Citation: Sinapi Umutoni, Hao Zhang, Jiayue Guo, Zehui Yu, Hao Shao, Xiaoli Yi, Chunmeng Sun, Lei Luo, Yinglan Yu. Oral anticancer drug delivery: Strategies for improving bioavailability[J]. Chinese Chemical Letters, ;2026, 37(12): 112362. doi: 10.1016/j.cclet.2026.112362 shu

Oral anticancer drug delivery: Strategies for improving bioavailability

Sinapi Umutoni ^{a, 1} ,
Hao Zhang ^{c, 1} ,
Jiayue Guo ^a ,
Zehui Yu ^a ,
Hao Shao ^a ,
Xiaoli Yi ^d ,
Chunmeng Sun ^{b, *,} ,
Lei Luo ^{a, *,} ,
Yinglan Yu ^{a, *,}

a.
College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China
b.
NMPA Key Laboratory for Research and Evaluation of Pharmaceutical Preparation and Excipients, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
c.
Medical Laboratory Department, Chongqing Changshou District People's Hospital, Chongqing 401220, China
d.
Department of Clinical Pharmacy, West China Hospital of Sichuan University, Chengdu 610041, China

suncmpharm@cpu.edu.cn

drluolei@swu.edu.cn

yuyinglan@swu.edu.cn

Received Date: 12 November 2025
Revised Date: 29 December 2025
Accepted Date: 3 January 2026
Available Online: 5 January 2026

Figures(7)

The oral administration of anticancer drugs emerged as a promising approach, offering improved patient acceptability, convenience for chronic treatment regimens, and the potential for optimized therapeutic outcomes. However, the clinical translation of oral anticancer agents remains hindered by gastrointestinal tract barriers, including poor aqueous solubility, variable pH, enzymatic degradation, mucus layer, limited intestinal epithelial permeation, and the influence of gut microbiota. To address these challenges, a wide range of innovative strategies have been explored, such as pH modifiers, enzyme inhibitors, permeation enhancers, prodrug design, and nanoparticle-based drug delivery systems. In addition, the integration of artificial intelligence and machine learning with nanomedicine offers new opportunities to accelerate formulation development, optimize drug design, and overcome existing absorption barriers. This review provides a comprehensive analysis of the current landscape of oral anticancer drug delivery and explores advanced strategies to enhance bioavailability, offering insights into future directions for improved therapeutic efficacy.
- Oral delivery,
- Anticancer drugs,
- Gastrointestinal barriers,
- Nanomedicine,
- Bioavailability
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沈阳化工大学材料科学与工程学院沈阳 110142