Bile acid transporter-mediated oral drug delivery

Deng, Feiyang; Bae, You Han

doi:10.1016/j.jconrel.2020.07.034

Cited by 90 publications

(80 citation statements)

References 190 publications

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“…It has assimilation enhancing ability and acts as solubilizing and permeation enhancing agent. It may enhance the drug permeability and bioavailability of poorly soluble therapeutics ( Deng and Bae, 2020 ). Bile salts absorbed through apical sodium-dependent bile acid transporter (ASBT) in the GIT, and may also act as an enhancer in the oral delivery ( Nurunnabi et al, 2016 ).…”

Section: Introductionmentioning

confidence: 99%

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

Zafar

Alruwaili

Imam

et al. 2021

Saudi Pharmaceutical Journal

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Aim Diabetic (type-2) is a metabolic disease characterized by increased blood glucose level from the normal level. In the present study, apigenin (AG) loaded lipid vesicles (bilosomes: BIL) was prepared, optimized and evaluated for the oral therapeutic efficacy. Experimental AG-BIL was prepared by a thin-film evaporation method using cholesterol, span 60 and sodium deoxycholate. The prepared formulation was optimized by 3-factor and 3-level Box-Behnken design using particle size, entrapment efficiency and drug release as a response. The selected formulation further evaluated for ex-vivo permeation, in vivo pharmacokinetic and pharmacodynamics study. Results The optimized AG bilosomes (AG-BILopt) has shown the vesicle size 183.25 ± 2.43 nm, entrapment efficiency 81.67 ± 4.87%. TEM image showed a spherical shape vesicle with sharp boundaries. The drug release study revealed a significant enhancement in AG release (79.45 ± 4.18%) from AG-BILopt as compared to free AG-dispersion (25.47 ± 3.64%). The permeation and pharmacokinetic studies result revealed 4.49 times higher flux and 4.67 folds higher AUC 0-t than free AG-dispersion. The antidiabetic activity results showed significant (P < 0.05) enhancement in therapeutic efficacy than free AG-dispersion. The results also showed marked improvement in biochemical parameters. Conclusion Our findings suggested, the prepared apigenin loaded bilosomes was found to be an efficient delivery in the therapeutic efficacy in diabetes.

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Section: Introductionmentioning

confidence: 99%

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

Zafar

Alruwaili

Imam

et al. 2021

Saudi Pharmaceutical Journal

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“…The ionically conjugated DL in PMX/DL has been shown to facilitate penetration of a cargo molecule (i.e. PMX) through the cell membrane by ASBT (Pangeni et al., 2019 ; Deng & Bae, 2020 ). In addition, DL, as well as Kolliphor P188 and Labrasol, can increase membrane flexibility to increase drug partitioning across the membrane (Gupta et al., 2013 ; DiMarco et al., 2017 ; Pavlović et al., 2018 ; Jha et al., 2020 ) DA in DL, as well as surfactants in CD, can reversibly open the tight junctions by autophosphorylation of epidermal growth factor receptor (EGFR) or dephosphorylation and rearrangement of zonula occludens-1 (ZO-1), which may facilitate the permeation of PMX or PMX/DL released from PMX/DL-CD through the cell membrane via the paracellular pathway (Raimondi et al., 2008 ; Stojančević et al., 2013 ; Zhou et al., 2013 ; Pavlović et al., 2018 ).…”

Section: Resultsmentioning

confidence: 99%

“…This suggests that the oral absorption of PMX/DL(1:1)-CD increased in a dose-dependent manner. This non-linear relationship between dose and oral absorption of PMX/DL(1:1)-CD may reflect limitations in the intestinal membrane permeation due to ASBT saturation (Kanda et al., 1998 ; Pavlović et al., 2018 ; Deng & Bae, 2020 ).…”

Section: Resultsmentioning

confidence: 99%

Metronomic delivery of orally available pemetrexed-incorporated colloidal dispersions for boosting tumor-specific immunity

et al. 2021

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“…2 ). Due to the scavenging ability and anti-inflammatory effect of potent reactive oxygen species (ROS), the engineering of bile acid-derived prodrugs has been explored for the improvement in oral bioavailability and antitumor activities [ 60 , 61 ]. Among various bile acid-based prodrugs in the current study, cholic acid-tethered tamoxifen with amine headgroup (CA-Tam 3 -Am) presented superior antitumor suppression.…”

Section: Conjugation Strategies Of Slpsmentioning

confidence: 99%

Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery

et al. 2022

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A widely established prodrug strategy can effectively optimize the unappealing properties of therapeutic agents in cancer treatment. Among them, lipidic prodrugs extremely uplift the physicochemical properties, site-specificity, and antitumor activities of therapeutic agents while reducing systemic toxicity. Although great perspectives have been summarized in the progress of prodrug-based nanoplatforms, no attention has been paid to emphasizing the rational design of small-molecule lipidic prodrugs (SLPs). With the aim of outlining the prospect of the SLPs approach, the review will first provide an overview of conjugation strategies that are amenable to SLPs fabrication. Then, the rational design of SLPs in response to the physiological barriers of chemotherapeutic agents is highlighted. Finally, their biomedical applications are also emphasized with special functions, followed by a brief introduction of the promising opportunities and potential challenges of SLPs-based drug delivery systems (DDSs) in clinical application. Graphical Abstract

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Bile acid transporter-mediated oral drug delivery

Cited by 90 publications

References 190 publications

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment

Metronomic delivery of orally available pemetrexed-incorporated colloidal dispersions for boosting tumor-specific immunity

Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery

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