International Journal of Nanomedicine
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2026
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IF 8.7
Jieying Zhou,Wei Luo,Lingxin Zeng,Shihao Xu,Ruohan Wu,Jiaqi Lu,Ying Li,Wei Xiong
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.
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高影响因子
INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY
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2019
·Vol. 54
·期 6
·2266-2276
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IF 2.281
Lingling Wang,Xiuhua Zhao,Fengjian Yang,Weiwei Wu,Yanjie Liu,Li Wang,Lu Wang,Zijian Wang
Summary The ginkgo biloba extract (GBE) nanoparticles were successfully prepared by adopting the liquid anti-solvent precipitation (LASP) method to enhance the antioxidant activity and oral bioavailability of GBE. Under the optimum preparation conditions, the particle size of GBE nanoparticles had reached 76.90 nm. Moreover, the antioxidant activity and intestinal transmittance of GBE nanoparticles were tested before and after the simulated in vitro digestion, which were both significantly higher than that of raw GBE. Significantly, the AUC ( 0→t) value of flavonoids and terpene lactones in GBE nanoparticles were 2.20 and 2.24 times of that in raw GBE, respectively. What cannot be ignored was that the residual amount of ethanol and n-hexane meets the safety standards for food.
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高影响因子
CHEMICAL ENGINEERING & TECHNOLOGY
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2016
·Vol. 39
·期 7
·1301-1308
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IF 2.385
Yuan Gang Zu,Lingling Wang,Xiuhua Zhao,Yuanyuan Li,Weiwei Wu,Chang Zu,Yannian Huang,Mingfang Wu,Ziqi Feng
The content of flavonoids in Gingko biloba extract (GBE) could be increased by antisolvent recrystallization (ASR) using ethanol as solvent and hexane as antisolvent. By means of the single-factor method, the effect of main factors on the content of flavonoids in purified GBE was investigated. Under optimal conditions, the content of flavonoids and ginkgo terpene lactones in purified GBE could be significantly enhanced. In addition, the content of total ginkgolic acid in purified GBE was reduced. The morphologies of raw and purified GBE were characterized by scanning electron microscopy. It was found that the particle size of purified GBE was much smaller than that of raw GBE. At the same time, the saturated solubility could be improved by more than four times.
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高影响因子
RSC Advances
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2016
·Vol. 6
·期 81
·77346-77357
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IF 3.289
Lingling Wang,Xiuhua Zhao,Yuangang Zu,Weiwei Wu,Yuanyuan Li,Chang Zu,Yin Zhang
Ginkgo biloba extract nanoparticles were successfully prepared by the method of emulsion solvent evaporation combined with freeze-drying (ESE-FR). By the single-factor method, the optimal parameters were determined: the concentration of GBE was 5 mg mL−1, volume ratio of water to organic phase was 1 : 1, homogenate speed and time were 12 000 rpm and 3 min, respectively, and homogeneous pressure and times were 500 bar and 3, respectively. The mean particle size (MPS) of the GBE nano-emulsion prepared using the optimized conditions was 56.0 nm. SEM detection results indicated that the morphology of raw GBE was irregular. But the morphology of GBE nanoparticles was close to spherical and the particle size of GBE nanoparticles was much smaller than that of raw GBE. The particle size of the freeze-dried powder was 277.0 nm. The characteristics of prepared GBE nanoparticles were detected via XRD, DSC and TG, which showed that the crystal structure of GBE nanoparticles was the same as that of raw GBE. Through the test of solubility and dissolution in vitro, the solubility and dissolution of GBE nanoparticles in artificial gastric juice, artificial intestinal juice and deionized water were obviously improved compared with that of raw GBE. The results of bioavailability showed that the Area Under Plasma Concentration Curves (AUC) of flavonoids and terpene lactones in GBE nanoparticles were improved about 1.81 times and 1.75 times compared with that in raw GBE, respectively. In addition, the residual amounts of chloroform and ethanol were less than the ICH limit for class II.
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高影响因子
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