Nanocrystallization of the Pharmaceutically Active Agent Genipin by an Emulsion Solvent Evaporation Method

Zu, Yuangang; Yu, Xinyang; Zhao, Xiuhua; Wang, Weiguo; Kun-Lun, Wang

doi:10.1155/2014/240950

Cited by 9 publications

(3 citation statements)

References 39 publications

(38 reference statements)

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“…Since the homogenization pressure exceeded 500 bar, the MPS became larger by degrees. Therefore, when the homogenization pressure was excessive, emulsion droplets would be damaged [31]. Finally, 500 bar was proved as the optimal homogenization pressure.…”

Section: Homogenization Pressure and Cyclesmentioning

confidence: 99%

Ursolic acid nanoparticles for oral delivery prepared by emulsion solvent evaporation method: characterization, in vitro evaluation of radical scavenging activity and bioavailability

Qiu

Zhao

et al. 2019

Artificial Cells, Nanomedicine, and Biotechnology

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2019) Ursolic acid nanoparticles for oral delivery prepared by emulsion solvent evaporation method: characterization, invitro evaluation of radical scavenging activity and bioavailability, Artificial Cells, Nanomedicine, and Biotechnology, 47:1, 609-620, ABSTRACTWith the purpose of improving the water solubility and oral bioavailability, ursolic acid nanoparticles (UANs) were prepared by the emulsion solvent evaporation method, and the nanosuspension was freeze-dried into powder. The optimal conditions for preparing nanoparticles were screened out using single-factor experiment. Take advantage of the optimal conditions, UA nanoemulsion had mean particle size (MPS) of 69.7 ± 15.6 nm and polydispersity index value (PI) of 0.005. The MPS of UA nanosuspension was gained at 100.2 ± 12.1 nm (PI ¼ 0.005), after the organic solvent was removed by rotary evaporator. Finally, UANs possessing an MPS of 157.5 ± 28.0 nm (PI ¼ 0.005) and zeta potential of 20.33 ± 1.67 mV were obtained after freeze-dried. UANs were investigated using SEM, XRD, DSC, TGA and further explored their equilibrium solubility, dissolution rate, solvent residue analysis, cellular antioxidant activity and oral bioavailability. All the results above showed that UA in UANs was in the amorphous state. The result of solubility test figured that the equilibrium solubility of UANs was 13.48 times in simulated gastric fluid (SGF), 11.79 times in simulated intestinal fluid (SIF) and 23.99 times in deionized water than raw UA. Accordingly, the dissolution rate of UANs in SGF and SIF had an apparent enhancement. The oral bioavailability of UANs increased 2.68 times than raw UA. UANs improved antioxidant activity toward cells compared with raw UA, and EC 50 of UANs reduced 37.5 times than raw UA. The residual contents of trichloromethane and ethanol were separated up to the mustard of the ICH limit for class III and class II solvents. The results above indicated that UANs possesses a value of application on enhancement oral bioavailability. ARTICLE HISTORY

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Section: Homogenization Pressure and Cyclesmentioning

confidence: 99%

Ursolic acid nanoparticles for oral delivery prepared by emulsion solvent evaporation method: characterization, in vitro evaluation of radical scavenging activity and bioavailability

Qiu

Zhao

et al. 2019

Artificial Cells, Nanomedicine, and Biotechnology

Self Cite

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“…Oral administration is the most common, ideal, and convenient route for many drugs or bioactive molecule administration [ 14 ]. To improve the bioavailability of genipin through oral administration, nanocrystals [ 15 ], cyclodextrin embedding [ 16 ], and hydrogel [ 17 ] were reported to improve its water solubility and intestinal absorption.…”

Section: Introductionmentioning

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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“…Theoretically, GP possesses the ability to react with the opulent oncoprotein, collagen, glycoprotein and proteoglycan in tumors, resulting in a dark-blue appearance of the tumor [ 35 , 41 , 42 ]. However, GP merely possesses 1% water solubility at room temperature (25 °C) [ 43 , 44 ], whose limited solubility hinders its application in vitro and in vivo. Although GP can be well dissolved in DMSO, the direct use of GP/DMSO solution is unbearable with great biosafety concerns as the definite carcinogenicity of DMSO.…”

Section: Introductionmentioning

confidence: 99%

In Situ Biosynthesis of Photothermal Parasite for Fluorescence Imaging-Guided Photothermal Therapy of Tumors

Wang

Pan

Meng

et al. 2022

Gels

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Photothermal therapy (PTT) has been widely known as a promising therapeutic strategy for cancer treatment in recent decades. However, some organic and inorganic photothermal agents exhibit shortcomings including potential long-term toxicity and lack of biodegradability. Biocompatible extracts from plants and animals provide several alternatives for the reformation of photothermal agents. Bio-inspired products still have inherent problems such as low accumulation in tumors, easy diffusion, and fast elimination. Herein, we aim to develop a biocompatible photothermal agent with tumor enrichment. Enlightened by “parasitized snails”, in situ biosynthesis of photothermal agents and fluorescence imaging-guided PTT are achieved with the assistance of alginate–calcium–genipin (ACG) hydrogel. ACG hydrogel is a mixture of alginate (ALG), calcium (Ca), and genipin (GP). Given that the crosslinking product of GP and protein displays fluorescent/photothermal features, the constructed ACG hydrogel can gradually react with the tumor and then “light up” and “ignite” the tumor under specific light excitation. The ACG hydrogel can be seen as a photothermal parasite, eventually leading to the death of tumor. The photothermal therapeutic effects of ACG hydrogel reacting with tumors are successfully proven in vivo. The naturally derived GP and ALG ensure the biosafety of the ACG hydrogel-based bio-application. This work is another successful practice of nature-inspired methodological strategy for in situ biosynthesis of the photothermal agent.

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Nanocrystallization of the Pharmaceutically Active Agent Genipin by an Emulsion Solvent Evaporation Method

Cited by 9 publications

References 39 publications

Ursolic acid nanoparticles for oral delivery prepared by emulsion solvent evaporation method: characterization, in vitro evaluation of radical scavenging activity and bioavailability

Ursolic acid nanoparticles for oral delivery prepared by emulsion solvent evaporation method: characterization, in vitro evaluation of radical scavenging activity and bioavailability

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

In Situ Biosynthesis of Photothermal Parasite for Fluorescence Imaging-Guided Photothermal Therapy of Tumors

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