Assessment of the potential skin irritation of lysine-derivative anionic surfactants using mouse fibroblasts and human keratinocytes as an alternative to animal testing.

Abstract:

PURPOSE:The aim of this study was to identify new surfactants with low skin irritant properties for use in pharmaceutical and cosmetic formulations, employing cell culture as an alternative method to in vivo testing. In addition, we sought to establish whether potential cytotoxic properties were related to the size of the counterions bound to the surfactants. METHODS:Cytotoxicity was assessed in the mouse fibroblast cell line 3T6 and the human keratinocyte cell line NCTC 2544 using the MTT assay and uptake of the vital dye neutral red 24 h after dosing (NRU). RESULTS:Lysine-derivative surfactants showed higher IC50s than did commercial anionic irritant compounds such as sodium dodecyl sulfate, proving to be no more harmful than amphoteric betaines. The aggressiveness of the surfactants depended on the size of their constituent counterions: surfactants associated with lighter counterions showed a proportionally higher aggressivity than those with heavier ones. CONCLUSIONS:Synthetic lysine-derivative anionic surfactants are less irritant than commercial surfactants such as sodium dodecyl sulfate and hexadecyltrimethylammonium bromide and are similar to betaines. These surfactants may offer promising applications in pharmaceutical and cosmetic preparations, representing a potential alternative to commercial anionic surfactants as a result of their low irritancy potential.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Sanchez L,Mitjans M,Infante MR,Vinardell MP

doi

10.1023/b:pham.0000041459.63362.6f

subject

Has Abstract

pub_date

2004-09-01 00:00:00

pages

1637-41

issue

9

eissn

0724-8741

issn

1573-904X

journal_volume

21

pub_type

杂志文章
  • Liposomal co-delivery of omacetaxine mepesuccinate and doxorubicin for synergistic potentiation of antitumor activity.

    abstract:PURPOSE:Anticancer chemotherapy usually involves the administration of several anticancer drugs that differ in their action mechanisms. Here, we aimed to test whether the combination of omacetaxine mepesuccinate (OMT) and doxorubicin (DOX) could show synergism, and whether the liposomal co-delivery of these two drugs c...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1317-3

    authors: Shim G,Lee S,Choi J,Lee S,Kim CW,Oh YK

    更新日期:2014-08-01 00:00:00

  • Transepithelial transport of insulin: I. Insulin degradation by insulin-degrading enzyme in small intestinal epithelium.

    abstract:PURPOSE:The purpose of this study was to determine the existence of insulin-degrading enzyme (EC 3.4.22.11) (IDE) in rat intestinal enterocytes. METHODS:Subcellular fractionation, biochemical characterization, immunoprecipitation, and western blots were employed. RESULTS:Insulin-degrading activity was localized in th...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016263926946

    authors: Bai JP,Chang LL

    更新日期:1995-08-01 00:00:00

  • Effect of Relative Humidity on Bipolar Electrostatic Charge Profiles of dry Powder Aerosols.

    abstract:PURPOSE:This work investigated the effect of relative humidity (RH) on bipolar electrostatic charge profiles of dry powder inhaler aerosols using the Bipolar Charge Analyzer (BOLAR). METHODS:Two commercial products, Pulmicort® (400 μg, budesonide) and Bricanyl® (500 μg, terbutaline sulfate) Turbuhaler®, were used as m...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-017-2178-3

    authors: Yu J,Wong J,Ukkonen A,Kannosto J,Chan HK

    更新日期:2017-08-01 00:00:00

  • Crystalline form information from multiwell plate salt screening by use of Raman microscopy.

    abstract:PURPOSE:The purpose of this study was to establish a useful methodology, possibly providing information on the stoichiometry of pharmaceutical drug salts obtained from salt screening by using a multiwell plate and a Raman microscope. METHODS:Tamoxifen salt screening was conducted with monobasic and polybasic acids on ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-006-9644-7

    authors: Kojima T,Onoue S,Murase N,Katoh F,Mano T,Matsuda Y

    更新日期:2006-04-01 00:00:00

  • Crystal growth kinetics of theophylline monohydrate.

    abstract::The crystal growth kinetics of theophylline monohydrate from aqueous buffered supersaturated solutions were investigated at 10, 20, 30, and 40 degrees C. Crystallization experiments were carried out isothermally at pH 6. During growth the crystal count and size distributions were monitored in situ. The growth rate was...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015817109932

    authors: Rodríguez-Hornedo N,Wu HJ

    更新日期:1991-05-01 00:00:00

  • Influence of molecular size on the retention of polymeric nanocarrier diagnostic agents in breast ducts.

    abstract:PURPOSE:To investigate the influence of nanocarrier molecular size and shape on breast duct retention in normal rats using a non-invasive optical imaging method. METHODS:Fluorescein-labeled PEG nanocarriers of different molecular weights and shapes (linear, two-arm, four-arm, and eight-arm) were intraductally administ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0763-z

    authors: Singh Y,Gao D,Gu Z,Li S,Rivera KA,Stein S,Love S,Sinko PJ

    更新日期:2012-09-01 00:00:00

  • Development of a Virosomal RSV Vaccine Containing 3D-PHAD® Adjuvant: Formulation, Composition, and Long-Term Stability.

    abstract:PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2453-y

    authors: Lederhofer J,van Lent J,Bhoelan F,Karneva Z,de Haan A,Wilschut JC,Stegmann T

    更新日期:2018-07-03 00:00:00

  • Anti-melanoma effects of vorinostat in combination with polyphenolic antioxidant (-)-epigallocatechin-3-gallate (EGCG).

    abstract:PURPOSE:Melanoma is an aggressive neoplasm with a propensity for metastases and resistance to therapy. Previously, we showed that (-)-epigallocatechin-3-gallate (EGCG), the major polyphenolic antioxidant present in green tea, resulted in a significant decrease in the viability and growth of melanoma and induction of ap...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-010-0054-5

    authors: Nihal M,Roelke CT,Wood GS

    更新日期:2010-06-01 00:00:00

  • Oral absorption of peptides: the effect of absorption site and enzyme inhibition on the systemic availability of metkephamid.

    abstract::In this study the intestinal degradation and absorption of a synthetic pentapeptide, metkephamid, were investigated in the rat by determination of its wall permeabilities in the small and large intestine and the extent and mechanism of its intestinal degradation. The peptide was metabolized in the gut wall through con...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018962415287

    authors: Langguth P,Merkle HP,Amidon GL

    更新日期:1994-04-01 00:00:00

  • Enhanced Cellular Uptake and Gene Silencing Activity of Survivin-siRNA via Ultrasound-Mediated Nanobubbles in Lung Cancer Cells.

    abstract:PURPOSE:Paclitaxel is a first-line drug for the therapy of lung cancer, however, drug resistance is a serious limiting factor, related to overexpression of anti-apoptotic proteins like survivin. To overcome this phenomenon, developing novel ultrasound responsive nanobubbles - nanosized drug delivery system- for the del...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-020-02885-x

    authors: Akbaba H,Erel-Akbaba G,Kotmakçı M,Başpınar Y

    更新日期:2020-08-05 00:00:00

  • Cocrystal formation during cogrinding and storage is mediated by amorphous phase.

    abstract:PURPOSE:The purpose of this work was to investigate the mechanisms of cocrystal formation during cogrinding and storage of solid reactants, and to establish the effects of water by cogrinding with hydrated form of reactants and varying RH conditions during storage. METHODS:The hydrogen bonded 1:1 carbamazepine-sacchar...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-006-9110-6

    authors: Jayasankar A,Somwangthanaroj A,Shao ZJ,Rodríguez-Hornedo N

    更新日期:2006-10-01 00:00:00

  • pH-dependent bidirectional transport of weakly basic drugs across Caco-2 monolayers: implications for drug-drug interactions.

    abstract:PURPOSE:The purpose of this study was to investigate the pH-dependent passive and active transport of weakly basic drugs across the human intestinal epithelium. METHODS:The bidirectional pH-dependent transport of weak bases was studied in Caco-2 cell monolayers in the physiologic pH range of the gastrointestinal tract...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1025032511040

    authors: Neuhoff S,Ungell AL,Zamora I,Artursson P

    更新日期:2003-08-01 00:00:00

  • Fabrication of TPGS-Stabilized Liposome-PLGA Hybrid Nanoparticle Via a New Modified Nanoprecipitation Approach: In Vitro and In Vivo Evaluation.

    abstract:PURPOSE:In this study, a new modified nanoprecipitation approach that more efficient and simpler than conventional approach was developed to synthesize D-alpha-Tocopheryl polyethylene glycol 1000 succinate stabilized liposome-PLGA hybrid nanoparticle, loaded with simvastatin (ST-TLPN). METHODS:The optimum formulation ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2485-3

    authors: Zhang M,He J,Zhang W,Liu J

    更新日期:2018-08-30 00:00:00

  • Solubility of small-molecule crystals in polymers: D-mannitol in PVP, indomethacin in PVP/VA, and nifedipine in PVP/VA.

    abstract:OBJECTIVE:Amorphous pharmaceuticals, a viable approach to enhancing bioavailability, must be stable against crystallization. An amorphous drug can be stabilized by dispersing it in a polymer matrix. To implement this approach, it is desirable to know the drug's solubility in the chosen polymer, which defines the maxima...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-008-9784-z

    authors: Tao J,Sun Y,Zhang GG,Yu L

    更新日期:2009-04-01 00:00:00

  • Sugar-Grafted Cyclodextrin Nanocarrier as a "Trojan Horse" for Potentiating Antibiotic Activity.

    abstract:PURPOSE:The use of "Trojan Horse" nanocarriers for antibiotics to enhance the activity of antibiotics against susceptible and resistant bacteria is investigated. METHODS:Antibiotic carriers (CD-MAN and CD-GLU) are prepared from β-cyclodextrin grafted with sugar molecules (D-mannose and D-glucose, respectively) via azi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-016-1861-0

    authors: Li M,Neoh KG,Xu L,Yuan L,Leong DT,Kang ET,Chua KL,Hsu LY

    更新日期:2016-05-01 00:00:00

  • Transfer of dopamine in the olfactory pathway following nasal administration in mice.

    abstract:PURPOSE:The aim of the study was to investigate whether dopamine is transferred along the olfactory pathway to the brain following nasal administration to mice. METHODS:[3H]-Dopamine was administered nasally or intravenously to female mice. Brain tissue samples were excised and the radioactive content was measured. Th...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1007542618378

    authors: Dahlin M,Bergman U,Jansson B,Björk E,Brittebo E

    更新日期:2000-06-01 00:00:00

  • Iontophoresis enhances the transport of acyclovir through nude mouse skin by electrorepulsion and electroosmosis.

    abstract:PURPOSE:Iontophoresis was employed for enhancing the transdermal delivery of acyclovir through nude mouse skin in vitro, with the aim of understanding the mechanisms responsible for drug transport, in order to properly set the conditions of therapeutical application. METHODS:Experiments were done in horizontal diffusi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016284815501

    authors: Volpato NM,Santi P,Colombo P

    更新日期:1995-11-01 00:00:00

  • Probing beta relaxation in pharmaceutically relevant glasses by using DSC.

    abstract:PURPOSE:This study was conducted to demonstrate the use of differential scanning calorimetry (DSC) in detecting and measuring beta-relaxation processes in amorphous pharmaceutical systems. METHODS:DSC was employed to study amorphous samples of poly(vinylpyrrolidone) (PVP), indomethacin (IM), and ursodeoxycholic acid (...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-005-9044-4

    authors: Vyazovkin S,Dranca I

    更新日期:2006-02-01 00:00:00

  • The effect of octanoic acid on the binding of the enantiomers of ibuprofen and naproxen to human serum albumin: a chromatographic implication.

    abstract:PURPOSE:The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to th...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016066325476

    authors: Cheruvallath VK,Riley CM,Narayanan SR,Lindenbaum S,Perrin JH

    更新日期:1996-01-01 00:00:00

  • Scale of health: indices of safety and efficacy in the evolving environment of large biological datasets.

    abstract::The interdependent relationship between pharmacology and toxicology is fundamental to the concepts of efficacy and safety of both drugs and xenobiotics. The traditional concept of establishing efficacious and tolerated doses to define a 'therapeutic window' appears simplistic in the context of an exponentially increas...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-014-1415-2

    authors: Sayes CM,Staats H,Hickey AJ

    更新日期:2014-09-01 00:00:00

  • Effect of selective lipid extraction from different body regions on epidermal barrier function.

    abstract:PURPOSE:To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig. METHODS:Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yor...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1010944529387

    authors: Monteiro-Riviere NA,Inman AO,Mak V,Wertz P,Riviere JE

    更新日期:2001-07-01 00:00:00

  • In Silico Predictions of Human Skin Permeability using Nonlinear Quantitative Structure-Property Relationship Models.

    abstract:PURPOSE:Predicting human skin permeability of chemical compounds accurately and efficiently is useful for developing dermatological medicines and cosmetics. However, previous work have two problems; 1) quality of databases used, and 2) methods for prediction models. In this paper, we attempt to solve these two problems...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1629-y

    authors: Baba H,Takahara J,Mamitsuka H

    更新日期:2015-07-01 00:00:00

  • Solid-state stability testing of drugs by isothermal calorimetry.

    abstract::A new technique has been developed to calculate rapidly the solid-state room-temperature degradation rate of drugs and drug candidates. The technique utilizes measurements of the initial rate of heat output at several elevated temperatures by isothermal calorimetry and the degradation rate of the compound determined a...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015865319250

    authors: Koenigbauer MJ,Brooks SH,Rullo G,Couch RA

    更新日期:1992-07-01 00:00:00

  • Contribution of protein binding, lipid partitioning, and asymmetrical transport to drug transfer into milk in mouse versus human.

    abstract:PURPOSE:Drug transfer into milk is a general concern during lactation. Because data are limited in human subjects, particularly for new drugs, experimental animal models of lactational drug transfer are critical. This study analyzed drug transfer into milk in a mouse model, as well as the contribution of similar and di...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-013-1085-5

    authors: Ito N,Ito K,Koshimichi H,Hisaka A,Honma M,Igarashi T,Suzuki H

    更新日期:2013-09-01 00:00:00

  • Electrospun Zein/PCL Fibrous Matrices Release Tetracycline in a Controlled Manner, Killing Staphylococcus aureus Both in Biofilms and Ex Vivo on Pig Skin, and are Compatible with Human Skin Cells.

    abstract:PURPOSE:To investigate the destruction of clinically-relevant bacteria within biofilms via the sustained release of the antibiotic tetracycline from zein-based electrospun polymeric fibrous matrices and to demonstrate the compatibility of such wound dressing matrices with human skin cells. METHODS:Zein/PCL triple laye...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1782-3

    authors: Alhusein N,Blagbrough IS,Beeton ML,Bolhuis A,De Bank PA

    更新日期:2016-01-01 00:00:00

  • Pharmacokinetic Modeling of the Impact of P-glycoprotein on Ondansetron Disposition in the Central Nervous System.

    abstract:PURPOSE:Modulation of 5-HT3 receptor in the central nervous system (CNS) is a promising approach for treatment of neuropathic pain. The goal was to evaluate the role of P-glycoprotein (Pgp) in limiting exposure of different parts of the CNS to ondansetron (5-HT3 receptor antagonist) using wild-type and genetic knockout...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-020-02929-2

    authors: Chiang M,Back HM,Lee JB,Oh S,Guo T,Girgis S,Park C,Haroutounian S,Kagan L

    更新日期:2020-09-28 00:00:00

  • Synthesis of 8-(3-Carboxy-l-methyl-propylammo)-6-methoxyquinoline: A Newly Characterized Primaquine Metabolite.

    abstract::Primaquine (I), a 6-methoxy-8-aminoqumoline derivative used for the treatment of malaria has previously been shown to be metabolized to 8-(3-carboxy-l-methyl-propylamino)-6-methoxyquinoline by both micro-organisms and laboratory rats. Reported herein is the synthesis of this novel metabolite. ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/A:1016311616719

    authors: McChesney JD,Sarangan S

    更新日期:1984-03-01 00:00:00

  • Cutaneous metabolism of nitroglycerin in vitro. II. Effects of skin condition and penetration enhancement.

    abstract::The effects of skin storage, skin preparation, skin pretreatment with a penetration enhancer, and skin barrier removal by adhesive tape-stripping on the concurrent cutaneous transport and metabolism of nitroglycerin (GTN) have been studied in vitro using hairless mouse skin. Storing the skin for 10 days at 4 degrees C...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015822431178

    authors: Higo N,Hinz RS,Lau DT,Benet LZ,Guy RH

    更新日期:1992-03-01 00:00:00

  • Ability of different polymers to inhibit the crystallization of amorphous felodipine in the presence of moisture.

    abstract:PURPOSE:To investigate the ability of various polymers to inhibit the crystallization of amorphous felodipine from amorphous molecular dispersions in the presence of absorbed moisture. METHODS:Spin coated films of felodipine with poly(vinylpyrrolidone) (PVP), hydroxypropylmethylcellulose acetate succinate (HPMCAS) and...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-007-9331-3

    authors: Konno H,Taylor LS

    更新日期:2008-04-01 00:00:00

  • Compression behavior of orthorhombic paracetamol.

    abstract:PURPOSE:Orthorhombic crystals of paracetamol exhibit good technological properties during compression. The purpose of this study was to investigate the compression behavior of this substance and to compare it to that of monoclinic paracetamol. From the crystal structure, it could be hypothesized that sliding planes are...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011954800246

    authors: Joiris E,Di Martino P,Berneron C,Guyot-Hermann AM,Guyot JC

    更新日期:1998-07-01 00:00:00