The Use of Lipid-Based Formulations to Increase the Oral Bioavailability of Panax Notoginseng Saponins Following a Single Oral Gavage to Rats

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

doi:10.1080/03639040701508292

Cited by 37 publications

(18 citation statements)

References 28 publications

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“…[24][25][26] Previous studies demonstrated that phospholipid complexes could improve the liposolubility and oral absorption of the hydrophilic drug. 10,12,27 Thus, APC was prepared, and the liposolubility significantly increased 11.4-fold after formation of APC, which was verified by the solubility test in n-octanol. Different from other studies, the hydrophilicity increased ~0.96-fold compared with ASD.…”

Section: Discussionmentioning

confidence: 99%

“…38 The exact mechanism(s) needs to be further studied. In addition, different hydrophilic drug-loaded phospholipid complexes had different lipid solubility, 10,27 so it was difficult to select appropriate absorption-enhancing oils which could dissolve a large amount of APC. In this study, Glyceryl monooleate (type 40) was found to have the largest dissolving capacity for APC among the oils tested.…”

Section: Discussionmentioning

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%

“…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%

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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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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

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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“…Some studies has been developed to overcome this problem, such as coadministration with adrenalin [38] or using lipid-based formulations [39, 40] and the suppression of p-glycoprotein efflux system [30] that are proven to increase the oral bioavailability of ginsenosides.…”

Section: Bioavailabilitymentioning

confidence: 99%

A Role of Ginseng and Its Constituents in the Treatment of Central Nervous System Disorders

Rokot

Kairupan

Cheng

et al. 2016

Evidence-Based Complementary and Alternative Medicine

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Ginseng, a perennial plant belonging to the Panax genus of the Araliaceae family, has been used in China, Korea, and Japan as a traditional herbal medicine for thousands of years. Ginseng is recorded to have exhibited a wide variety of beneficial pharmacological effects and has become a popular and worldwide known health supplement and drug. The protective effects of ginseng on central nervous system are discussed in this review. Ginseng species and ginsenosides and their intestinal metabolism and bioavailability are concisely introduced. The molecular mechanisms of the effects of ginseng on central nervous system, mainly focused on the neuroprotection properties of ginseng, memory, and learning enhanced properties, and the effects on neurodegenerative disorders are presented. Thus, ginseng and its constituents are of potential merits in the treatment of cerebral disorders.

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Differential metabolic profiles of ginsenosides in artificial gastric juice using ultra‐high‐pressure liquid chromatography coupled with linear ion trap‐Orbitrap mass spectrometry

Huang

Gong

Bai

et al. 2022

Biomedical Chromatography

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Ginsenosides have poor oral bioavailability and undergo rapid biological transformation in the complex gastrointestinal environment. Most studies on the metabolism of ginsenosides have focused on gut bacteria, yet gastric juice remains a nonnegligible factor. Metabolic profiles of ginsenoside monomers formed in artificial gastric juice were separately investigated and qualitatively identified using ultra-high-pressure liquid chromatography coupled with linear ion trap-Orbitrap mass spectrometry (UHPLC-LTQ-Orbitrap MS n ). A common pattern of their metabolic pathways was established, showing that ginsenosides were transformed via deglycosylation, hydration, and dehydration pathways. Two major structure types, 20(S), 20(R)protopanaxatriols and 20(S), 20(R)-protopanaxadiols, basically shared similar transformation pathways and yielded deglycosylated, hydrated, and dehydrated products.Fragmentation patterns of major ginsenosides were also discussed. Consequently, gastric juice, as the primary link in ginsenoside metabolism and as important as the intestinal flora, produces considerable amounts of degraded ginsenosides, providing a partial explanation for the low bioavailabilities of primary ginsenosides.

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The Use of Lipid-Based Formulations to Increase the Oral Bioavailability of Panax Notoginseng Saponins Following a Single Oral Gavage to Rats

Cited by 37 publications

References 28 publications

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

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

A Role of Ginseng and Its Constituents in the Treatment of Central Nervous System Disorders

Differential metabolic profiles of ginsenosides in artificial gastric juice using ultra‐high‐pressure liquid chromatography coupled with linear ion trap‐Orbitrap mass spectrometry

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The Use of Lipid-Based Formulations to Increase the Oral Bioavailability of Panax Notoginseng Saponins Following a Single Oral Gavage to Rats

Cited by 37 publications

References 28 publications

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

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

A Role of Ginseng and Its Constituents in the Treatment of Central Nervous System Disorders

Differential metabolic profiles of ginsenosides in artificial gastric juice using ultra‐high‐pressure liquid chromatography coupled with linear ion trap‐Orbitrap mass spectrometry

Contact Info

Product

Resources

About

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

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