Self-micelle formation and the incorporation of lipid in the formulation affect the intestinal absorption of Panax notoginseng

Xiong, Jing; Guo, Zhixiong; Huang, Luosheng; Meng, Boyu; Ping, Qineng

doi:10.1016/j.ijpharm.2008.04.016

Cited by 43 publications

(28 citation statements)

References 22 publications

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“…The presence of an amphiphilic molecule in aqueous solution decreases the surface tension significantly because the surfactant concentration increases until micelles form (Xiong et al, 2008). The CMC of the biosurfactant aqueous solution was estimated to be 1.5 mg mL À1 for the commercial saponins and 12.1 mg mL À1 for the BGR saponins, which were based on the first derivative of the cubic equation when setting, dSTF=dCON ¼ 0 where STF is the surface tension of the solution and CON is the biosurfactant concentration.…”

Section: Critical Micellar Concentrationmentioning

confidence: 99%

Obtaining annatto seed oil miniemulsions by ultrasonication using aqueous extract from Brazilian ginseng roots as a biosurfactant

María

Silva

Santos

et al. 2016

Journal of Food Engineering

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a b s t r a c tThe purpose of this study was to produce an oil-in-water (O/W) emulsion of d-tocotrienol-rich oil obtained from annatto seeds by a supercritical fluid extraction process. The effects of emulsification by ultrasound (US) were evaluated and compared to emulsification by dispax reactor (DR) at similar energy densities. Saponin-rich extract from Brazilian ginseng roots (BGR) was obtained from BGR by pressurized liquid extraction and used as a biosurfactant. A model O/W emulsion system was prepared with soybean oil and commercial saponin. The influence of the emulsification process, energy density, oil type, biosurfactant type and biosurfactant concentration on the size and stability of the resulting droplets was examined through the experimental design and proper statistical analysis. The results showed that US produced more stable emulsion with smaller droplet sizes in comparison with the DR device at the same energy density. In general, increasing the energy density helped to reduce the emulsion droplet size. The minimum average droplet size observed in the mini-emulsions was 0.35 lm. The data show that both biosurfactants were capable of forming emulsions containing relatively small droplets (<0.83 lm) andwere rather stable (96-99%), with some creaming. The emulsion droplets also showed a surface potential of approximately À49 mV because of the adsorbed biosurfactants, which minimized the flocculation of the oil droplets. These results indicate that BGR-extracted saponin might be an attractive biosurfactant choice for emulsion formulations for use in food and beverage products.

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Section: Critical Micellar Concentrationmentioning

confidence: 99%

Obtaining annatto seed oil miniemulsions by ultrasonication using aqueous extract from Brazilian ginseng roots as a biosurfactant

María

Silva

Santos

et al. 2016

Journal of Food Engineering

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“…11 The formation of self-micelles might reduce the absorption rate and amount of ASD absorbed from gastrointestinal tract.…”

Section: Discussionmentioning

confidence: 99%

“…10,11 It seemed that a W/O microemulsion was suitable for ASD. However, phase inversion happened frequently in vivo when the W/O microemulsion formulation was diluted with gastrointestinal fluid, leading to the leakage of compounds into the aqueous media and loss of absorption enhancement.…”

Section: Introductionmentioning

confidence: 99%

“…12 In oils, some hydrophobic esters and their hydrolysis products by pancreatic lipase could significantly promote intestinal absorption of poorly absorbed drugs. 10,11,13 Nevertheless, emulsions would form when these hydrophobic esters are diluted with gastrointestinal fluid, leading to a longer release time and a delayed absorption of drugs in vivo, 10,11 which is undesired for any drug.…”

Section: Introductionmentioning

confidence: 99%

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Preparation and evaluation of a self-nanoemulsifying drug delivery system loaded with Akebia saponin D–phospholipid complex

Shen¹,

Bi²,

Tian³

et al. 2016

IJN

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Background Akebia saponin D (ASD) exerts various pharmacological activities but with poor oral bioavailability. In this study, a self-nanoemulsifying drug delivery system (SNEDDS) based on the drug–phospholipid complex technique was developed to improve the oral absorption of ASD. Methods ASD–phospholipid complex (APC) was prepared using a solvent-evaporation method and characterized by infrared spectroscopy, differential scanning calorimetry, morphology observation, and solubility test. Oil and cosurfactant were selected according to their ability to dissolve APC, while surfactant was chosen based on its emulsification efficiency in SNEDDS. Pseudoternary phase diagrams were constructed to determine the optimized APC-SNEDDS formulation, which was characterized by droplet size determination, zeta potential determination, and morphology observation. Robustness to dilution and thermodynamic stability of optimized formulation were also evaluated. Subsequently, pharmacokinetic parameters and oral bioavailability of ASD, APC, and APC-SNEDDS were investigated in rats. Results The liposolubility significantly increased 11.4-fold after formation of APC, which was verified by the solubility test in n -octanol. Peceol (Glyceryl monooleate [type 40]), Cremophor ® EL (Polyoxyl 35 castor oil), and Transcutol HP (Diethylene glycol monoethyl ether) were selected as oil, surfactant, and cosurfactant, respectively. The optimal formulation was composed of Glyceryl monooleate (type 40), Polyoxyl 35 castor oil, Diethylene glycol monoethyl ether, and APC (1:4.5:4.5:1.74, w/w/w/w), which showed a particle size of 148.0±2.7 nm and a zeta potential of −13.7±0.92 mV after dilution with distilled water at a ratio of 1:100 (w/w) and good colloidal stability. Pharmacokinetic studies showed that APC-SNEDDS exhibited a significantly greater C max 1 (733.4±203.8 ng/mL) than ASD (437.2±174.2 ng/mL), and a greater C max 2 (985.8±366.6 ng/mL) than ASD (180.5±75.1 ng/mL) and APC (549.7±113.5 ng/mL). Compared with ASD, T max 1 and T max 2 were both remarkably shortened by APC-SNEDDS. The oral bioavailability in rats was enhanced significantly to 183.8% and 431.8% by APC and APC-SNEDDS, respectively. Conclusion These results indicated that APC-SNEDDS was a promising drug delivery system to enhance the oral bioavailability of ASD.

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“…Self-formulation of micelles of ginseng saponins such as ginsenosides has been reported to prevent permeation or absorption through the cell membrane of mucosal cells of the gastrointestinal tract. Incorporation of lipidophilic compounds into the micelle may enhance the bioavailability of ingredients of ginger and ginseng (Xiong et al, 2008). The saponin effect of ginseng on enhancement of the blood concentrations of salvianolic acids, a medication for treat- ment of myocardial ischemia in China, has also been reported .…”

Section: Discussionmentioning

confidence: 99%

Profiling of the Compounds Absorbed in Human Plasma and Urine after Oral Administration of a Traditional Japanese (Kampo) Medicine, Daikenchuto

Iwabu¹,

Watanabe²,

Hirakura³

et al. 2010

Drug Metab Dispos

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ABSTRACT:Daikenchuto (DKT), a pharmaceutical-grade traditional Japanese (Kampo) medicine, has been widely used for the treatment of various gastrointestinal disorders including postoperative ileus and has been integrated into the modern medical care system in Japan as a prescription drug. DKT is a multiherbal medicine consisting of Japanese pepper (zanthoxylum fruit), processed ginger, and ginseng with maltose as an additive. Despite substantial research on the pharmacological activities of DKT and its ingredients, the lack of studies on absorption, distribution, metabolism, and excretion of DKT has made it difficult to obtain a consistent picture of its mechanism of action. In the present study, we constructed an analysis procedure consisting of seven conditions of liquid chromatography and mass spectrometric analysis, which enabled the identification of 44 ingredients of DKT component herbs. We investigated the plasma and urine profiles of these ingredients 0.5 to 8 h after oral administration of 15.0 g of DKT in four healthy volunteers. The results indicated that 1) hydroxy-␣-sanshool and [6]-shogaol, the prominent peaks in plasma derived from Japanese pepper and ginger, respectively, were detected at 0.5 h and thereafter decreased throughout the sampling period; 2) ginsenoside Rb 1 , a prominent peak derived from ginseng, increased gradually during the sampling period; 3) glucuronide conjugates of hydroxy-sanshools, shogaols, and gingerols were detected in plasma and urine; and 4) no obvious differences between samples from the two male and the two female individuals were observed. These results provide a strong basis for future studies on pharmacokinetics and pharmacology of DKT.

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Self-micelle formation and the incorporation of lipid in the formulation affect the intestinal absorption of Panax notoginseng

Cited by 43 publications

References 22 publications

Obtaining annatto seed oil miniemulsions by ultrasonication using aqueous extract from Brazilian ginseng roots as a biosurfactant

Obtaining annatto seed oil miniemulsions by ultrasonication using aqueous extract from Brazilian ginseng roots as a biosurfactant

Preparation and evaluation of a self-nanoemulsifying drug delivery system loaded with Akebia saponin D–phospholipid complex

Profiling of the Compounds Absorbed in Human Plasma and Urine after Oral Administration of a Traditional Japanese (Kampo) Medicine, Daikenchuto

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Self-micelle formation and the incorporation of lipid in the formulation affect the intestinal absorption of Panax notoginseng

Cited by 43 publications

References 22 publications

Obtaining annatto seed oil miniemulsions by ultrasonication using aqueous extract from Brazilian ginseng roots as a biosurfactant

Obtaining annatto seed oil miniemulsions by ultrasonication using aqueous extract from Brazilian ginseng roots as a biosurfactant

Preparation and evaluation of a self-nanoemulsifying drug delivery system loaded with Akebia saponin D&ndash;phospholipid complex

Profiling of the Compounds Absorbed in Human Plasma and Urine after Oral Administration of a Traditional Japanese (Kampo) Medicine, Daikenchuto

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Preparation and evaluation of a self-nanoemulsifying drug delivery system loaded with Akebia saponin D–phospholipid complex