scholarly journals Lipid-Based Nanocarrier System for the Effective Delivery of Nutraceuticals

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5510
Author(s):  
Parthasarathi Subramanian
Keyword(s):  
Intestinal Absorption ◽  
Health Benefits ◽  
Lipid Nanoparticles ◽  
Lymphatic Transport ◽  
Mass Ratio ◽  
Carrier System ◽  
Current Limitation ◽  
Effective Delivery ◽  
Critical Overview

Nutraceuticals possess several health benefits and functions; however, most nutraceuticals are prone to degradation in the gastrointestinal environment and have poor bioavailability. Application of a novel carrier system is of increasing importance to overcome obstacles and provide efficient applicability. Lipid-based nanocarriers provide a large surface-to-mass ratio, enhanced intestinal absorption by solubilization in the intestinal milieu, intestinal lymphatic transport, and altering enterocyte-based transport. A critical overview of the current limitation, preparation, and application of lipid-based nanocarriers (liposomes and niosomes) and lipid nanoparticles (SLNs and NLCs) is discussed. Physical and gastrointestinal stability and bioavailability of nanoencapsulated nutraceuticals are considered as well.

Can lipid nanoparticles improve intestinal absorption?

2016 ◽  
Vol 515 (1-2) ◽  
pp. 69-83 ◽  
Author(s):  
M. Mendes ◽  
H.T Soares ◽  
L.G Arnaut ◽  
J.J Sousa ◽  
A.A.C.C. Pais ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Lipid Nanoparticles

Effect of soy protein and casein intake on intestinal absorption and lymphatic transport of cholesterol and oleic acid

1984 ◽  
Vol 40 (6) ◽  
pp. 1156-1164 ◽  
Author(s):  
G V Vahouny ◽  
W Chalcarz ◽  
S Satchithanandam ◽  
I Adamson ◽  
D M Klurfeld ◽  
...  
Keyword(s):  
Oleic Acid ◽  
Intestinal Absorption ◽  
Soy Protein ◽  
Lymphatic Transport

Triacylglycerol and cholesterol transport during absorption of glycerol trioleate vs. glycerol trielaidate

1996 ◽  
Vol 270 (2) ◽  
pp. G268-G276
Author(s):  
T. J. Kalogeris ◽  
L. Gray ◽  
Y. Y. Yeh ◽  
P. Tso
Keyword(s):  
Fatty Acid Composition ◽  
Fatty Acid ◽  
Intestinal Absorption ◽  
Acid Composition ◽  
Trans Fatty Acid ◽  
Cholesterol Absorption ◽  
Lymphatic Transport ◽  
Cholesterol Transport ◽  
Lipid Emulsions ◽  
Intestinal Lymph

We used conscious, chronic lymph-fistula rats to compare intestinal lymphatic transport of glycerol trioleate (TO) vs. glycerol trielaidate (TE) and to determine the effect of TO vs. TE on absorption and transport of cholesterol. Rats were implanted with intestinal lymph fistulas and duodenal cannulas and then given intraduodenal infusions of lipid emulsions containing purified TO or TE (40 mumol/h) and cholesterol (7.8 mumol/h + 2 microCi [14C]cholesterol). Lymph samples were collected at 0, 2, 4, 5, 6, 7, and 8 h after the start of lipid infusion. Lymphatic output and luminal and gut wall recovery of radioactive lipid at 8 h were quantified. Triacylglycerol (TG) fatty acid isomers did not affect lymphatic output of TG; lymph TG fatty acid composition and output reflected infusate composition. Lymphatic output of cholesterol (mass and radioactivity) did not differ between groups; luminal and gut wall recovery of [14C]cholesterol was also similar between groups. Similar lymphatic transport of TG and cholesterol between triolein- and trielaidin-infused rats was maintained for up to 16 h after the cessation of an infused lipid load. These results indicate that TO and TE are transported into lymph similarly, and that cholesterol absorption and transport are similar irrespective of whether TO or TE is the TG source. The data suggest that trans fatty acid-induced hypercholesterolemia is not due to altered intestinal absorption and transport of cholesterol.

scholarly journals Polyelectrolyte Nanoparticles of Amphiphilic Chitosan/Pectin from Banana Peel as Potential Carrier System of Hydrophobic Molecules

Polymers ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 2109
Author(s):  
Paula A. Méndez ◽  
Betty L. López
Keyword(s):  
Particle Size ◽  
Nile Red ◽  
Banana Peel ◽  
Loading Capacity ◽  
Mass Ratio ◽  
Carrier System ◽  
Acid Type ◽  
Hydrophobic Molecule ◽  
Acidic Conditions ◽  
Banana Wastes

In this study, pectins were extracted from banana wastes Musa paradisiaca under different acidic conditions, obtaining pectins with different degrees of esterification (DE) depending on the acid type and pH. The formation of the polyelectrolyte nanoparticles was evaluated according to the DE of the pectin, the mass ratio of the polymers of pectin to amphiphilic chitosan (AmCh), and their concentration. The properties of the polyelectrolyte nanoparticles were evaluated at different pH and temperatures. The pectin with 24.3% DE formed polyelectrolyte nanoparticles through the electrostatic interaction with AmCh, which was evidenced by changes in the zeta potential and particle size. The study of mass ratio AmCh:Pectin, to get a stable system, showed that it must be at least equal (1:1), or AmCh must be in higher proportion (6:1, 50:1, 100:1), and the polymers concentration must be 1 mg/mL. The study of the temperature effect showed that, when the temperature increases, the particle size decreases, and the pH study showed a stable particle size for the polyelectrolyte nanoparticles in the range of pH 5–6. Nile Red (NR), a hydrophobic molecule, was encapsulated in the polyelectrolyte nanoparticles with a loading capacity of 1.8% and an encapsulation efficiency of 80%.

scholarly journals Factorial Design Studies and Biopharmaceutical Evaluation of Simvastatin Loaded Solid Lipid Nanoparticles for Improving the Oral Bioavailability

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Kovoru Krishnam Raju ◽  
Beeravelli Sudhakar ◽  
Kolapalli Venkata Ramana Murthy
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Competitive Inhibition ◽  
Polymeric Nanoparticles ◽  
Analytical Techniques ◽  
Lipid Nanoparticles ◽  
Lymphatic Transport ◽  
Solid Lipid ◽  
Reductase Inhibitors ◽  
Coa Reductase

Statins are HMG-CoA reductase inhibitors, which lower the cholesterol level through reversible and competitive inhibition; they are involved in the biosynthesis of cholesterol and other sterols. Simvastatin exhibits poor oral bioavailability (<5%) and undergoes extensive microsomal metabolism by CYP enzymes. CYP3A4 is the major metabolizing enzyme that metabolizes lactone form of simvastatin and significantly lowers intestinal uptake. The hydrophobic properties of simvastatin prevent complete dissolution of the drug in the intestinal fluid which also contributes to its lower bioavailability. SLNs are alternative carrier system to polymeric nanoparticles. SLNs are in submicron size range (1–1000 nm). To overcome the hepatic first pass metabolism and to enhance the bioavailability, intestinal lymphatic transport of drugs can be exploited. In the present study, attempt has been made to prepare solid lipid nanoparticles of simvastatin to improve the bioavailability. SLNs of simvastatin were prepared with Trimyristin by hot homogenization followed by ultrasonication method. The SLNs were characterized for various physicochemical properties and analytical techniques like PXRD, DSC to study thermal nature and morphology of formulation and excipients. Promising results of the study indicated the applicability of simvastatin solid lipid nanoparticles as potential tools for improvement of bioavailability of poorly soluble drugs.

scholarly journals The proportion of lycopene isomers in human plasma is modulated by lycopene isomer profile in the meal but not by lycopene preparation

2011 ◽  
Vol 107 (10) ◽  
pp. 1482-1488 ◽  
Author(s):  
Myriam Richelle ◽  
Pierre Lambelet ◽  
Andreas Rytz ◽  
Isabelle Tavazzi ◽  
Anne-France Mermoud ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Human Plasma ◽  
Health Benefits ◽  
Healthy Men ◽  
Low Level

Dietary lycopene consists mostly of the (all-E) isomer. Upon absorption, (all-E) lycopene undergoes isomerisation into various (Z)-isomers. Because these isomers offer potentially better health benefits than the (all-E) isomer, the aim of the present study was to investigate if the profile of lycopene isomers in intestinal lipoproteins is affected by the profile of lycopene isomers in the meal and by the tomato preparation. Six postprandial, crossover tests were performed in healthy men. Three meals provided about 70 % of the lycopene as (Z)-isomers, either mainly as 5-(Z) or 13-(Z), or as a mixture of 9-(Z) and 13-(Z) lycopene, while three tomato preparations provided lycopene mainly as the (all-E) isomer. Consumption of the 5-(Z) lycopene-rich meal led to a high (60 %) proportion of this isomer in TAG-rich lipoproteins (TRL), indicating a good absorption and/or a low intestinal conversion of this isomer. By contrast, consumption of meals rich in 9-(Z) and 13-(Z) lycopene isomers resulted in a low level of these isomers but high amounts of the 5-(Z) and (all-E) isomers in TRL. This indicates that the 9-(Z) and 13-(Z) isomers were less absorbed or were converted into 5-(Z) and (all-E) isomers. Dietary (Z)-lycopene isomers were, therefore, differently isomerised and released in TRL during their intestinal absorption in men. Consuming the three meals rich in (all-E) lycopene resulted in similar proportions of lycopene isomers in TRL: 60 % (all-E), 20 % 5-(Z), 9 % 13-(Z), 2 % 9-(Z) and 9 % unidentified (Z)-isomers. These results show that the tomato preparation has no impact on the lycopene isomerisation occurring during absorption in humans.

scholarly journals A review: Possible optimization of Cas9-sgRNA nuclease delivery via ingested lipid nanoparticles bioencapsulated within plant cell-based enfolding

2019 ◽  
Author(s):  
Tatiana Hillman
Keyword(s):  
Dna Sequences ◽  
Genetic Disorders ◽  
Single Point ◽  
Lipid Nanoparticles ◽  
Single Point Mutation ◽  
Cas9 Nuclease ◽  
Target Dna ◽  
Effective Delivery ◽  
Sgrna Design

The possibility of gene editing to correct disorders is one of the most impactful therapeutic agents, currently. CRISPR Cas9-sgRNA nucleases can be used to cleave and to delete harmful or pathogenic DNA sequences, which cause genetic disorders. Cas9 nuclease includes palindromic repeats that cut and delete a single point mutation or multiple DNA target site sequences. The Cas9, attached to a sgRNA or a guiding RNA, finds and then cleaves the target DNA sequence. The Cas9-sgRNA method of cleavage has corrected DNA mutations that cause cataracts in the eyes, cystic fibrosis, and chronic granulomatous disease. However, there are issues with an effective delivery of Cas9-sgRA to target DNA sequences. Delivering Cas-9 nucleases are negatively affected by off-target DNA sites, sgRNA design, off-target cleavage, Cas9 activation, and the method of delivery. This review focuses on oral and ingested delivery methods to effectively guide the transport of Cas9-sgRNA nucleases in vivo. This review presents possible alternatives for nuclease delivery within optimized lipid-nanoparticles, plant, algae, and bacterial-based orally ingested edibles. This review attempts to provide evidence in support of the higher effectiveness of ingesting therapeutic bioencapsulated edibles because the edibles can directly contact immune cells within the gastrointestinal tract for blood or lymph circulation.

scholarly journals Case studies of enhanced pharmacodynamic activity of poorly oral bioavailable drugs via solid lipid nanoparticles

2021 ◽  
Vol 11 (2) ◽  
pp. 204-208
Author(s):  
D Raju
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Absorption ◽  
Lipid Nanoparticles ◽  
Lymphatic Transport ◽  
Therapeutic Effectiveness ◽  
Therapeutic Activity ◽  
Solid Lipid ◽  
Current Review ◽  
Colloidal Carrier ◽  
Carrier Systems

Solid lipid nanoparticles (SLNs) considered as an alternative vehicle for the enhanced oral absorption of drugs, and also to enhance therapeutic effectiveness after oral administration. Pharmacodynamic activity of drug is mainly describes the pharmacological and therapeutic activity of drug to the biological system. Lipid nanoparticles especially SLNs made of physiological inert lipid molecules and helps the lymphatic transport. Numerous literatures is available on the effect of SLNs and other colloidal carrier systems on the pharmacokinetic activity of poorly bioavailable drugs, to improve their oral absorption and also respective mechanisms for the improved oral bioavailability. However, very few literatures is reported on the pharmacodynamic activity and the effect of dose on the pharmacodynamic activity. Therefore, the current review is mainly dealing with the effect of SLNs on the pharmacodynamic activity discussed.   Keywords: Oral absorption, solid lipid nanoparticles, lymphatic transport, pharmacokinetics, pharmacodynamics.

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