Geniposide-Loaded Liposomes for Brain Targeting: Development, Evaluation, and In Vivo Studies

Wan, Jinyan; Long, Yu; Liu, Songyu; Zhang, Haoyang; Yan, Xiang; Li, Dan; Ai, Shi; Yu, Shuang; Liu, Ying; He, Yanan; Li, Nan; Guan, Yongmei

doi:10.1208/s12249-021-02093-9

Cited by 9 publications

(3 citation statements)

References 48 publications

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“…The EE and DL of the GMEs were 64.11 ± 0.58% and 3.21 ± 0.03%, respectively. The EE (%) of the GMEs was higher than that of the geniposide liposomes (44.87%) prepared with lecithin/cholesterol, but its DL (%) was lower than that of the geniposide liposomes (5.16%) [ 51 ]. Microemulsions developed by EO, Tween 80: CO-40, and ethanol can effectively embed genipin.…”

Section: Resultsmentioning

confidence: 99%

Microemulsion Delivery System Improves Cellular Uptake of Genipin and Its Protective Effect against Aβ1-42-Induced PC12 Cell Cytotoxicity

Zheng

et al. 2022

Pharmaceutics

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Genipin has attracted much attention for its hepatoprotective, anti-inflammatory, and neuroprotection activities. However, poor water solubility and active chemical properties limit its application in food and pharmaceutical industries. This article aimed to develop a lipid-based microemulsion delivery system to improve the stability and bioavailability of genipin. The excipients for a genipin microemulsion (GME) preparation were screened and a pseudo-ternary phase diagram was established. The droplet size (DS), zeta potential (ZP), polydispersity index (PDI), physical and simulated gastrointestinal digestion stability, and in vitro drug release properties were characterized. Finally, the effect of the microemulsion on its cellular uptake by Caco-2 cells and the protective effect on PC12 cells were investigated. The prepared GME had a transparent appearance with a DS of 16.17 ± 0.27 nm, ZP of −8.11 ± 0.77 mV, and PDI of 0.183 ± 0.013. It exhibited good temperature, pH, ionic strength, and simulated gastrointestinal digestion stability. The in vitro release and cellular uptake data showed that the GME had a lower release rate and better bioavailability compared with that of free genipin. Interestingly, the GME showed a significantly better protective effect against amyloid-β (Aβ1-42)-induced PC12 cell cytotoxicity than that of the unencapsulated genipin. These findings suggest that the lipid-based microemulsion delivery system could serve as a promising approach to improve the application of genipin.

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Section: Resultsmentioning

confidence: 99%

Microemulsion Delivery System Improves Cellular Uptake of Genipin and Its Protective Effect against Aβ1-42-Induced PC12 Cell Cytotoxicity

Zheng

et al. 2022

Pharmaceutics

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“…Subsequently, the in vivo experiments revealed three-fold longer availability and bio-distribution of GE-LP than the GE solution. Also, the middle cerebral artery occlusion (MCAO) rat model contemplated the neuroprotective effect of GE by preventing the injury of CIRI [ 98 ]. The liposomal formulations experimented with for AD and PD are discussed in the following sections and represented in Figure 3 .…”

Section: Liposomal Approaches To Brain Tumormentioning

confidence: 99%

Liposomes: An emerging carrier for targeting Alzheimer's and Parkinson's diseases

Pandian

Vijayakumar

Murugesan³

et al. 2022

Heliyon

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“…Meanwhile, after the peroral administration of geniposide, the results of tissue distribution studies in rats showed that the concentration of geniposide was the highest in the kidney and the lowest in the brain [ 92 ]. In order to improve the problem of poor brain targeting by geniposide, the preparation of geniposide into geniposide liposome could significantly prolong the half-life of geniposide, enhance brain targeting, and better improve cerebral ischemia reperfusion injury (CIRI) rat [ 93 ]. The analysis of the pharmacokinetics of geniposide in adjuvant-induced arthritis (AA) rats by intragastric administration showed that the Cmax value and the average AUC of geniposide in the plasma of the high-dose group (120 mg/kg group) were significantly higher than those of the middle-dose group (60 mg/kg group) and the low-dose group (30 mg/kg group); the dose-dependent PK parameter t 1/2 of each group was also significantly different.…”

Section: Pharmacokinetic Study Of Geniposidementioning

confidence: 99%

Updated Pharmacological Effects, Molecular Mechanisms, and Therapeutic Potential of Natural Product Geniposide

Liu

Chen

et al. 2022

Molecules

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At present, the potential of natural products in new drug development has attracted more and more scientists’ attention, and natural products have become an important source for the treatment of various diseases or important lead compounds. Geniposide, as a novel iridoid glycoside compound, is an active natural product isolated from the herb Gardenia jasminoides Ellis (GJ) for the first time; it is also the main active component of GJ. Recent studies have found that geniposide has multiple pharmacological effects and biological activities, including hepatoprotective activity, an anti-osteoporosis effect, an antitumor effect, an anti-diabetic effect, ananti-myocardial dysfunction effect, a neuroprotective effect, and other protective effects. In this study, the latest research progress of the natural product geniposide is systematically described, and the pharmacological effects, pharmacokinetics, and toxicity of geniposide are also summarized and discussed comprehensively. We also emphasize the major pathways modulated by geniposide, offering new insights into the pharmacological effects of geniposide as a promising drug candidate for multiple disorders.

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Geniposide-Loaded Liposomes for Brain Targeting: Development, Evaluation, and In Vivo Studies

Cited by 9 publications

References 48 publications

Microemulsion Delivery System Improves Cellular Uptake of Genipin and Its Protective Effect against Aβ1-42-Induced PC12 Cell Cytotoxicity

Microemulsion Delivery System Improves Cellular Uptake of Genipin and Its Protective Effect against Aβ1-42-Induced PC12 Cell Cytotoxicity

Liposomes: An emerging carrier for targeting Alzheimer's and Parkinson's diseases

Updated Pharmacological Effects, Molecular Mechanisms, and Therapeutic Potential of Natural Product Geniposide

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