Erythrocyte hemolysis and shape changes induced by new lysine-derivate surfactants

Vives, M.; Infante, M. R.; García, Elena Gómez; Selve, C.; Maugras, M.; Vinardell, M. Pilar

doi:10.1016/s0009-2797(98)00111-2

Cited by 55 publications

(24 citation statements)

References 14 publications

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“…It has a molecular weight of 421.5 g/mol, a critical micellar concentration (CMC) of 3 x 10 3 µg/ml and its chemical structure is formed by two alkyl chains, each one with eight carbon atoms (Sánchez et al 2006(Sánchez et al , 2007. This surfactant was synthesized as previously described (Vives et al 1999). …”

Section: Surfactant Included In the Nanoparticlesmentioning

confidence: 99%

Inclusion of a pH-responsive amino acid-based amphiphile in methotrexate-loaded chitosan nanoparticles as a delivery strategy in cancer therapy

et al. 2015

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The encapsulation of antitumor drugs in nanosized systems with pH-sensitive behavior is a promissing approach that may enhance the success of chemotherapy in many cancers. The nanocarrier dependence on pH might trigger an efficient delivery of the encapsulated drug both in the acidic extracellular environment of tumors and, especially, in the intracellular compartments through disruption of endosomal membrane. In this context, here we reported the preparation of chitosan-based nanoparticles encapsulating methotrexate as a model drug (MTX-CS-NPs), which comprises the incorporation of an amino acid-based amphiphile with pHresponsive properties (77KS) on the ionotropic complexation process. The presence of 77KS clearly gives a pH-sensitive behavior to NPs, which allowed accelerated release of MTX with decreasing pH as well as pH-dependent membrane-lytic activity. This latter performance demonstrates the potential of these NPs to facilitate cytosolic delivery of endocytosed materials.Outstandingly, the cytotoxicity of MTX-loaded CS-NPs was higher than free drug to MCF-7 tumor cells and, to a lesser extent, to HeLa cells. Based on the overall results, MTX-CS-NPs modified with the pH-senstive surfactant 77KS could be potentially useful as a carrier system for intracellular drug delivery and, thus, a promising targeting anticancer chemotherapeutic agent.

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Section: Surfactant Included In the Nanoparticlesmentioning

confidence: 99%

Inclusion of a pH-responsive amino acid-based amphiphile in methotrexate-loaded chitosan nanoparticles as a delivery strategy in cancer therapy

et al. 2015

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“…1). These surfactants were synthesized in our laboratory as previously described [25,29]. The commercial anionic surfactant sodium dodecyl sulfate (SDS) was used as reference compound.…”

Section: Surfactants Testedmentioning

confidence: 99%

The role of counterions in the membrane-disruptive properties of pH-sensitive lysine-based surfactants

et al. 2011

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Surfactants are among the most versatile and widely used excipients in pharmaceuticals.This versatility, together with their pH-responsive membrane-disruptive activity and low toxicity, could also enable their potential application in drug delivery systems. Here we studied five anionic lysine-based surfactants that differ in the nature of their counterion.We examined their capacity to disrupt the cell membrane under a range of pH values, concentrations and incubation times using a standard hemolysis assay as a model for endosomal membranes. The surfactants showed pH-sensitive hemolytic activity and improved kinetics at the endosomal pH range. Low concentrations resulted in negligible hemolysis at physiological pH and high membrane lytic activity at pH 5.4, which is in the range characteristic of late endosomes. With increasing concentration, the surfactants showed an enhanced capacity to lyse cell membranes, and also caused significant membrane disruption at physiological pH. This observation indicates that at high concentrations surfactant behavior is independent of pH. We addressed the mechanism of surfactant-mediated membrane destabilization, and also performed scanning electron microscopy studies to evaluate the effects of the compounds on erythrocyte morphology as a function of pH. The in vitro cytotoxicity of the surfactants was assessed by MTT and NRU assays with the 3T3 cell line. The influence of different types of counterion on hemolytic activity and the potential applications of these surfactants in drug delivery are discussed. The possibility of using pH-sensitive surfactants for endosome disruption could hold great promise for intracellular drug delivery systems in future therapeutic applications.

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“…1). These surfactants were synthesized in our laboratory as previously described (Sánchez et al, 2006a;Vives et al, 1999).…”

Section: Chemicals and Reagentsmentioning

confidence: 99%

Comparative sensitivity of tumor and non-tumor cell lines as a reliable approach for in vitro cytotoxicity screening of lysine-based surfactants with potential pharmaceutical applications

Nogueira

Mitjans

Infante

et al. 2011

International Journal of Pharmaceutics

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Surfactants are used as additives in topical pharmaceuticals and drug delivery systems.The biocompatibility of amino acid-based surfactants makes them highly suitable for use in these fields, but tests are needed to evaluate their potential toxicity. Here we addressed the sensitivity of tumor (HeLa, MCF-7) and non-tumor (3T3, 3T6, HaCaT, NCTC 2544) cell lines to the toxic effects of lysine-based surfactants by means of two in vitro endpoints (MTT and NRU). This comparative assay may serve as a new approach for predictive toxicity screening of chemicals prior to pharmaceutical applications. After 24-h of cell exposure to surfactants, differing toxic responses were observed. NCTC 2544 and 3T6 cell lines were the most sensitive, while both tumor cells and 3T3 fibroblasts were more resistant to the cytotoxic effects of surfactants. IC 50 -values revealed that cytotoxicity was detected earlier by MTT assay than by NRU assay, regardless of the compound or cell line. The overall results showed that surfactants with organic counterions were less cytotoxic than those with inorganic counterions. Our findings highlight the relevance of the correct choice and combination of cell lines and bioassays in toxicity studies for a safe and reliable screen of chemicals with potential interest in pharmaceutical industry.

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Erythrocyte hemolysis and shape changes induced by new lysine-derivate surfactants

Cited by 55 publications

References 14 publications

Inclusion of a pH-responsive amino acid-based amphiphile in methotrexate-loaded chitosan nanoparticles as a delivery strategy in cancer therapy

Inclusion of a pH-responsive amino acid-based amphiphile in methotrexate-loaded chitosan nanoparticles as a delivery strategy in cancer therapy

The role of counterions in the membrane-disruptive properties of pH-sensitive lysine-based surfactants

Comparative sensitivity of tumor and non-tumor cell lines as a reliable approach for in vitro cytotoxicity screening of lysine-based surfactants with potential pharmaceutical applications

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