from 4.75 % to 12.54 %. In vivo organ distribution and pharmacokinetic studies demonstrated that quercetin could be sustainably released in the colon after oral administration of composite nanofibers. Besides, the enhanced anticancer activity of composite nanofibers was confirmed against HCT-116 cells by analyzing their effect on cell viability, cell cycle, and apoptosis. Overall, these novel composite nanofibers could deliver efficiently quercetin to the colon and achieve its sustained release, thus potential to regulate colon health. This system is also helpful in delivering other bioactives to the colon and exerting their functional effects.

Materials

Shellac was obtained from Yuanye Biotechnology Co., Ltd. (Shanghai, China). Gelatin (Type B, Bloom 250), quercetin (97 %), pepsin (3000 U/mg), and trypsin (250 U/mg) were the products of Aladdin Chemistry Co., Ltd. (Shanghai, China). The cell counting kit (CCK-8) was from Meilun Biotechnology (Dalian, China). The cell cycle and apoptosis detection kits were purchased from KGI Biotechnology (Nanjing, China).

Shu-Fang Li, Teng-Gen Hu, Hong Wu, Development of quercetin-loaded electrospun nanofibers through shellac coating on gelatin: Characterization, colon-targeted delivery, and anticancer activity, International Journal of Biological Macromolecules, Volume 277, Part 2, 2024, 134204, ISSN 0141-8130
https://doi.org/10.1016/j.ijbiomac.2024.134204.

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