Evaluation of Cell Tolerability of a Series of Lipoamino Acids Using Biological Membranes and a Biomembrane Model.

Pignatello, Rosario; Noce, Concettina; Campisi, A.; Acquaviva, Rosaria; Bucolo, Claudio; Puglisi, Giovanni; Tóth, István

doi:10.2174/156720107780362348

Cited by 10 publications

(7 citation statements)

References 39 publications

(44 reference statements)

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“…The AUC and C max of low molecular weight heparin were improved following co-administration of polylysine-(LAA 10 ) 2 per oral [63]. Of note, the enantiomeric diversity of LAAs should be considered in LAA lipidation [30,69,70,143].…”

Section: Lipoamino Acids (Laas)mentioning

confidence: 99%

Converting Peptides into Drug Leads by Lipidation

Zhang¹,

Bułaj²

2012

CMC

172

139

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Ulceration in the gastrointestinal (GI) mucosa is a common disorder in humans. It has been shown that cigarette smoking is closely related to the increase of peptic ulcer and also plays an inhibitory role on ulcer healing. However, the underlying mechanisms by which cigarette smoke exerts these adverse effects remain largely unknown. It is perhaps partly due to the complexity of chemical compositions in the smoke and furthermore their pathological actions are largely undefined. In this review, we have highlighted the potential adverse effects of the toxic chemical components in cigarette smoke and summarized their possible mechanisms of actions on ulcer formation and healing in the GI tract. We also discuss in detail how cigarette smoke disturbs cell proliferation, influences mucus synthesis and secretion, delays blood vessel formation, and interferes the innate immune responses during ulceration and repair in the GI mucosa.

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Section: Lipoamino Acids (Laas)mentioning

confidence: 99%

Converting Peptides into Drug Leads by Lipidation

Zhang¹,

Bułaj²

2012

CMC

172

139

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“…[ 18 ] evaluated the effects of nanoformulated bovine lactoferrin or SurR9-C84A proteins on normal or insulted ex vivo bovine cornea models observing eye-irritating properties on neither model. Generally, the eye irritation potential of ocular drug carriers appears to increase with increasing lipophilicity as was assessed using a set of different non-nanosized lipoamino acids in saline solution [ 19 ].…”

Section: Introductionmentioning

confidence: 99%

Eye irritation testing of nanomaterials using the EpiOcular™ eye irritation test and the bovine corneal opacity and permeability assay

Kolle

Sauer²,

Moreno

et al. 2015

Part Fibre Toxicol

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BackgroundAssessment of eye irritation hazard has long been a core requirement in any chemical legislation. Nevertheless, publications focussing on the eye damaging potential of nanomaterials are scarce. Traditionally, eye irritation testing was performed using rabbits. The OECD Test Guideline 437 Bovine Corneal Opacity and Permeability (BCOP) test method allows determining severely irritating substances without animals, and the recently adopted OECD Test Guideline 492 Reconstructed human cornea-like epithelium test method allows identifying chemicals that neither induce eye irritation nor serious eye damage. For substances applicable to these tests, huge progress has been made in replacing animal testing.MethodsThe in vitro eye irritation potential of 20 nanosized and 3 non-nanosized materials was investigated in a 2-tier EpiOcular™ Eye Irritation Test (EpiOcular™-EIT) and BCOP testing strategy including histopathology of the bovine corneas. Furthermore, applicability of the testing strategy for nanomaterials was assessed. Test materials encompassed OECD representative nanomaterials (metals (Ag), metal oxides (ZnO, TiO2, CeO2), amorphous SiO2 and MWCNTs), three organic pigments, quartz, and talc.ResultsNone of the dry-powder nanomaterials elicited eye irritation in either the EpiOcular™-EIT or the BCOP assay. Likewise, an amorphous SiO2 nanomaterial that was supplied as suspension was tested negative in both assays. By contrast, in the EpiOcular™-EIT, the silver nanomaterial that was supplied as dispersion was tested positive, whereas its surfactant-containing dispersant was borderline to negative. In the BCOP assay, the silver nanomaterial elicited highly variable results and dark-brown patches remained on the corneal surface, whereas the results for its dispersant alone were borderline to positive, which was assessed as inconclusive due to high inter-assay variability.ConclusionThe present study points to the low eye irritation potential of a spectrum of nanomaterials, which is consistent with available in vivo data for the same test materials or for nanosized or bulk materials of the same composition.Electronic supplementary materialThe online version of this article (doi:10.1186/s12989-016-0128-6) contains supplementary material, which is available to authorized users.

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“…They possess some structural features of lipids as well as of peptides; in this manner, they maintain a polar character but possess also a certain degree of lipophilicity [10]. LAA conjugation to different drugs has shown to impart to the drug more membrane affinity, allowing to enhance the interaction with cell membranes and/or crossing biological barriers [11,12]. We conjugated NAP with different LAAs through the spacer ethylenediamine (EDA) and used differential scanning calorimetry (DSC), Langmuir-Blodgett (LB) technique, and biomembrane models represented by multilamellar vesicles (MLV) and monolayers made of 1,2-dimyristoylsn-glycero-3-phosphocholine (DMPC) to investigate whether the LAA moiety can affect the interaction of the drug with the biomembranes.…”

Section: Introductionmentioning

confidence: 99%