Biopharmaceutics classification and intestinal absorption study of apigenin

Zhang, Jianjun; Liu, Dapeng; Huang, Yanting; Gao, Yuan; Qian, Shuai

doi:10.1016/j.ijpharm.2012.07.002

Cited by 151 publications

(87 citation statements)

References 59 publications

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“…Briefly, 0.5 ml INS (4 mg/ml) plus surfactin (4 mg/ml) or INS (4 mg/ml) alone was syringed into a 5-cm jejunum for transport study, which was incubated in oxygenated Kreb's-Ringer buffer at 37 C with smooth shaking. INS concentration in the incubation buffer was quantified by ELISA and the effective permeability (Peff) was calculated by the methods described previously (Yin et al, 2009;Zhang et al, 2012).…”

Section: Determination Of Ins Absorbed By Intestine Ex Vivo and In Vivomentioning

confidence: 99%

A natural lipopeptide of surfactin for oral delivery of insulin

et al. 2016

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Surfactin, a natural lipopeptide produced by Bacillus, is gaining attention for potentially biomedical and pharmaceutical applications. Here, surfactin was assayed for oral delivery of insulin (INS) by its ability to bind to and promote protein to penetrate through the cell membrane. Analysis by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, surfactin was found to form co-precipitates with INS to protect it from acidic and enzymatic attack in the gastrointestinal tract. Further analysis by non-reductive electrophoresis showed surfactin could bind to INS forming heteropolymers. Analysis with circular dichroism, we found this binding significantly influenced the INS structure with decreased rigid a-helix and b-turn, but with increased flexible b-sheet and random coil. The change with more flexible structure was favorable for INS to penetrate through the cell membrane. Fluorescence spectra analysis also showed surfactin could lead Phe and Tyr in the inner of INS exposed outside, further promoting INS permeabilization by improving the hydrophobic-lipophilic interactions between INS and cell membrane. As a result, the effective permeability (Peff) of INS plus surfactin was 4.3 times of that of INS alone. In vivo assay showed oral INS with surfactin displayed excellent hypoglycemic effects with a relative bioavailability of 12.48% and 5.97% in diabetic mice and non-diabetic dogs, respectively. Summary, surfactin is potential for oral delivery of INS by its role as an effective protease inhibitor and permeability enhancer.

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Section: Determination Of Ins Absorbed By Intestine Ex Vivo and In Vivomentioning

confidence: 99%

A natural lipopeptide of surfactin for oral delivery of insulin

et al. 2016

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“…[7][8][9][10] However, the clinical use of apigenin is restricted, owing to its poor biopharmaceutical properties, including water insolubility and poor absorption. 11 Although apigenin is predicted to be safe for lung cancer treatment, similar to the majority of antitumor drugs, resistance could develop during the course of treatment, which could result in therapeutic failure. These drawbacks could be overcome by using a liposomal form of apigenin and combining it with other chemotherapeutic drugs.…”

Section: Introductionmentioning

confidence: 99%

Synergistic apoptotic effects of apigenin TPGS liposomes and tyroservatide: implications for effective treatment of lung cancer

Jin¹,

Yang²,

Zhang³

2017

IJN

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To develop an alternative treatment for lung cancer, a combination of two potent chemotherapeutic agents – liposomal apigenin and tyroservatide – was developed. The therapeutic potential of this combination was investigated using A549 cells. Apigenin and tocopherol derivative-containing D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) liposomes might improve the delivery of apigenin to tumor cells, both in vitro and in vivo. Importantly, compared to either agent alone, the combination of apigenin TPGS liposomes and tyroservatide exhibited superior cytotoxicity, induced stronger G2 arrest, and suppressed A549 cancer cell invasion at a lower dose. The proapoptotic synergistic effects were also observed in A549 cells using terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling, flow cytometry, and Western blot analysis. More importantly, in vivo results showed that the combination of apigenin TPGS liposomes and tyroservatide exhibited tumor-growth inhibitory effects in A549 cell-bearing mice. In conclusion, our study showed that this combination therapy could serve as a promising synergistic therapeutic approach to improve outcomes in patients with lung cancer.

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“…It has an antiproliferative activity against pancreatic, colorectal, skin, neuroblastoma, and breast cancer cell lines. [1][2][3][4][5] However, the oral bioavailability of AP is relatively low because of its low lipid (0.001-1.63 mg/mL in nonpolar solvents) 6 and water (2.16 µg/mL in water) 7 solubility, which has severely limited its clinical development. Therefore, it is necessary to develop new technologies or formulations to improve AP bioavailability.…”

Section: Introductionmentioning

confidence: 99%

“…According to the Biopharmaceutics Classification System, AP is a class II drug with high intestinal membrane permeability and poor solubility, 7 which can be improved by increasing the dissolution rate of the drug. Numerous studies have shown that solid dispersion (SD) is a successful and widely used approach to enhancing the dissolution rate of poorly water-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

Enhanced bioavailability of apigenin via preparation of a carbon nanopowder solid dispersion

Ding¹,

Zhang²,

Song³

et al. 2014

IJN

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In this study, a novel carbon nanopowder (CNP) drug carrier was developed to improve the oral bioavailability of apigenin (AP). Solid dispersions (SDs) of AP with CNP were prepared, and their in vitro drug release and in vivo performance were evaluated. The physicochemical properties of the formulations were examined by differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy. Drug release profiles showed that AP dissolution from the CNP-AP system (weight ratio, 6:1) after 60 minutes improved by 275% compared with that of pure AP. Moreover, the pharmacokinetic analysis of SD formulations in rats showed that the AP area under the curve 0–t value was 1.83 times higher for the CNP-AP system than for pure AP, indicating that its bioavailability was significantly improved. In addition, compared with pure AP, SDs had a significantly higher peak and shorter time to peak. Preliminary intestinal toxicity tests indicated that there was no significant difference in the tissues of the rats treated with the CNP-AP system, rats treated with the CNP alone, and controls. In conclusion, CNP-based SDs could be used for enhancing the bioavailability of poorly water-soluble drugs while also improving drug safety.

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Biopharmaceutics classification and intestinal absorption study of apigenin

Cited by 151 publications

References 59 publications

A natural lipopeptide of surfactin for oral delivery of insulin

A natural lipopeptide of surfactin for oral delivery of insulin

Synergistic apoptotic effects of apigenin TPGS liposomes and tyroservatide: implications for effective treatment of lung cancer

Enhanced bioavailability of apigenin via preparation of a carbon nanopowder solid dispersion

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