Safety Assessment of Lactate Esters

Clary, John J.; Feron, V.J.; Velthuijsen, J. A. Van

doi:10.1006/rtph.1997.1175

Cited by 86 publications

(45 citation statements)

References 5 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The oral 50% lethal dose of n-butyl L-lactate is .5000 mg/ kg in rats, 21 so it is considered as a safe oil phase in this study. A pseudo-ternary phase diagram of oil (n-butyl L-lactate)/ surfactant (Tween 80)/cosurfactant (ethanol, 1-propanol, and PEG 600) with/without saturation of FFB in the oil phase was constructed to determine the SMEPMS region.…”

Section: Results and Discussion Construction Of Pseudo-ternary Phase mentioning

confidence: 99%

Development and characterization of dilutable self-microemulsifying premicroemulsion systems (SMEPMS) as templates for preparation of nanosized particulates

Lin¹,

Chen

Ho³

et al. 2013

IJN

View full text Add to dashboard Cite

Section: Results and Discussion Construction Of Pseudo-ternary Phase mentioning

confidence: 99%

Development and characterization of dilutable self-microemulsifying premicroemulsion systems (SMEPMS) as templates for preparation of nanosized particulates

Lin¹,

Chen

Ho³

et al. 2013

IJN

View full text Add to dashboard Cite

“…Chew 1979; Florin et al 1980;Yamaguchi 1982;Wild et al 1983;Andersen & Jensen 1984;Shimizu et al 1985;Al-Ani & Al-Lami 1988;Clary et al 1998;Zeiger & Margolin 2000). Based on the results of sub-acute toxicity/carcinogenicity and genotoxicity studies, we concluded that the metabolites of the four flavouring substances as well as substances structurally related to these flavouring substances do not pose a safety concern when used at low levels of intake or as flavouring substances.…”

Section: Genotoxicitymentioning

confidence: 95%

Japan Flavour and Fragrance Materials Association’s (JFFMA) safety assessment of food-flavouring substances uniquely used in Japan that belong to the class of aliphatic primary alcohols, aldehydes, carboxylic acids, acetals and esters containing additional oxygenated functional groups

Saito¹,

Hasegawa-Baba

Sekiya³

et al. 2017

Food Additives & Contaminants: Part A

View full text Add to dashboard Cite

We performed a safety evaluation using the procedure devised by the Joint FAO/WHO Expert Committee on Food Additives (JECFA) of the following four flavouring substances that belong to the class of 'aliphatic primary alcohols, aldehydes, carboxylic acids, acetals, and esters containing additional oxygenated functional groups' and are uniquely used in Japan: butyl butyrylacetate, ethyl 2-hydroxy-4-methylpentanoate, 3-hydroxyhexanoic acid and methyl hydroxyacetate. Although no genotoxicity study data were found in the published literature, none of the four substances had chemical structural alerts predicting genotoxicity. All four substances were categorised as class I by using Cramer's classification. The estimated daily intake of each of the four substances was determined to be 0.007-2.9 μg/person/day by using the maximised surveyderived intake method and based on the annual production data in Japan in 2001, 2005 and 2010, and was determined to be 0.250-600.0 μg/person/day by using the single-portion exposure technique and based on average-use levels in standard portion sizes of flavoured foods. Both of these estimated daily intake ranges were below the threshold of toxicological concern for class I substances, which is 1800 μg/person/day. Although no information from in vitro and in vivo toxicity studies for the four substances was available, these substances were judged to raise no safety concerns at the current levels of intake. ARTICLE HISTORY

show abstract

“…After careful removal of the hair on the abdominal area of the sacrificed rat using an electric clipper, the skin was cut and the adherent fat and other debris were carefully removed. Finally, the full-thickness skin was obtained and examined microscopically to ensure the integrity of the skin (20,26).…”

Section: In Vitro Skin Permeation Studiesmentioning

confidence: 99%

“…Moreover, a large number of studies have suggested that aliphatic esters displayed excellent enhancement activities for a wide variety of drugs (10)(11)(12)(13)(14)(15)(16)(17)(18)(19). Chukwumerije et al measured the in vitro enhancement effects of a series of methyl esters of n-alkyl fatty acids using various skin types and revealed that the medium chain n-alkyl fatty acid esters appeared to be better enhancers of a variety of drugs than Azone (20). In addition, Karande et al (21) investigated the enhancement ratio (ER) and irritation potential (IP) of about 300 chemical penetration enhancers in silico and in vitro and found the stearyl methacrylate yielded the highest ER/IP among the commercially available substance of structures which indicated stearyl methacrylate should be greatly safe and competent to enhance percutaneous penetration.…”

Section: Introductionmentioning

confidence: 99%

In vitro Enhancement of Lactate Esters on the Percutaneous Penetration of Drugs with Different Lipophilicity

et al. 2010

View full text Add to dashboard Cite

Abstract. Lactate esters are widely used as food additives, perfume materials, medicine additives, and personal care products. The objective of this work was to investigate the effect of a series of lactate esters as penetration enhancers on the in vitro skin permeation of four drugs with different physicochemical properties, including ibuprofen, salicylic acid, dexamethasone and 5-fluorouracil. The saturated donor solutions of the evaluated drugs in propylene glycol were used in order to keep a constant driving force with maximum thermodynamic activity. The permeability coefficient (K p ), skin concentration of drugs (SC), and lag time (T), as well as the enhancement ratios for K p and SC were recorded. All results indicated that lactate esters can exert a significant influence on the transdermal delivery of the model drugs and there is a structure-activity relationship between the tested lactate esters and their enhancement effects. The results also suggested that the lactate esters with the chain length of fatty alcohol moieties of 10-12 are more effective enhancers. Furthermore, the enhancement effect of lactate esters increases with a decrease of the drug lipophilicity, which suggests that they may be more efficient at enhancing the penetration of hydrophilic drugs than lipophilic drugs. The influence of the concentration of lactate esters was evaluated and the optimal concentration is in the range of 5∼10 wt.%. In sum, lactate esters as a penetration enhancer for some drugs are of interest for transdermal administration when the safety of penetration enhancers is a prime consideration.

show abstract

Safety Assessment of Lactate Esters

Cited by 86 publications

References 5 publications

Development and characterization of dilutable self-microemulsifying premicroemulsion systems (SMEPMS) as templates for preparation of nanosized particulates

Development and characterization of dilutable self-microemulsifying premicroemulsion systems (SMEPMS) as templates for preparation of nanosized particulates

Japan Flavour and Fragrance Materials Association’s (JFFMA) safety assessment of food-flavouring substances uniquely used in Japan that belong to the class of aliphatic primary alcohols, aldehydes, carboxylic acids, acetals and esters containing additional oxygenated functional groups

In vitro Enhancement of Lactate Esters on the Percutaneous Penetration of Drugs with Different Lipophilicity

Contact Info

Product

Resources

About