Absorption-enhancing effect of glycyrrhizin induced in the presence of capric acid

Imai, Teruko; Sakai, Mitsuru; Ohtake, Hiroshi; Azuma, Hidekazu; Otagiri, Masaki

doi:10.1016/j.ijpharm.2004.12.029

Cited by 24 publications

(16 citation statements)

References 21 publications

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“…Glycyrrhizin showed a more potent absorption enhancing activity than caproic acid at the same concentration tested [58] . The absorption-enhancing activity obtained from the simultaneous treatment of sodium deoxycholate and dipotassium-glycyrrhizin was much greater than sodium deoxycholate alone in Caco-2 cell monolayers [59] .…”

Section: Glycyrrhizinmentioning

confidence: 78%

See 1 more Smart Citation

Bioavailability enhancers of herbal origin: An overview

Kesarwani

Gupta

2013

Asian Pacific Journal of Tropical Biomedicine

362

197

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Section: Glycyrrhizinmentioning

confidence: 78%

“…The absorption-enhancing activity obtained from the simultaneous treatment of sodium deoxycholate and dipotassium-glycyrrhizin was much greater than sodium deoxycholate alone in Caco-2 cell monolayers [59] . The absorption enhancing activity of glycyrrhizin was increased by presence of the other absorption enhancers [58] .…”

Section: Glycyrrhizinmentioning

confidence: 98%

Bioavailability enhancers of herbal origin: An overview

Kesarwani

Gupta

2013

Asian Pacific Journal of Tropical Biomedicine

362

197

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“…C 10 also mobilized intracellular Ca 2+ from stores in Caco-2 cells (Fig. 2c) [144,151,154], while pretreatment with the intracellular Ca 2+ chelator, BAPTA-AM, attenuated C10's permeationenhancing activity [97,143,145] and its effects on F-actin reorganization [145].…”

Section: [12] Intestinal Absorption Promotersmentioning

confidence: 99%

Safety and efficacy of sodium caprate in promoting oral drug absorption: from in vitro to the clinic

Maher

Leonard²,

Jacobsen

et al. 2009

Advanced Drug Delivery Reviews

191

176

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A major challenge in oral drug delivery is the development of novel dosage forms to promote absorption of poorly permeable Class III drugs across the intestinal epithelium.To date, no absorption promoter has been approved in a formulation specifically designed for oral delivery of Class III molecules. Promoters that are designated safe for human consumption have been licensed for use in a recently approved buccal insulin spray delivery system and also for many years as part of an ampicillin rectal suppository.Unlike buccal and rectal delivery, oral formulations containing absorption promoters have the additional technical hurdle whereby the promoter and payload must be coreleased in high concentrations at the small intestinal epithelium in order to generate significant but rapidly reversible increases in permeability. The most advanced promoter in the clinic is the medium chain fatty acid (MCFA), sodium caprate (C 10 ) , a compound already approved as a direct food additive. We discuss how it has evolved to a matrix tablet format suitable for administration to humans under the headings of mechanism of action at the cellular and tissue level and in vitro and in vivo efficacy and safety studies.In specific clinical examples, we review how C 10 -based formulations are being tested for oral delivery of bisphosphonates using Gastro Intestinal Permeation Enhancement Technology, GIPET® (Merrion Pharmaceuticals, Ireland) and in a related solid dose format for anti-sense oligonucleotides (ISIS Pharmaceuticals, USA).Keywords: Oral drug delivery, Sodium caprate (C 10 ), absorption promoter, drug delivery platforms, clinical trials, oral formulation, drug delivery systems.3 TJs form a barrier to the uncontrolled absorption of noxious luminal antigens (gate function), and maintain epithelial polarity (fence function) [8,9]. In general, the TJ consists of a restrictive pathway (shunt) with a sharp molecular size cut off, and a second unrestrictive pathway (small pore) that permits paracellular permeation of molecules of radii <4.0 Å [10,11]. Depending on the intestinal region, TJ pore sizes range from 6-22Å, sufficient to permit mannitol (6.7 Å) and EDTA (10.8 Å) to permeate to an extent, whereas the passage of inulin (30-40 Å) and fluorescent-dextran 4kDa (FD-4, 26 Å) is essentially impeded [12][13][14][15][16].A number of approaches have been used to promote oral delivery of Class III drugs ( Alternatively, the use of nanoparticles comprising biocompatible polymers (e.g. chitosan,polylactide-co-glycolide, starch and glucans) can protect cargoes from GI proteases, increase GI retention and promote absorption across gut associated lymphoid tissue (GALT) and to a lesser extent, enterocytes [45][46][47]. Most data on nanoparticle absorption from rodent models suggest that M cells in the follicle-associated epithelium of Peyer's patches (PP) are the favored site of uptake for particles of diameter 500nm-1000nm [45].Given the paucity of M cells in the GI tract of adults, the relevance of PP uptake remains controversial ...

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“…In this study, we first demonstrated that MAG had a specific stimulatory effect on junB gene expression in HepG2 cells. We then examined a possible mechanism of MAG action using inhibitors for signal transduction cascades (58).…”

Section: Discussionmentioning

confidence: 99%

“…Studies with five inhibitors of different signaling cascades revealed no influence on the MAG-induced activation of junB mRNA expression. From these observations, MAG activation of endogenous junB gene expression is predicted to be dependent on other signaling pathways than signaling cascades, such as MAP kinase, JAK/STAT and PKC cascades (56)(57)(58).…”

Section: Discussionmentioning

confidence: 99%

Expression of junB is markedly stimulated by glycyrrhizin in a human hepatoma cell line

Koike

2011

Oncol Rep

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Absorption-enhancing effect of glycyrrhizin induced in the presence of capric acid

Cited by 24 publications

References 21 publications

Bioavailability enhancers of herbal origin: An overview

Bioavailability enhancers of herbal origin: An overview

Safety and efficacy of sodium caprate in promoting oral drug absorption: from in vitro to the clinic

Expression of junB is markedly stimulated by glycyrrhizin in a human hepatoma cell line

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