Amounts Of Phosphatidylcholine Research Articles

Berberine HCl and diacerein loaded dual delivery transferosomes: Formulation and optimization using Box-Behnken design

Introduction: Berberine is a poorly water-soluble alkaloid compound showing significant anti-inflammatory characteristics. It reduces the levels of pro-inflammatory and inflammatory cytokines, including tumour necrosis factor (TNF-????, IFN-????) and interleukin (IL-23, IL-12, and IL-23). Diacerein significantly reduces the splenomegaly associated with psoriasis. It downregulates the production of TNF-α and IL-12. Method: This study reported the development of transferosomes containing berberine HCl and diacerein using a film hydration method followed by optimization using a Box-Behnken design. Sodium deoxycholate was used as an edge activator. The impact of independent variables (amount of phosphatidylcholine, amount of edge activator, and sonication cycles) on dependent variables (particle size and entrapment efficiency) was examined. The optimized formulation was characterized for polydispersity index, vesicle size, entrapment efficiency, ζ potential, spectral analysis like Fourier transform infrared, thermal analysis, X-ray diffraction, deformability, transmission electron microscopy, antioxidant assay, in-vitro release, and ex-vivo skin permeation studies. Results: The optimized formulation had a particle size of 110.90±2.8 nm with high entrapment efficiency (89.50±1.5 of berberine HCl and 91.23±1.8 of diacerein). Deformability, polydispersity index, ζ potential, and antioxidant activity of the optimized formulation were 2.44, 0.296, -13.3, and 38.36 %, respectively. Optimized transferosomes exhibited 82.093±0.81 % and 85.02±3.81 % release of berberine HCl and diacerein after 24 h of dissolution study. The transdermal flux of optimized formulation was 0.0224 µg cm-2 h-1 (2.24 cm h-1 permeation coefficient) and 0.0462 µg cm-2 h-1 (4.62 cm h-1 permeation coefficient), respectively, for berberine HCl and diacerein. Raman analysis of treated pig skin confirmed that the transferosomes can permeate the skin. No change in the skin condition or irritation was observed in BALB/c mice. Formulation stored at 4 and 25±2 °C / 60±5 % relative humidity was stable for 3 months. Conclusions: Thus, the results demonstrated successful optimization of the transferosomes for the efficient topical delivery of berberine HCl and diacerein in the effective management of psoriasis.

Normal HDL Cholesterol Efflux and Anti-Inflammatory Capacities in Type 2 Diabetes Despite Lipidomic Abnormalities.

ObjectiveTo assess whether, in type 2 diabetes (T2D) patients, lipidomic abnormalities in high-density lipoprotein (HDL) are associated with impaired cholesterol efflux capacity and anti-inflammatory effect, 2 pro-atherogenic abnormalities.Design and MethodsThis is a secondary analysis of the Lira-NAFLD study, including 20 T2D patients at T0 and 25 control subjects. Using liquid chromatography/tandem mass spectrometry, we quantified 110 species of the main HDL phospholipids and sphingolipids. Cholesterol efflux capacity was measured on THP-1 macrophages. The anti-inflammatory effect of HDL was measured as their ability to inhibit the tumor necrosis factor α (TNFα)-induced expression of vascular cell adhesion molecule-1 (VCAM-1) and intercellular cell adhesion molecule-1 (ICAM-1) on human vascular endothelial cells (HUVECs).ResultsThe cholesterol-to-triglyceride ratio was decreased in HDL from T2D patients compared with controls (-46%, P = 0.00008). As expressed relative to apolipoprotein AI, the amounts of phosphatidylcholines, sphingomyelins, and sphingosine-1-phosphate were similar in HDL from T2D patients and controls. Phosphatidylethanolamine-based plasmalogens and ceramides (Cer) were, respectively, 27% (P = 0.038) and 24% (P = 0.053) lower in HDL from T2D patients than in HDL from controls, whereas phosphatidylethanolamines were 41% higher (P = 0.026). Cholesterol efflux capacity of apoB-depleted plasma was similar in T2D patients and controls (36.2 ± 4.3 vs 35.5 ± 2.8%, P = 0.59). The ability of HDL to inhibit the TNFα-induced expression of both VCAM-1 and ICAM-1 at the surface of HUVECs was similar in T2D patients and controls (-70.6 ± 16.5 vs -63.5 ± 18.7%, P = 0.14; and -62.1 ± 13.2 vs -54.7 ± 17.7%, P = 0.16, respectively).ConclusionDespite lipidomic abnormalities, the cholesterol efflux and anti-inflammatory capacities of HDL are preserved in T2D patients.

Перспективы разработки хлебобулочных изделий, обогащённых липидными фракциями морских водорослей

The paper presents the results of studying the lipid composition of bakery products (HBI) with the addition of new ingredients to its formulation - water-ethanol extracts, four types of seaweed: green algae – Ulva lactuca; two types of brown algae – Sargassum pallidum and Japanese saccharin; red algae – Anfeltia tobuchinskaya, containing the main lipids – neutral lipids and glycolipids. The data obtained showed a change in the lipid composition of the developed bread. A statistically significant increase in all fractions of neutral lipids was registered in the developed CBI, a decrease in the amount of cholesterol and its cholesterol esters, compared with those in control samples. An increase in the amount of phosphatidylcholine (lecithin) in bread with the addition of kelp and anfeltia extracts was noted; a significant increase in phosphatidylethanolamine in bread with the introduction of all algal extracts. The revealed facts demonstrate the stability of lipid fractions in the composition of CBI with the addition of algae extracts and are positive in terms of giving them preventive properties. Particularly indicative is the appearance of the phosphatidylglycerol fraction in bread, which is the basis for the synthesis of other phospholipid compounds from it, which are essential substances that enter the human body exclusively through food, reducing the risks and consequences of adverse environmental factors affecting the body.

Fatty Acids and Sterols in Avena Sativa L. in Yakutia Permafrost

The authors of this study examined the seasonal changes in qualitative and quantitative contents of fatty acids, total lipids, phospholipids, and sterols of the common oat (Avena sativa L.) that were sown at different times. They grow in Yakutia permafrost and undergo inter-season cold hardening. During the first phase of cold hardening (fall period), the total lipid content in oat biomass grows considerably. Moreover, the content of phospholipids and polyunsaturated fatty acids increased, compared them to other summer fodder plants. In fall, the amount of phosphatidylcholine in oats increased 3.9 times compared to summer. Alpha-linolenic polyunsaturated acid was predominant in summer and fall (14.8 mg/g and 28.4 mg/g in dry mass, respectively). The inter-season (summer-fall) dominance of polyunsaturated fatty acids at low above-zero temperatures allows keeping the membrane fluidity at a necessary level. The total sterol content in A. sativa biomass was 0.8%. The authors concluded that fall vegetation is the primary source of pre-winter fattening of the Far North herbivorous animals.

UV-SPECTROMETRY AND THE LIPID COMPOSITION OF THE WATER-PROPYLENEGLYCOL EXTRACTS FROM SEVERAL HERBS

The physico-chemical properties by means of UV-spectroscopy and the lipid composition of extracts from Salvia officinalis L. leaves, the Calendula officinalis L and Matricaria chamomilla L. flowers; Hippophoe rhamnoides L fruits were studied. It is shown that extracts characterized the low shares of phospholipids and a trace content of sterols in the total lipid composition. Extracts studied are in the following sequence in accordance with decreasing the phospholipid share in the total lipid composition: Salvia officinalis L. leaves > Calendula officinalis L flowers = Hippophoe rhamnoides L fruits > Matricaria chamomilla L. flowers. It is shown that the quantitative ratio of phospholipid fractions is determined by the nature of the plant. Thus, the highest relative content of the phospholipid lysoforms in extracts was found in Calendula officinalis L flowers and Hippophoe rhamnoides L fruits, the highest share of sphingolipids was revealed in phospholipids of Calendula officinalis L and Matricaria chamomilla L flower extracts, and the phospholipids of Hippophoe rhamnoides L fruit extracts contained the highest amount of phosphatidylcholine. The high content of the more easily oxidizable fractions in the phospholipid composition especially for Salvia officinalis L. leaves are revealed. Using UV-spectrometry of extracts and mathematical analysis of these data the presence of flavonoids with different chemical structure is confirmed.

Impact of ApoE Polymorphism and Physical Activity on Plasma Antioxidant Capability and Erythrocyte Membranes.

The allele epsilon 4 (ε4) of apolipoprotein E (ApoE) is the strongest genetic risk factor for Alzheimer’s disease (AD). ApoE protein plays a pivotal role in the synthesis and metabolism of amyloid beta (Aβ), the major component of the extracellular plaques that constitute AD pathological hallmarks. Regular exercise is an important preventive/therapeutic tool in aging and AD. Nevertheless, the impact of physical exercise on the well-being of erythrocytes, a good model of oxidative stress and neurodegenerative processes, remains to be investigated, particularly depending on ApoE polymorphism. Herein, we evaluate the oxidative status, Aβ levels, and the membrane’s composition of erythrocytes in a cohort of human subjects. In our hands, the plasma antioxidant capability (AOC), erythrocytes membrane fluidity, and the amount of phosphatidylcholine (PC) were demonstrated to be significantly decreased in the ApoE ε4 genotype and non-active subjects. In contrast, erythrocyte Aβ content and lipid peroxidation increased in ε4 carriers. Regular physical exercise was associated with an increased plasma AOC and membrane fluidity, as well as to a reduced amount of erythrocytes Aβ. Altogether, these data highlight the influence of the ApoE genotype on erythrocytes’ well-being and confirm the positive impact of regular physical exercise.

Lipid Profile Changes During the Development of Artemia franciscana, From Cysts to the First Two Naupliar Stages.

The brine shrimp Artemia is an interesting experimental system for studies of developmental processes. Hatching of dormant cysts gives rise to shrimp larvae called nauplii, characterized by numerous naupliar stages representing the first forms of brine shrimp life cycle. Here combined Thin Layer Chromatography (TLC) and Matrix-Assisted Laser Desorption Ionization-Time-of-Flight/Mass Spectrometry (MALDI-TOF/MS) analyses have been performed to gain information on the lipid profiles of cysts and two naupliar stages. Lipid bands isolated after preparative TLC of the lipid extracts have been analyzed to detect various species of each lipid class; in addition Post-Source Decay (PSD) analyses allowed the identification of phospholipid chains. We compared the relative abundance of various polar and neutral lipid species in the lipid extracts, proving for the first time that during the development of nauplii there is an increase of cardiolipin (CL) and lysophospholipid levels; in parallel, the amount of phosphatidylcholine (PC) decreases. In addition, as regards neutral lipids, we found an increase of diacylglycerols (DAGs) in correspondence of the decrease of triacylglycerols (TAGs). Data reflect the fact that naupliar stages, being an active form of life, are more metabolically active and offer a platform to develop further studies on the importance of lipid metabolic pathways and bioactive lipids during the development.

Abstract 552: Enhancement of Rat Lymphatic Lipid Transport by Glucose or Amino Acids Ingestion

Objectives: Dietary lipid absorption usually occurs with absorption of other nutrients because lipid is contained in foods fed as a meal. The effect of simultaneously fed carbohydrate and protein on lipid absorption is not clear. In this study, lymphatic lipid transports in the rat intestine were observed during intraduodenal lipid feeding with or without simultaneous feeding of glucose or amino acids. Methods: Mesenteric lymph duct was cannulated in male SD rats and a feeding tube was inserted into the duodenum through the fundus of the stomach. Postoperatively, the rats were intraduodenally infused with saline. On the day after surgery, the saline infusion was replaced by a lipid infusion containing 40 μmol/h (35.4 mg/h) of triolein, 2.74 μmol/h (1.06 mg/h) of cholesterol, 7.8 μmol/h ( 6.08 mg/h) of egg lecithin with 300 mg/h of glucose (the Glucose group), with 150 mg/h of amino acids derived from medical amino acid injections (the Amino Acids group), or without any additive (the Control group). The lipid emulsion was infused at 3mL/h for 8 hours. Results: The amounts of triglyceride transported in lymph for 8 hours were 185 ± 12 (mean ± SE) mg in the Amino Acids group (n=4), 175 ± 3 mg in the Glucose group (n=5), and 147 ± 7 mg in the Control group (n=4), respectively, with a statistically significant difference (p < 0.05) among the groups. The amount of cholesterol transported in lymph for 8 hours were 7.30 ± 0.63 mg in the Amino Acids group, 6.82 ± 0.46 mg in the Glucose group, and 5.96 ± 0.17 mg in the Control group, respectively. The amount of phosphatidylcholine transported in lymph for 8 hours were 16.4 ± 1.0 mg in the Amino Acids group, 15.7 ± 0.4 mg in the Glucose group, and 12.4 ± 0.3 mg in the Control group, respectively, with a statistically significant difference (p < 0.01) among the groups. Conclusions: Simultaneous glucose or amino acids feeding enhanced lymphatic lipid transport in the rat intestine during lipid feeding.

A pair of nonspecific phospholipases C, NPC2 and NPC6, are involved in gametophyte development and glycerolipid metabolism in Arabidopsis.

Phospholipases play crucial roles in plant membrane lipid homeostasis. Nonspecific phospholipase C (NPCs) establish a unique class of phospholipases found only in plants and certain bacteria. Here, we show that two previously uncharacterized NPC isoforms, NPC2 and NPC6, are required for male and female gametophyte development in Arabidopsis. Double mutant plants of npc2-1 npc6-2 could not be retrieved because npc2-1 npc6-2 ovule and pollen development is affected. Genetic complementation, reciprocal crossing and microscope observation of npc2-1/- npc6-2/+ and npc2-1/+ npc6-2/- plants suggest that NPC2 and NPC6 are redundant and are required for normal gametophyte development. Both NPC2 and NPC6 proteins are localized to the plastids. Promoter-GUS assays in transgenic Arabidopsis revealed that NPC2 and NPC6 are preferentially expressed in floral organs rather than in leaves. In vitro enzyme assays showed that NPC2 and NPC6 hydrolyze phosphatidylcholine and phosphatidylethanolamine, but not phosphatidate, being consistent with the reported substrate selectivity of NPCs. The amounts of phosphatidylcholine, phosphatidylethanolamine and phosphatidylglycerol were increased in buds but not in flowers of npc2-1/- npc6-2/+ and npc2-1/+ npc6-2/- plants, presumably due to reduced phospholipid hydrolysis activity in developing flowers. Our results demonstrate that NPC2 and NPC6 play crucial roles in gametogenesis during flower development.

Fast determination of β-endosulfan, α-hexachlorocyclohexane and pentachlorobenzene in the river water from northeast of China

ABSTRACTA magnetic solid-phase extraction method for the preconcentration of three organochlorine pesticides (OCPs) from water samples has been proposed, based on magnetic phosphatidylcholine (MPC) as adsorbents. The extraction procedure was carried out in a single step by stirring the mixture of MPC and water samples. Subsequently, the MPC was collected by an external magnetic field without additional centrifugation or filtration. The analytes were desorbed from the MPC and finally analysed by gas chromatography–tandem mass spectrometry. The influence of various parameters on OCPs recoveries was studied. Results show that phosphatidylcholine amount and extraction time were critical in enhancing extraction performance, and the presence of humic acid was shown to significantly reduce the extraction efficiency. The limits of detection obtained were in the range of 0.1–0.15 ng L−1. Recoveries of spiked water samples ranged from 76.2% to 101.5% with relative standard deviations varying from 3.8% to 7.7%. The proposed method was employed for analysis of pentachlorobenzene, α-hexachlorocyclohexane and β-endosulfan in the surface water from two rivers in northeast China.

Age-related changes phospholipids of sterlet in liver and dorsal muscles.

Study of phospholipids changes peculiarities in the liver and dorsal muscles of sterlet (Acipenser ruthenus Linnaeus) may be important to determine the etiology and pathogenesis of fatty liver. We established that the content of total phospholipids in tissues of the liver and dorsal muscles of three-year-old sterlet was less than for two-year-old fish by 15% and 20% (P ≤ 0.01), respectively. The amount of phosphatidylcholine (P ≤ 0.05), phosphatidylethanolamine, phosphatidylserine (P ≤ 0.01), phosphatidylinositol (P ≤ 0.01) and cardiolipin in the liver of 3-year-old sterlet was lower than for the 2-year-old fish, while quantitative indices for lysophosphatidylcholine and sphingomyelin were slightly increased. Similarly, in the cells of the dorsal muscles, the amount of phospholipid components (except lysophosphatidylcholine) was decreased with age. A decrease in the amount of phosphatidylethanolamine and phosphatidylserine in the dorsal muscles of 3-year-old sterlet was significant. The major phospholipids respective distribution was stable, except for phosphatidylethanolamine and particularly sphingomyelin.

Alteration of phospholipids in the blood of patients with Duchenne muscular dystrophy (DMD): in vitro, high resolution 31P NMR-based study.

In vitro, high-resolution 31P NMR (Nuclear Magnetic Resonance) spectroscopy-based analysis of phospholipids in serum is well recognized in leukemia, lymphoma, non-hematological cancers and renal cell carcinoma. In context of these studies, phospholipids were analyzed in blood of thirty-two (n=32) patients with Duchenne muscular dystrophy (DMD) (Age, Mean±SD; 8.0±1.6years) and sixteen (n=16) healthy subjects (Age, Mean±SD; 8.6±2.3years). Quantity of phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidylinositol (PI), phosphatidylserine (PS) and lyso-phosphatidylcholine (Lys-PC) was significantly higher (p<0.05) in DMD patients as compared to healthy subjects. There were no significant differences (p>0.05) observed for the quantity of phospholipids in blood of gene deletion positive cases of DMD as compared to negative gene deletion cases of DMD. Quantity of phospholipids in negative gene deletion cases of DMD patients as well as DMD cases with positive gene deletion was significantly higher (p<0.05) as compared to normal individuals. The present study distinguishes the patients with DMD from the healthy subjects on the basis of the quantity of phospholipids in blood. These observations may be useful in future for the development of new diagnostic method of DMD.

Liver lipid metabolism is altered by increased circulating estrogen to androgen ratio in male mouse

Estrogens are suggested to lower the risk of developing metabolic syndrome in both sexes. In this study, we investigated how the increased circulating estrogen-to-androgen ratio (E/A) alters liver lipid metabolism in males. The cytochrome P450 aromatase (P450arom) is an enzyme converting androgens to estrogens. Male mice overexpressing human aromatase enzyme (AROM+ mice), and thus have high circulating E/A, were used as a model in this study. Proteomics and gene expression analyses indicated an increase in the peroxisomal β-oxidation in the liver of AROM+ mice as compared with their wild type littermates. Correspondingly, metabolomic analysis revealed a decrease in the amount of phosphatidylcholines with long-chain fatty acids in the plasma. With interest we noted that the expression of Cyp4a12a enzyme, which specifically metabolizes arachidonic acid (AA) to 20-hydroxy AA, was dramatically decreased in the AROM+ liver. As a consequence, increased amounts of phospholipids having AA as a fatty acid tail were detected in the plasma of the AROM+ mice. Overall, these observations demonstrate that high circulating E/A in males is linked to indicators of higher peroxisomal β-oxidation and lower AA metabolism in the liver. Furthermore, the plasma phospholipid profile reflects the changes in the liver lipid metabolism.

Search for Potential Biomarkers by UPLC/Q-TOF–MS Analysis of Dynamic Changes of Glycerophospholipid Constituents of RAW264.7 Cells Treated With NSAID

It is well-known that alteration of the glycerophospholipid (GPL) constituents of tissues can lead to disease. We report dynamic changes of GPL constituents of RAW264.7 cells with different status, revealed by use of modern analytical techniques and chemometrics to find potential biomarkers. An inflammation model of Kdo2-lipid A (KLA)-stimulated RAW264.7 cells was developed. Effects on the model of treatment with three non-steroidal anti-inflammatory drugs (NSAID), aspirin, indomethacin, and brufen, were determined by use of UPLC-Q/TOF–MS analysis. Total-ion-current profiles representative of GPL metabolism under different conditions were acquired and the data were processed by principal-components analysis (PCA) and partial least-squares discriminant analysis (PLSDA). The results revealed changes of GPL metabolites related to the anti-inflammatory effects of the NSAID. Seventeen potential biomarkers were selected by use of t tests, Shrinkt, Principal Component Linear Discriminant (PCLDA), Variable importance in projection (VIP), and PLSDA. Among these biomarkers, amounts of phosphatidylcholine (PC, 16:0/18:1) and phosphatidylethanolamine (PE, 18:0/18:1) changed significantly in the three NSAID treatment groups and may be the important GPL biomarkers of the occurrence and resolution of inflammation. UPLC/Q-TOF–MS-based metabolomics provide novel insight into the mechanism of action of anti-inflammatory drugs distinct from that afforded by traditional biological investigations.

Effect of Surfactants on Characteristic and &lt;i&gt;In Vitro&lt;/i&gt; Release of Meloxicam Loaded in Deformable Liposomes

The aim of this study was to investigate the effect of surfactants on characteristic and in vitro release of liposomes containing meloxicam (MX), model of water insoluble drug. The potential use of deformable liposomes for drug delivery system was developed and investigated. The formulation composed of constant amount of phosphatidylcholine (PC) and MX and various amounts of cholesterol (Chol), sodium cholate (NaChol), sodium oleate (NaO) and stearylamine (SA) was formulated by reverse phase evaporation method. The vesicle size, zeta potential, morphology, entrapment efficiency, loading efficiency, stability andin vitrorelease study were evaluated. The result indicated that the entrapment efficiency andin vitrorelease study of vesicle formulations containing surfactants were significantly higher than the conventional liposome and MX suspension. The formulation of 10:2:2:5 PC/MX/Chol/NaO provided the maximum entrapment efficiency and drug release. Our research suggested that MX loaded in deformable liposomes containing surfactants can be potentially used as a drug delivery carrier for water insoluble drug.

Jamming dynamics of stretch-induced surfactant release by alveolar type II cells

Secretion of pulmonary surfactant by alveolar epithelial type II cells is vital for the reduction of interfacial surface tension, thus preventing lung collapse. To study secretion dynamics, rat alveolar epithelial type II cells were cultured on elastic membranes and cyclically stretched. The amounts of phosphatidylcholine, the primary lipid component of surfactant, inside and outside the cells, were measured using radiolabeled choline. During and immediately after stretch, cells secreted less surfactant than unstretched cells; however, stretched cells secreted significantly more surfactant than unstretched cells after an extended lag period. We developed a model based on the hypothesis that stretching leads to jamming of surfactant traffic escaping the cell, similar to vehicular traffic jams. In the model, stretch increases surfactant transport from the interior to the exterior of the cell. This transport is mediated by a surface layer with a finite capacity due to the limited number of fusion pores through which secretion occurs. When the amount of surfactant in the surface layer approaches this capacity, interference among lamellar bodies carrying surfactant reduces the rate of secretion, effectively creating a jam. When the stretch stops, the jam takes an extended time to clear, and subsequently the amount of secreted surfactant increases. We solved the model analytically and show that its dynamics are consistent with experimental observations, implying that surfactant secretion is a fundamentally nonlinear process with memory representing collective behavior at the level of single cells. Our results thus highlight the importance of a jamming dynamics in stretch-induced cellular secretory processes.

Morphology and structure of lipoproteins revealed by an optimized negative-staining protocol of electron microscopy

Plasma lipoprotein levels are predictors of risk for coronary artery disease. Lipoprotein structure-function relationships provide important clues that help identify the role of lipoproteins in cardiovascular disease. The compositional and conformational heterogeneity of lipoproteins are major barriers to the identification of their structures, as discovered using traditional approaches. Although electron microscopy (EM) is an alternative approach, conventional negative staining (NS) produces rouleau artifacts. In a previous study of apolipoprotein (apo)E4-containing reconstituted HDL (rHDL) particles, we optimized the NS method in a way that eliminated rouleaux. Here we report that phosphotungstic acid at high buffer salt concentrations plays a key role in rouleau formation. We also validate our protocol for analyzing the major plasma lipoprotein classes HDL, LDL, IDL, and VLDL, as well as homogeneously prepared apoA-I-containing rHDL. High-contrast EM images revealed morphology and detailed structures of lipoproteins, especially apoA-I-containing rHDL, that are amenable to three-dimensional reconstruction by single-particle analysis and electron tomography.

ABCA3+/- mice have significantly decreased amounts of phosphatidylcholine and phosphatidylglycerol in lung tissue

ABCA3+/- mice have significantly decreased amounts of phosphatidylcholine and phosphatidylglycerol in lung tissue

Lipid composition of the mucoraceous fungus Blakeslea trispora under lycopene formation-stimulating conditions

Stimulation of lycopene synthesis in the mycelium of the mucoraceous fungus Blakeslea trispora was accompanied by major changes in its lipid composition. The phospholipid content in the membrane lip-ids doubled, whereas the sterol and sphingolipid levels changed insignificantly. The amounts of phosphatidyl-choline, phosphatidylethanolamine, and phosphatidic acid in the phospholipids and the triacylglycerol content in the acylglycerols increased. The desaturation degree of fatty acids drastically increased against the background of a decrease in that of the neutral lipids. The data obtained are discussed in relation to the mechanism of action of the lycopene formation stimulator.

Phosphatidyl choline-based colloidal systems for dermal and transdermal drug delivery

In this study we have prepared various phosphatidyl choline based colloidal systems, namely liposomes, transfersomes, microemulsions and micelles, using similar excipients and compared their ability to deliver drugs into and through the skin under occlusive and non-occlusive conditions. Hydrophilic propranolol hydrochloride (PHCl) and lipophilic propranolol base (PB) were used as model drugs. All tested parameters, that is formulation composition, drug characteristics and testing conditions, influenced skin permeability and skin retention. A trend was observed showing that the skin permeation as well as skin retention decreases with the amount of phosphatidyl choline in the formulations for both tested model drugs (micelles > transfersomes > liposomes > microemulsion). The lipophilic model drug had higher skin permeability especially when incorporated into the systems containing mainly hydrophilic excipients. Skin retention, however, was not affected by the drug hydrophilicity to the same extent as skin permeability. Occlusion increased both skin retention and skin permeation for both model drugs.