Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes

Kong, Ruiping; Zhu, Xingyi; Meteleva, Elizaveta S.; Chistyachenko, Yulia S.; Suntsova, Lyubov P.; Polyakov, Nikolay E.; Хвостов, Михаил В.; Baev, Dmitry S.; Толстикова, Т. Г.; Yu, Jianming; Душкин, А. В.; Su, Weike

doi:10.1016/j.ijpharm.2017.10.011

Cited by 75 publications

(36 citation statements)

References 53 publications

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“…These results show that GA and salbutamol demonstrate synergistic anti-asthmatic effects. Complexes of GA with atorvastatin and simvastatin also demonstrated their higher effectiveness in comparison with pure drugs (Kong et al, 2017;Stakhneva et al, 2013). The amount of 3-hydroxy-3-methyl-glutaryl-CoA reductase protein in rats decreased by 13 and 25% after 24 h of treatment with GA complex with atorvastatin and simvastatin, respectively.…”

Section: Complex Formation With Drugsmentioning

confidence: 94%

“…Various physicochemical methods have been applied to get the evidence of complexes formation between GA self-associates and drug molecules in solid state as well as in aqueous and non-aqueous solutions. Such complexes were investigated by Fourier-transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction and scanning electron microscopy techniques (Lekar et al, 2011a;Yang et al, 2015;Zu et al, 2013;Kong et al, 2017). The physicochemical properties and behavior of GA complexes in solution were characterized by NMR, mass spectroscopy, electrochemical and optical techniques (Baltina, 2003;Apanasenko et al, 2015;Konkina et al, 2015;Polyakov et al, 2005).…”

Section: Complex Formation With Drugsmentioning

confidence: 99%

“…Complexes of simvastatin with Na 2 GA also shows enhanced solubility and bioavailability (Kong et al, 2017). Simvastatin is an inhibitor of 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase and is widely used to control hyper-cholesterolemia and prevent cardiovascular diseases.…”

Section: Self-association Of Ga and Its Use In Drug Deliverymentioning

confidence: 99%

“…It provides broad prospects of applying of glycyrrhizic acid as a multifunctional DDS. It was also established that GA enhance absorption effects of the variety of drugs (Kong et al, 2017;Sapra et al, 2008;Radwant and Aboul-Enein, 2002;Chen et al, 2009;Chakotiya et al, 2016). In view of the fact that the movement of small drug molecules through gastrointestinal epithelium is regulated by the distension and constriction of the tight junctions, observed effects could be connected with the ability of glycyrrhizin to enhance the penetration of molecules into the cells.…”

Section: Permeability Enhancement and Membrane-modifying Activitymentioning

confidence: 99%

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Glycyrrhizic acid as a multifunctional drug carrier – From physicochemical properties to biomedical applications: A modern insight on the ancient drug

Selyutina

Polyakov

2019

International Journal of Pharmaceutics

150

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A B S T R A C TGlycyrrhizic acid is the main active component of Licorice root which has been known in traditional Chinese and Japanese medicine since ancient times. In these cultures glycyrrhizic acid (GA) is one of the most frequently used drugs. However, only in 21-st century a novel unusual property of the GA to enhance the activity of other drugs has been discovered. The review describes briefly the experimental evidences of wide spectrum of own biological activities of glycyrrhizic acid as well as discusses the possible mechanisms of the ability of GA to enhance the activity of other drugs. We have shown that due to its amphiphilic nature GA is able to form self-associates in aqueous and non-aqueous media, as well as water soluble complexes with a wide range of lipophilic drugs. The main purpose of our review is to focus reader's attention on physicochemical studies of the molecular mechanisms of GA activity as a drug delivery system (DDS). In our opinion, the most intriguing feature of glycyrrhizic acid which might be the key factor in its therapeutic activity is the ability of GA to incorporate into the lipid bilayer and to increase the membrane fluidity and permeability. The ability of biomolecules and their aggregates to change the properties of cell membranes is of great significance, from both fundamental and practical points of view. monstrated the ability of GA to interact with cell membrane and to https://doi.

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Section: Complex Formation With Drugsmentioning

confidence: 94%

Section: Complex Formation With Drugsmentioning

confidence: 99%

Section: Self-association Of Ga and Its Use In Drug Deliverymentioning

confidence: 99%

Section: Permeability Enhancement and Membrane-modifying Activitymentioning

confidence: 99%

See 2 more Smart Citations

Glycyrrhizic acid as a multifunctional drug carrier – From physicochemical properties to biomedical applications: A modern insight on the ancient drug

Selyutina

Polyakov

2019

International Journal of Pharmaceutics

150

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“…Simvastatin (Zocor) is one of the most pharmaceutically important cholesterol‐lowering drugs with annual sales exceeding $3 billion. It is industrially manufactured from lovastatin through a multistep chemical route, which is composed of three modules: fermentation production of lovastatin in Aspergillus terreus , alkaline hydrolysis of lovastatin to monacolin J, and chemical transformation of monacolin J to simvastatin (Figure ).…”

Section: Introductionmentioning

confidence: 99%

Enhanced Single-Step Bioproduction of the Simvastatin Precursor Monacolin J in an Industrial Strain ofAspergillus terreusby Employing the Evolved Lovastatin Hydrolase

et al. 2018

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Biosynthesis of simvastatin, the active pharmaceutical ingredient of cholesterol-lowering drug Zocor, has drawn increasing global attention in recent years. Although single-step in vivo production of monacolin J, the intermediate biosynthetic precursor of simvastatin, has been realized by utilizing lovastatin hydrolase (PcEST) in our previous study, about 5% of residual lovastatin is still a problem for industrial production and quality control. In order to improve conversion efficiency and reduce lovastatin residues, modification of PcEST is carried out through directed evolution and a novel two-step high-throughput screening method. The mutant Q140L shows 18-fold improved whole-cell activity as compared to the wild-type, and one fold enhanced catalytic efficiency and 3 °C increased T over the wild-type are observed by characterizing the purified protein. Finally, the engineered A. terreus strain overexpressing Q140L mutant exhibited the increased conversion efficiency and the reduced lovastatin residues by comparing with A. terreus strain overexpressing the wild-type PcEST, where almost 100% of the produced lovastatin is hydrolyzed to monacolin J. Therefore, this improved microbial cell factory can realize single-step bioproduction of monacolin J in a more efficient way, providing an attractive and eco-friendly substitute over the existing chemical synthetic routes of monacolin J and promoting complete bioproduction of simvastatin at industrial scale.

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Preparation, characterization and evaluation of cefixime ternary inclusion complexes formated by mechanochemical strategy

Kong,

Xu,

Zhu

et al. 2023

J Incl Phenom Macrocycl Chem

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Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes

Cited by 75 publications

References 53 publications

Glycyrrhizic acid as a multifunctional drug carrier – From physicochemical properties to biomedical applications: A modern insight on the ancient drug

Glycyrrhizic acid as a multifunctional drug carrier – From physicochemical properties to biomedical applications: A modern insight on the ancient drug

Enhanced Single-Step Bioproduction of the Simvastatin Precursor Monacolin J in an Industrial Strain ofAspergillus terreusby Employing the Evolved Lovastatin Hydrolase

Preparation, characterization and evaluation of cefixime ternary inclusion complexes formated by mechanochemical strategy

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