Role of phosphatidylcholine saturation in preventing bile salt toxicity to gastrointestinal epithelia and membranes

Dial, Elizabeth J.; Rooijakkers, Suzan H.M.; Darling, Rebecca; Romero, Jimmy J.; Lichtenberger, Lenard M.

doi:10.1111/j.1440-1746.2007.05153.x

Cited by 36 publications

(29 citation statements)

References 27 publications

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“…From the plot, it can be concluded that the cell growth inhibition between CUR inside mixed micelles and free CUR had no significant differences at the concentration range from 0.75 to 3 mg/ml and 12 to 24 mg/ml; however, great changes occurred from 3 to 12 mg/ml. Empty micelles, just containing PC and bile salt, also represented a certain cell toxicity probably owing to the toxicity of SDC to epithelia and membranes, which could be counteracted partly by PCs (Dial et al, 2008). The IC 50 values on MCF-7 cells of CUR-PC-SDC-MMs and free drug solution were 4.10 mg/ml and 6.93 mg/ml, respectively.…”

Section: Cell Toxicity Assaysmentioning

confidence: 87%

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

et al. 2014

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Although curcumin (CUR) can inhibit proliferation and induce apoptosis of tumors, the poor water solubility restricted its clinical application. The aim of this study was to improve the aqueous solubility of CUR and make more favorable changes to bioactivity by preparing curcumin-loaded phospholipid-sodium deoxycholate-mixed micelles (CUR-PC-SDC-MMs). CUR-PC-SDC-MMs were prepared by the thin-film dispersion method. Based on the results of single factor exploration, the preparation technology was optimized using the central composite design-response surface methodology with drug loading and entrapment efficiency (EE%) as indicators. The images of transmission electron microscopy showed that the optimized CUR-PC-SDC-MMs were spherical and well dispersed. The average size of the mixed micelles was 66.5 nm, the zeta potential was about À26.96 mV and critical micelle concentration was 0.0087 g/l. CUR was encapsulated in PC-SDC-MMs with loading capacity of 13.12%, EE% of 87.58%, and the solubility of CUR in water was 3.14 mg/ml. The release results in vitro showed that the mixed micelles presented sustained release behavior compared to the propylene glycol solution of CUR. The IC 50 values of CUR-loaded micelles and free drug in human breast carcinoma cell lines were 4.10 mg/ml and 6.93 mg/ml, respectively. It could be concluded from the above results that the CUR-PC-SDC-MMs system might serve as a promising nanocarrier to improve the solubility and bioactivity of CUR.

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Section: Cell Toxicity Assaysmentioning

confidence: 87%

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

et al. 2014

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“…Bile salts are a class of surfactants that cause irritation and toxicity to the cell membrane. 25 Although some reports have shown that phospholipids can attenuate the toxicity of bile salts, 26,27 the toxicity of liposomes containing bile salts has not been evaluated in detail for ophthalmic drug delivery systems. Liposomes containing sodium deoxycholate showed greater toxicity in SDHCECs than the other liposomes.…”

Section: Cytotoxicitymentioning

confidence: 99%

Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation

Dai¹,

Zhou²,

Liu³

et al. 2013

IJN

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Abstract:The objective of this study was to investigate the potential of liposomes containing bile salts as an ophthalmic delivery system for tacrolimus to improve corneal permeability. Liposomes containing bile salts, including sodium taurocholate, sodium deoxycholate, and sodium glycocholate, were produced by the thin-film dispersion method with a particle size of approximately 100 nm and an entrapment efficiency of more than 90%. Less than 5% tacrolimus was released from conventional liposomes and from liposomes containing sodium taurocholate, sodium deoxycholate, or sodium glycocholate over 12 hours. The cellular uptake of conventional liposomes was significantly higher than that of liposomes containing bile salts. However, liposomes containing bile salts exerted a 3-4-fold increase of tacrolimus in ex vivo corneal transport of tacrolimus compared with conventional liposomes. When rabbit eyes were treated with a DiI perchlorate-loaded liposome suspension, liposomes containing bile salts showed fast and sustained penetration across the cornea. Unfortunately, liposomes containing sodium deoxycholate caused toxicity or irritation to both spontaneously derived human corneal epithelial cells and the rabbit cornea. Therefore, liposomes containing sodium taurocholate and sodium glycocholate are potential carriers in ocular drug delivery systems, given their low toxicity and vastly improved permeability.

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“…However, some researches have shown that PL can reduce the noxiousness of bile salts (Dial et al, 2008). In this domain, Niu et al (2014) evaluated the cytotoxicity of BS-liposomes in concentration range of 0.25-6.25 mmol/L using cell growth inhibition assay employing Caco-2 cell monolayers.…”

Section: Cytotoxicity Of Bs-vesiclesmentioning

confidence: 99%

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Aburahma¹

2014

Drug Delivery

103

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Most of the new drugs, biological therapeutics (proteins/peptides) and vaccines have poor performance after oral administration due to poor solubility or degradation in the gastrointestinal tract (GIT). Though, vesicular carriers exemplified by liposomes or niosomes can protect the entrapped agent to a certain extent from degradation. Nevertheless, the harsh GIT environment exemplified by low pH, presence of bile salts and enzymes limits their capabilities by destabilizing them. In response to that, more resistant bile salts-containing vesicles (BS-vesicles) were developed by inclusion of bile salts into lipid bilayers constructs. The effectiveness of orally administrated BS-vesicles in improving the performance of vesicles has been demonstrated in researches. Yet, these attempts did not gain considerable attention. This is the first review that provides a comprehensive overview of utilizing BS-vesicles as a promising pharmaceutical carrier with a special focus on their successful applications in oral delivery of therapeutic macromolecules and vaccines. Insights on the possible mechanisms by which BSvesicles improve the oral bioavailability of the encapsulated drug or immunological response of entrapped vaccine are explained. In addition, methods adopted to prepare and characterize BSvesicles are described. Finally, the gap in the scientific researches tackling BS-vesicles that needs to be addressed is highlighted.

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Role of phosphatidylcholine saturation in preventing bile salt toxicity to gastrointestinal epithelia and membranes

Cited by 36 publications

References 27 publications

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

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