The effect of various liposome formulations on insulin penetration across Caco-2 cell monolayer

Değim, Zelihagül; Ünal, Nilay; Eşsiz, Dinç; Abbasoğlu, Ufuk

doi:10.1016/j.lfs.2004.05.027

Cited by 68 publications

(44 citation statements)

References 17 publications

(33 reference statements)

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“…However, the integrity of sodium glycocholate liposomes needs to be studied in vivo. The bile salts used could be either sodium glycocholate, sodium taurocholate, 20 or sodium deoxycholate. 40,41 These three bile salts were compared to highlight the effect of sodium glycocholate as an enzyme inhibitor.…”

Section: Figurementioning

confidence: 99%

Liposomes containing glycocholate as potential oral insulin delivery systems: preparation, in vitro characterization, and improved protection against enzymatic degradation

Niu

Lü²,

Hovgaard³

et al. 2011

IJN

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Background: Oral delivery of insulin is challenging and must overcome the barriers of gastric and enzymatic degradation as well as low permeation across the intestinal epithelium. The present study aimed to develop a liposomal delivery system containing glycocholate as an enzyme inhibitor and permeation enhancer for oral insulin delivery. Methods: Liposomes containing sodium glycocholate were prepared by a reversed-phase evaporation method followed by homogenization. The particle size and entrapment efficiency of recombinant human insulin (rhINS)-loaded sodium glycocholate liposomes can be easily adjusted by tuning the homogenization parameters, phospholipid:sodium glycocholate ratio, insulin:phospholipid ratio, water:ether volume ratio, interior water phase pH, and the hydration buffer pH. Results: The optimal formulation showed an insulin entrapment efficiency of 30% ± 2% and a particle size of 154 ± 18 nm. A conformational study by circular dichroism spectroscopy and a bioactivity study confirmed the preserved integrity of rhINS against preparative stress. Transmission electron micrographs revealed a nearly spherical and deformed structure with discernable lamella for sodium glycocholate liposomes. Sodium glycocholate liposomes showed better protection of insulin against enzymatic degradation by pepsin, trypsin, and α-chymotrypsin than liposomes containing the bile salt counterparts of sodium taurocholate and sodium deoxycholate. Conclusion: Sodium glycocholate liposomes showed promising in vitro characteristics and have the potential to be able to deliver insulin orally.

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Section: Figurementioning

confidence: 99%

Liposomes containing glycocholate as potential oral insulin delivery systems: preparation, in vitro characterization, and improved protection against enzymatic degradation

Niu

Lü²,

Hovgaard³

et al. 2011

IJN

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“…Bile salts, such as sodium glycocholate (Niu et al, 2011), sodium taurocholate (Degim et al, 2004) and sodium deoxycholate (Niu et al, 2012) were most widely used to modify insulin-loaded liposomes as a penetration enhancer. These might be attributed to the good deformability of liposomes containing bile salts (Hu et al, 2013).…”

Section: Paracellular Routementioning

confidence: 99%

“…About 51% blood glucose level reductions were achieved in severely diabetic rats (Kebede et al, 2013). This approach is (Su et al, 2012;Chuang et al, 2013) Bile salts Open the tight junctions and improve deformability and permeation (Degim et al, 2004;Niu et al, 2011Niu et al, , 2012Hu et al, 2013) Enteric coatings HPMCP, Eudragit Õ pH-sensitive Rapid release in intestinal Maroni et al, 2009;Wang & Zhang, 2012;Wu et al 2012a,b,c;Marais et al, 2013;Viehof et al, 2013;Zhao et al, 2013) …”

Section: Natural Polymersmentioning

confidence: 99%

“…The loading efficiency of insulin on hydrophobic carriers could be improved by the addition of distearyldimethylammonium bromide or soybean phospholipid Li et al, 2013). Other studies used enteric coatings (Zhao et al, 2013), enzyme inhibitors (Werle et al, 2007) and permeation enhancers (Degim et al, 2004;Zhang et al, 2011a,b) to enhance the absorption of insulin. But most of the recent literatures concentrate on the novel drug delivery systems made of biodegradable macromolecular materials, which could be used to carry insulin.…”

Section: Introductionmentioning

confidence: 99%

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A review of biodegradable polymeric systems for oral insulin delivery

Luo

Xiong

Tian³

et al. 2015

Drug Delivery

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Currently, repeated routine subcutaneous injections of insulin are the standard treatment for insulin-dependent diabetic patients. However, patients' poor compliance for injections often fails to achieve the stable concentration of blood glucose. As a protein drug, the oral bioavailability of insulin is low due to many physiological reasons. Several carriers, such as macromolecules and liposomes have been used to deliver drugs in vivo. In this review article, the gastrointestinal barriers of oral insulin administration are described. Strategies for increasing the bioavailability of oral insulin, such absorption enhancers, enzyme inhibitors, enteric coatings are also introduced. The potential absorption mechanisms of insulin-loaded nanoparticles across the intestinal epithelium, including intestinal lymphatic route, transcellular route and paracellular route are discussed in this review. Natural polymers, such as chitosan and its derivates, alginate derivatives, g-PGA-based materials and starch-based nanoparticles have been exploited for oral insulin delivery; synthetic polymers, such as PLGA, PLA, PCL and PEA have also been developed for oral administration of insulin. This review focuses on recent advances in using biodegradable natural and synthetic polymers for oral insulin delivery along with their future prospects.

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“…11,[19][20][21][22] It has been documented that the drug efficacy can be enhanced or degraded through nanoparticle, 23,24 micelles, 25 and liposomal formulations. 26 Nevertheless, relatively few studies have been carried out concerning the influence of the nanosuspension of a drug on its antitumor efficacy. 22,27 Thus, in the present study, we demonstrated that nanosuspension could influence the ORI efficacy on proliferation and apoptosis of PC-3 cells.…”

Section: Introductionmentioning

confidence: 99%

Effects of oridonin nanosuspension on cell proliferation and apoptosis of human prostatic carcinoma PC-3 cell line

Zhang

Zhang²,

Xue³

et al. 2010

IJN

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This study aims to investigate the inhibitory effects of oridonin nanosuspension on human prostatic carcinoma PC-3 cell line in vitro. The PC-3 cells were incubated with increasing concentrations of oridonin solution and nanosuspensions for 12 hours, 24 hours, and 36 hours. MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay was performed to measure cellular viability and investigate the effect of oridonin on cell growth of PC-3. Annexin V-FITC/PI staining method was used to determine the effect of oridonin by fluorescence microscope and flow cytometry, respectively. Nanosuspension on early apoptosis of PC-3 cells was also evaluated. Oridonin significantly inhibited the growth of PC-3 cells after 12 hours, 24 hours, and 36 hours of treatment in a dose-dependent manner (P , 0.05). Compared with the same concentration of oridonin solution, oridonin nanosuspension enhanced the inhibition ratio of proliferation. The observation of propidium iodide fluorescence staining confirmed the MTT assay results. The cell proportion of PC-3 at the G2/M phase in the nanosuspension treatment group was upregulated compared with that of the control and oridonin solution groups. Both oridonin solution and nanosuspension promoted the early apoptosis of PC-3 cells. Furthermore, while improving the ratio of early apoptosis, oridonin nanosuspensions also enhanced growth suppression, and induced apoptosis of PC-3 cells. This shows great potential in the treatment of androgen-independent carcinoma of prostate by oridonin nanosuspensions.

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The effect of various liposome formulations on insulin penetration across Caco-2 cell monolayer

Cited by 68 publications

References 17 publications

Liposomes containing glycocholate as potential oral insulin delivery systems: preparation, in vitro characterization, and improved protection against enzymatic degradation

Liposomes containing glycocholate as potential oral insulin delivery systems: preparation, in vitro characterization, and improved protection against enzymatic degradation

A review of biodegradable polymeric systems for oral insulin delivery

Effects of oridonin nanosuspension on cell proliferation and apoptosis of human prostatic carcinoma PC-3 cell line

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