pH-responsive chitosan-mediated spherical mesoporous silica microspheres for high loading and controlled delivery of 5-Fluorouracil

• Published in: Carbohydrate research Vol. 543; p. 109206
• Main Authors: Zhang, Qianqian, Wan, Tong, Jin, Guocheng, Xu, Shiai
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier Ltd 01.09.2024
• Subjects: 5-Fluorouracil; Chitosan; Drug release kinetics; Mesoporous silica nanoparticles; pH-sensitive; Sustained-release; Mesoporous silica nanoparticles; pH-sensitive; Drug release kinetics; Sustained-release; Chitosan; 5-Fluorouracil
• ISSN: 0008-6215; 1873-426X; 1873-426X
• DOI: 10.1016/j.carres.2024.109206

The objective of this study is to develop a drug carrier to overcome the inherent drawbacks of 5-Fluorouracil (5-Fu), including low bioavailability, short half-life, and systemic toxicity. In the present work, mesoporous silica nanoparticles (MSNs) capped by chitosan (CS) to encapsulate 5-Fu (5-Fu MSNs/CS) were fabricated by the sol-gel process, ultrasonic impregnation, and emulsion cross-linking. The 5-Fu MSNs/CS microspheres exhibit pH-responsive drug release and remarkable drug encapsulation capacity, as well as perfect sphericity, high specific surface area (680.62 cm2/g), and uniform particle size (2.64 ± 0.05 μm). The drug-loading content and encapsulation efficiency are 14.12 ± 0.53 % and 82.21 ± 2.13 %, respectively. The cumulative release of 5-Fu from MSNs/CS microspheres is fast and sustained at pH 5.0 (89.56 ± 0.97 %) compared to that at pH 7.4 (57.88 ± 0.91 %) in 96 h, and it is Fickian diffusion controlled. In conclusion, the MSNs/CS microspheres prepared in this study could be potential carriers for 5-Fu delivery. [Display omitted] •Mesoporous silica nanoparticles (MSNs) with a uniform particle size were prepared.•GA cross-linked chitosan was wrapped onto the MSNs via electrostatic interaction.•Drug release was controlled by pH-responsive chitosan.•5-Fu MSNs/CS microspheres exhibited high DL (14.12 %) and EE (82.21 %).