Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers

Rege, Bhagwant D.; Kao, Joseph P. Y.; Polli, James E.

doi:10.1016/s0928-0987(02)00055-6

Cited by 454 publications

(280 citation statements)

References 35 publications

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“…These excipients primarily act as P-gp inhibitors by rendering P-gp substrate site competition (Roger et al, 2010;Hoosain et al, 2015). In this context, Tween 80, being a surfactant also seemed to play significant role in inhibiting P-gp, leading to membrane fluidization and consequently, enhanced permeability (Rege et al, 2002).…”

Section: P-gp Efflux Assaymentioning

confidence: 99%

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

Khurana

Bansal

Beg

et al. 2017

International Journal of Pharmaceutics

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Mangiferin (Mgf), largely expressed out from the leaves and stem bark of Mango, is a potent antioxidant. However, its in vivo activity gets tremendously reduced owing to poor aqueous solubility and inconsistent gastrointestinal absorption, high hepatic first-pass metabolism and high P-gp efflux. The current research work, therefore, was undertaken to overcome the biopharmaceutical hiccups by developing the Mgfphospholipid complex (PLCs) loaded in nanostructured lipidic carriers (NLCs). The PLCs and NLCs were prepared using refluxing, solvent evaporation and hot emulsification technique, respectively with various molar ratios of Mgf and Phospholipon 90 G, i.e., 1:1; 1:2; and 1:3. The complex was evaluated for various physicochemical parameters like drug content (96.57%), aqueous solubility (25-fold improved) and oil-water partition coefficient (10-fold enhanced). Diverse studies on the prepared complex using FTIR, DSC, PXRD and SEM studies ratified the formation of PLCs at 1:1 ratio. The PLCs were further incorporated onto NLCs, which were systematically optimized employing a face centered cubic design (FCCD), while evaluating for particle size, zeta potential, encapsulation efficiency and in vitro drug release as the CQAs. Caco-2 cell line indicated insignificant cytotoxicity, and P-gp efflux, bi-directional permeability model and in situ perfusion studies specified enhanced intestinal permeation parameters. In vivo pharmacokinetic studies revealed notable increase in the values of Cmax (4.7-fold) and AUC (2.1-fold), respectively, from PLCs-loaded NLCs vis-à-vis Mgf solution. In a nutshell, the promising results observed from the present research work signified boosted biopharmaceutical potential of the optimized PLCs-loaded NLCs for potentially augmenting the therapeutic efficacy of Mgf.

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Section: P-gp Efflux Assaymentioning

confidence: 99%

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

Khurana

Bansal

Beg

et al. 2017

International Journal of Pharmaceutics

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“…Surfactants can enhance skin permeation by increasing membrane fluidity, drug solubilization, and extraction of lipid from the SC. 17 However, as the level of surfactant increases, the thermodynamic activity of the ME drug cargo may decrease, leading to decreased drug transport. 18 In addition, permeation profiles are affected by droplet size and viscosity, whereby low viscosity and small size tend to increase skin permeation.…”

Section: In Vitro Skin Permeationmentioning

confidence: 99%

Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis

Shen

Zhang

Wang

et al. 2014

IJN

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The aims of the present study were to investigate the skin permeation and cellular uptake of a microemulsion (ME) containing total flavone of rhizoma arisaematis (TFRA), and to evaluate its effects on skin structure. Pseudo-ternary phase diagrams were constructed to evaluate ME regions with various surfactants and cosurfactants. Eight formulations of oil-in-water MEs were selected as vehicles, and in vitro skin-permeation experiments were performed to optimize the ME formulation and to evaluate its permeability, in comparison to that of an aqueous suspension. Laser scanning confocal microscopy and fluorescent-activated cell sorting were used to explore the cellular uptake of rhodamine 110-labeled ME in human epidermal keratinocytes (HaCaT) and human embryonic skin fibroblasts (CCC-ESF-1). The structure of stratum corneum treated with ME was observed using a scanning electron microscope. Furthermore, skin irritation was tested to evaluate the safety of ME. ME formulated with 4% ethyl oleate (weight/weight), 18% Cremophor EL ® (weight/weight), and 18% Transcutol ® P, with 1% Azone to enhance permeation, showed good skin permeability. ME-associated transdermal fluxes of schaftoside and isoschaftoside, two major effective constituents of TFRA, were 3.72-fold and 5.92-fold higher, respectively, than those achieved using aqueous suspensions. In contrast, in vitro studies revealed that uptake by HaCaT and CCC-ESF-1 cells was lower with ME than with an aqueous suspension. Stratum corneum loosening and shedding was observed in nude mouse skin treated with ME, although ME produced no observable skin irritation in rabbits. These findings indicated that ME enhanced transdermal TFRA delivery effectively and showed good biocompatibility with skin tissue.

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“…The material used in the positive control group was a non-ionic surfactant (Tween), a toxic agent to biological membranes (Rege et al, 2002), This non-ionic surfactant consists of polyethylene sorbitol fatty acid esters, which is characterised for stimulating protein secretion in microorganisms (Stutzenberger, 1992), for altering both morphology and surface wall of the cells (Domingues et al, 2000). As expected, the positive control group showed high toxicity, being statistically different compared to the other groups (p<0.05).…”

Section: Discussionmentioning

confidence: 81%

Cytotoxicity of Dental Alginates

Pithon

Santos

Martins

et al. 2010

Int. J. Odontostomat.

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Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers

Cited by 454 publications

References 35 publications

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis

Cytotoxicity of Dental Alginates

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