scholarly journals New Insights on the Mechanism of Fatty Acids as Buccal Permeation Enhancers

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 201 ◽  
Author(s):  
Cristina Padula ◽  
Silvia Pescina ◽  
Sara Nicoli ◽  
Patrizia Santi

Buccal mucosa has recently received much attention as a potential route for systemic delivery of drugs, including biologics and vaccines. The aim of this work was to gain insight into the mechanism of fatty acids as buccal permeation enhancers, by studying the effect of a series of medium and long chain fatty acids on the permeation of a model high molecular weight and hydrophilic molecule, fluorescein isothiocyanate labelled dextran (FD-4, m.w. 4 kDa) across porcine esophageal epithelium. A parabolic relationship between fatty acid lipophilicity and enhancement was obtained, regardless of the presence and number of double bonds. The relationship, which resembles the well-known relationship between permeability and lipophilicity of transdermal delivery, presents a maximum value in correspondence of C10 (logP approx. 4). This is probably the ideal lipophilicity for the fatty acid to interact with the lipid domains of the mucosa. When the same analysis was performed on skin data, the same trend was observed, although the maximum value was reached for C12 (logP approx. 5), in agreement with the higher lipophilicity of the skin. The results obtained in the present work represent a significant advancement in the understanding of the mechanisms of action of fatty acids as buccal penetration enhancers.

1994 ◽  
Vol 77 (5) ◽  
pp. 2374-2379 ◽  
Author(s):  
J. Calles-Escandon ◽  
P. Driscoll

The impact of aerobic fitness level on the production and disposal of serum free fatty acids was investigated in 26 normal young volunteers. The fitness level was ascertained by history and confirmed by determination of maximal aerobic capacity. Energy expenditure and substrate oxidation at rest were measured with indirect calorimetry. Free fatty acid turnover was measured with an infusion of [14C]palmitic acid. All tests were done > or = 48 h after the last bout of exercise. The sedentary (SED) volunteers had higher rates of systemic delivery of fatty acids than aerobically fit (FIT) individuals (532 +/- 53.4 vs. 353 +/- 62.3 mumol/min; P = 0.05). This difference was accentuated when the values were normalized to fat-free mass (9.2 +/- 0.8 and 5.9 +/- 0.98 mumol.kg-1.min-1 for SED and FIT, respectively). Fatty acid oxidation was similar between FIT and SED volunteers in absolute numbers (209 +/- 25 vs. 202 +/- 21 mumol/min, respectively; NS) as well as when normalized to fat-free mass (3.8 +/- 0.9 vs. 3.6 +/- 1.4 mumol.kg-1.min-1, respectively; NS). In contrast, the nonoxidative disposal of serum fatty acids was higher in SED (330 +/- 46.1 mumol/min) than in FIT individuals (144 +/- 52 mumol/min; P = 0.026). Thus, the ratio of nonoxidative to oxidative disposal rates of fatty acids was higher in SED than in FIT individuals (1.65 +/- 0.29 vs. 0.75 +/- 0.17; P = 0.021). The data support the hypothesis that high aerobic fitness level is associated with a low rate of systemic delivery of fatty acids at rest. Nevertheless, subjects with high aerobic fitness levels have fat oxidation at the same rate as unfit individuals.


HortScience ◽  
2004 ◽  
Vol 39 (4) ◽  
pp. 858A-858
Author(s):  
Sameera Bafeel* ◽  
Frank Matta

Temperature is a major environmental factor governing the distribution of both wild and cultivated plant species. During acclimation and deacclimation plants undergo a series of metabolic changes that lead to cold hardiness or loss of hardiness. One of these changes is the accumulation of certain lipids. This research was conducted to compare hardiness among three pecan cultivars: `Desirable', `Jackson', and `Owens' growing under Mississippi condition and to determine the relationship between fatty acid levels and cold hardiness of pecan shoots. Differential thermal analysis (DTA), electrical conductivity, and tetrazolium tests were used to determine cold hardiness. Pecan stems were collected from September to March in 2002 and 2003 to determine cold acclimation and deacclimation. Fatty acid composition of pecan stems during this time period was determined by gas chromatography. DTA indicated that pecan stems acclimated in October and deacclimated in March. During cold acclimation, there was a shift in the fatty acid composition to more unsaturated fatty acids. The percentage of linoleic and linolenic fatty acids increased, while the percentage of palmitic and stearic fatty acids decreased. The correlation between unsaturated fatty acids and cold hardiness suggests that unsaturated fatty acid may play a role in membrane fluidity.


Author(s):  
Sang-Hee Lee ◽  
Yu-Jin Kim ◽  
Byeong Ho Kang ◽  
Choon-Keun Park

This study investigated the relationship of acrosome reactions and fatty acid composition on fertility in boar sperm. The acrosome reaction of sperm was induced via methyl-beta-cyclodextrin (MBCD), and acrosome reaction, plasma membrane integrity, and fertility were analyzed. The fatty acid composition of the excess acrosome reacted sperm was determined via gas chromatography. The results showed that the acrosome reaction in sperm was induced over 85% of the time by 60 mM MBCD treatment, and the plasma membrane integrity was significantly decreased and was dependent on the MBCD level. The acrosome reacted sperm resulted in significantly higher saturated fatty acids (SFAs) and lower unsaturated fatty acids (PUFAs) than the non-acrosome reaction group. Moreover, the acrosome reacted sperm from 60 mM MBCD significantly decreased in vitro fertility and blastocyst formation relative to non-acrosome reacted sperm, and the acrosome reaction was positively correlated with SFAs and negatively correlated with PUFAs. Of these fatty acids, C22:5n-6 (docosapentaenoic acid [DPA]) and C22:6n-3 (docosahexaenoic acid [DHA]) were directly negatively correlated with the acrosome reaction (r = -0.982 and -0.947, respectively). In conclusion, the excessive acrosome reactions may occur by reducing the PUFAs, which may then dramatically decrease sperm fertility in pigs.


1978 ◽  
Vol 174 (1) ◽  
pp. 119-130 ◽  
Author(s):  
S J Smith ◽  
E D Saggerson

1. Dose-dependent effects of adrenaline on PDHa activity were investigated with both incubated rat epidiymal fat-pads and isolated adipocytes. 2. Adrenaline (10nM- 5 micrometer) decreased PDHa activity in fat-pads incubated with 5 mM-[U-14C]glucose + insulin (20 munits/ml). Changes in [U-14C]glucose incorporation into fatty acids in these tissues correlated only loosely with changes in PDHa activity. There was a good inverse relationship between adrenaline-induced changes in PDHa activity and increases in lipolysis (glycerol release). 3. Adrenaline (10nM - 0.5 micrometer) decreased PDHa activity in fat-pads incubated with 5 mM-[U-14C]pyruvate + insulin (20 munits/ml), whereas 1 micrometer- and 5 micrometer-adrenaline slightly increased PDHa activity. All concentrations of adrenaline tested decreased [U-14C]pyruvate incorporation into fatty acids. Between 10nM- and 0.5 micrometer-adrenaline percentage decreases in PDHa activity paralleled decreases in faty acid synthesis. 4. Effects of adrenaline on PDHa activity and fatty acid synthesis in fat-pads incubated with 5mM-[U-14C]pyruvate + insulin (20 munits/ml) could not be mimicked by addition of albumin-bound palmitate. 5. The response of PDHa activity to adrenaline (0.1 nM - 1 micrometer) in isolated adipocytes differed with the carbohydrate substrate used in the incubations. With 5 mM-glucose + insulin (20 munits/ml), PDHa activity was significantly increased by 10 nM-adrenaline, but not by 1 micrometer-adrenaline, the response to adrenaline being biphasic. There was some correlation between PDHa activity and accumulation of non-esterified fatty acids. With 5 mM-glucose alone adrenaline (0.1 nM - 1 micrometer) had no effect on PDHa activity even though lipolysis was increased by adrenaline (0.1 micrometer - 1 micrometer). With 5mM-fructose in the presence and absence of insulin, lipolytic doses of adrenaline decreased PDHa activity. No tested concentrations of adrenaline increased PDHa with this substrate. 6. In the presence of 5 mM-fructose, palmitate was significantly more effective than adrenaline with respect to the maximum decrease in PDHa activity that could be elicited. 4. The relationship of changes in PDHa activity to changes in lipogenesis and the likelihood of adrenaline-induced changes in PDHa activity being secondary to changes in non-esterified fatty acid metabolism are discussed.


2020 ◽  
Vol 37 (4) ◽  
pp. 335-342
Author(s):  
Nurgül Sen Özdemir ◽  
Ali Muzaffer Feyzioglu ◽  
Fatma Caf

In this study, the relationship between the fatty acid composition, abundance of carnivore Sagitta setosa (S. setosa) and total copepod abundance (copepodites and nauplii) which are the main diets of S. setosa was investigated. Sampling was conducted monthly during a year. During the sampling period, S. setosa and the total the copepod abundance showed a parallel distribution until November. Average total lipid was at the highest with 3% in spring and autumn, while the lowest was 2% in winter and summer. While DHA/EPA ratio (2.23) as carnivory index in S. setosa and the total copepod (copepodites and nauplii) abundance (1375 ind/m3) were at the highest in winter, but another carnivory index, 18:1ω9/18:1ω7 ratio did not show a parallel increase with copepod abundance. However, 18:1ω9 which increases the carnivory index, is among the main fatty acids in S. setosa. This might be indicated that S. setosa does not related to predation on the copepods, but it shows that feeding in a carnivorous style. Additionally, the herbivory index ∑ n-3/∑ n-6 ratio was detected in spring and autumn at the highest level. Consequently, although there is no direct effect between the copepod abundance and S. setosa fatty acids, it is possible an indirect effect.


2017 ◽  
Vol 2 (6) ◽  
pp. 333 ◽  
Author(s):  
Abdelhay Benyaich

Poor dietary habits lead to the emergence of chronic diseases such as coronary heart disease, stroke, hypertension, diabetes mellitus, dyslipidemia, cancer, dementia, obesity and oxidative stress involved through the aggression of cells by free radicals, Knowing that these diseases cause a global burden both individually and economically, Several studies focus on the relationship between diet and chronic disease. Studies suggest that the Mediterranean diet, (MD) traditional eating habits and lifestyle specific to the Mediterranean region, reduce the incidence of chronic diseases and improve longevity. The MD is known to be one of the healthiest diets, this diet is based on herbs, spices, vegetables, fruits, olive oils, cereals (preferably whole grains), legumes and nuts, fish and shellfish, white meat, so the main source of dietary fat from MD is olive oil. Moderate consumption of eggs and dairy products, and reduced consumption of red meats, processed meats and foods rich in sugars and fats. MD has a beneficial fatty acid profile with a higher content of monounsaturated fatty acids (MSFA) and a higher MSFA / saturated fatty acid (SFA) ratio than non-Mediterranean diets. High consumption of dietary fiber. a low glycemic index, anti-inflammatory effects, and antioxidant compounds, can work together to produce favorable effects on health status. MD is rich in vitamins and minerals, such as: vitamin B (B1, B2, niacin, B6, folate and B12) and antioxidant vitamins (vitamins E and C), and polyphenol, flavonoids, phytosterols, n-fatty acids 3 (alpha linoleic acid), resveratrol, quercetin, oleic acid, carotenoids and lutein. The purpose of this review is to provide an update on the current state of science regarding the relationship between the traditional Mediterranean diet and lifestyle related chronic diseases, and discuss the mechanisms involved and opportunities. in this area of research, to clarify and increase the confidence of the role of nutrition in the etiology of chronic diseases.


2003 ◽  
Vol 2003 ◽  
pp. 23-23
Author(s):  
F. Noci ◽  
A. P. Moloney ◽  
P. French ◽  
F. J. Monahan

Current medical advice is to reduce consumption of saturated fat, in favour of polyunsaturated fat, and to increase the consumption of ω-3 polyunsaturated fatty acids (PUFAs) at the expense of ω-6 PUFAs. Fat of ruminant origin, although it has a nutritionally favourable ω-6: ω-3 ratio, is rich in saturated fatty acids (SFAs), which have been linked to incidence of coronary heart disease in humans. However, when compared to non-ruminant fat, fat of ruminant origin has a high concentration of conjugated linoleic acid (CLA), which is considered to have anticarcinogenic properties (Belury, 1995). Grass finishing of cattle increased the concentration of CLA and the PUFA:SFA ratio (P:S) when compared with concentrate-based finishing (French et al., 2000). The objective of this study was to investigate the relationship between duration of grass-finishing of cattle and the fatty acid profile of intramuscular lipid.


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