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已发表论文
气泡驱动药物递送系统增强难溶性穿心莲内酯的口服吸收和退热疗效
Authors Zhou J , Luo W, Zeng L , Xu S, Wu R, Lu J, Li Y, Xiong W
Received 30 October 2025
Accepted for publication 23 January 2026
Published 3 February 2026 Volume 2026:21 574265
DOI https://doi.org/10.2147/IJN.S574265
Checked for plagiarism Yes
Review by Single anonymous peer review
Peer reviewer comments 2
Editor who approved publication: Dr RDK Misra
Jieying Zhou,1,* Wei Luo,1,* Lingxin Zeng,1,* Shihao Xu,2 Ruohan Wu,3 Jiaqi Lu,4 Ying Li,1 Wei Xiong1
1School of Pharmacy, Shenzhen University Medical School, Shenzhen University, Shenzhen, 518055, People’s Republic of China; 2School of Chinese Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016, People’s Republic of China; 3Shenzhen College of International Education, Shenzhen, 518043, People’s Republic of China; 4Production Center, Raytor Instruments, Shenzhen, 518001, People’s Republic of China
*These authors contributed equally to this work
Correspondence: Ying Li, School of Pharmacy, Shenzhen University Medical School, Shenzhen University, 1066 Xueyuan Avenue, Nanshan District, Shenzhen, 518055, People’s Republic of China, Email li.ying@szu.edu.cn Wei Xiong, School of Pharmacy, Shenzhen University Medical School, Shenzhen University, 1066 Xueyuan Avenue, Nanshan District, Shenzhen, 518055, People’s Republic of China, Tel +86075526913026, Email weixiong@szu.edu.cn
Purpose: While bubble-carrier systems hold great promise for enhancing the oral bioavailability of poorly water-soluble drugs, a deeper understanding of their underlying absorption mechanisms is still required. This study aimed to address this gap by developing a bubble-driven delivery system (BDDS) using the poorly water-soluble andrographolide (AG) as a model drug, and systematically evaluating its solubilization capacity and intestinal permeability.
Methods: The BDDS was optimized through the screening of effervescent formulations (citric acid: Na2CO3 = 6:5) and bile salts (sodium deoxycholate, SDC). Its performance was comprehensively assessed via in vitro dissolution tests, an everted intestinal sac assay, Caco-2 cell monolayer experiments, pharmacokinetic studies, and yeast-induced fever rat models.
Results: The BDDS achieved 75.0%– 88.7% dissolution in gastrointestinal pH media, which was markedly superior to that of commercial dripping pills (DP; 30.5– 50.2%). Its apparent permeability coefficient was 7.7-fold and 3.6-fold higher than that of free AG and DP, respectively. Transport studies indicated that SDC enhanced AG permeability primarily via the apical sodium-dependent bile acid transporter (ASBT)-mediated pathway, a mechanism further confirmed by inhibition with linerixibat. The relative oral bioavailability of BDDS versus DP reached 257.1%. BDDS demonstrated enhanced efficacy by significantly inhibiting key pro-inflammatory cytokines and thermoregulatory mediators in yeast-induced fever rats.
Discussion: The BDDS effectively overcomes AG’s low solubility (by SDC solubilization and CO2 bubbles) and permeability (via ASBT transport), outperforming conventional formulations in terms of preparation simplicity and storage stability.
Conclusion: BDDS is a promising strategy to improve oral absorption and therapeutic efficacy of BCS Class IV drugs like AG, with ASBT-mediated transport as a key mechanism.
Keywords: bubble, poorly water-soluble, intestinal permeability, oral bioavailability, andrographolide
1School of Pharmacy, Shenzhen University Medical School, Shenzhen University, Shenzhen, 518055, People’s Republic of China; 2School of Chinese Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016, People’s Republic of China; 3Shenzhen College of International Education, Shenzhen, 518043, People’s Republic of China; 4Production Center, Raytor Instruments, Shenzhen, 518001, People’s Republic of China
*These authors contributed equally to this work
Correspondence: Ying Li, School of Pharmacy, Shenzhen University Medical School, Shenzhen University, 1066 Xueyuan Avenue, Nanshan District, Shenzhen, 518055, People’s Republic of China, Email li.ying@szu.edu.cn Wei Xiong, School of Pharmacy, Shenzhen University Medical School, Shenzhen University, 1066 Xueyuan Avenue, Nanshan District, Shenzhen, 518055, People’s Republic of China, Tel +86075526913026, Email weixiong@szu.edu.cn
Purpose: While bubble-carrier systems hold great promise for enhancing the oral bioavailability of poorly water-soluble drugs, a deeper understanding of their underlying absorption mechanisms is still required. This study aimed to address this gap by developing a bubble-driven delivery system (BDDS) using the poorly water-soluble andrographolide (AG) as a model drug, and systematically evaluating its solubilization capacity and intestinal permeability.
Methods: The BDDS was optimized through the screening of effervescent formulations (citric acid: Na2CO3 = 6:5) and bile salts (sodium deoxycholate, SDC). Its performance was comprehensively assessed via in vitro dissolution tests, an everted intestinal sac assay, Caco-2 cell monolayer experiments, pharmacokinetic studies, and yeast-induced fever rat models.
Results: The BDDS achieved 75.0%– 88.7% dissolution in gastrointestinal pH media, which was markedly superior to that of commercial dripping pills (DP; 30.5– 50.2%). Its apparent permeability coefficient was 7.7-fold and 3.6-fold higher than that of free AG and DP, respectively. Transport studies indicated that SDC enhanced AG permeability primarily via the apical sodium-dependent bile acid transporter (ASBT)-mediated pathway, a mechanism further confirmed by inhibition with linerixibat. The relative oral bioavailability of BDDS versus DP reached 257.1%. BDDS demonstrated enhanced efficacy by significantly inhibiting key pro-inflammatory cytokines and thermoregulatory mediators in yeast-induced fever rats.
Discussion: The BDDS effectively overcomes AG’s low solubility (by SDC solubilization and CO2 bubbles) and permeability (via ASBT transport), outperforming conventional formulations in terms of preparation simplicity and storage stability.
Conclusion: BDDS is a promising strategy to improve oral absorption and therapeutic efficacy of BCS Class IV drugs like AG, with ASBT-mediated transport as a key mechanism.
Keywords: bubble, poorly water-soluble, intestinal permeability, oral bioavailability, andrographolide