Untitled

Seeballuck, Fergal; Ashford, Marianne; O’Driscoll, Caitriona M.

doi:10.1023/a:1024422625596

Cited by 64 publications

(4 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In the present study, SLNs were fabricated using surfactant mixture composed of lecithin and poloxamer 188, and the ratio of lecithin to poloxamer 188 was fixed at 1:4 to achieve a small particle size. It has been reported that the presence of phospholipid on the shell layer of SLNs could increase the absorption and entrapment in microvilli because the phospholipid of soy lecithin is similar to the phospholipid bilayer structure of cellular membrane [30]. Formulation variables involved in the preparation of SLNs were optimized to achieve a smaller particle size (238 ± 10.9 nm) and high EE% (79 ± 2.8%).…”

Section: Discussionmentioning

confidence: 99%

Preparation, Characterization and Anti-Ulcer Efficacy of Sanguinarine Loaded Solid Lipid Nanoparticles

Sun¹,

Liu

et al. 2017

Pharmacology

View full text Add to dashboard Cite

Aim: This study was designed to develop sanguinarine-loaded solid lipid nanoparticles (SG-SLNs) and investigate its gastroprotective effect on ethanol-induced gastric mucosal lesions in mice. Methods: SG-SLNs were prepared by high temperature melt-cool solidification method using glycerol monostearate as the lipid and a combination of lecithin with poloxamer 188 as the surfactants. Solid lipid nanoparticles (SLNs) were designed at varying lipid concentrations (5, 10, 15, and 20 mg/mL), surfactant mixture concentrations (6, 12, and 18 mg/mL), and drug contents (5, 10, 15, and 20 mg/mL) in “one factor at a time” fashion. Ethanol-induced gastric ulcer model was performed on Kunming mice to examine the anti-inflammatory activity of SG-SLNs and compare it with sanguinarine (SG). Results: The high temperature melt-cool solidification method provided consistent production of SLNs with smaller size and high entrapment efficiency (EE%). The composition of optimal formulation was 10 mg/mL lipid concentration, 18 mg/mL surfactant mixture concentration, and 15 mg/mL drug amount. The mean particle size and EE% of optimized formulation were 238 ± 10.9 nm and 79 ± 2.8%, respectively. Additionally, SG-SLNs significantly decreased tumor necrosis factor-alpha and interleukin-6 levels in the serum and gastric tissue, and reduced the content of NO in serum, and strengthened the protection of mucosal membrane. Moreover, SG-SLNs treatment markedly inhibited ethanol-induced nuclear factor-kappa B (NF-κB) activation when compared with SG. Conclusions: SLNs could be potentially applied as a delivery system of SG. The protective effect of SG-SLNs is due to the suppression of NF-κB expression and subsequent pro-inflammatory cytokines release.

show abstract

Section: Discussionmentioning

confidence: 99%

Preparation, Characterization and Anti-Ulcer Efficacy of Sanguinarine Loaded Solid Lipid Nanoparticles

Sun¹,

Liu

et al. 2017

Pharmacology

View full text Add to dashboard Cite

show abstract

“…Both Pluronic block copolymers L-81 and P-85 have been examined together in the same studies including lipid-Pluronic interactions [23], cellular uptake of proteins [24], and functional activity of multidrug resistance-associated proteins [25]. Both nonionic surfactants have also been shown to inhibit intestinal P-glycoprotein efflux [26, 27]. In this study, we investigated the effect of the inhibition of chylomicron formation by L-81 and P-85 on the secretion of GLP-1 and GIP, as well as the role of free fatty acids (FFA) on incretin release.…”

Section: Introductionmentioning

confidence: 99%

Chylomicron Formation and Secretion is Required for Lipid‐Stimulated Release of Incretins GLP‐1 and GIP

Yang

et al. 2012

Lipids

View full text Add to dashboard Cite

Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are incretins produced in the intestine that play a central role in glucose metabolism and insulin secretion. Circulating concentrations of GLP-1 and GIP are low and can be difficult to assay in rodents. These studies utilized the novel intestinal lymph fistula model we have established to investigate the mechanism of lipid-stimulated incretin secretion. Peak concentrations of GLP-1 and GIP following an enteral lipid stimulus (Liposyn) were significantly higher in intestinal lymph than portal venous plasma. To determine whether lipid-stimulated incretin secretion was related to chylomicron formation Pluronic L-81 (L-81), a surfactant inhibiting chylomicron synthesis, was given concurrently with Liposyn. The presence of L-81 almost completely abolished the increase in lymph triglyceride seen with Liposyn alone (P < 0.001). Inhibition of chylomicron formation with L-81 reduced GLP-1 secretion into lymph compared to Liposyn stimulation alone (P = 0.034). The effect of L-81 relative to Liposyn alone had an even greater effect on GIP secretion, which was completely abolished (P = 0.004). These findings of a dramatic effect of L-81 on lymph levels of GLP-1 and GIP support a strong link between intestinal lipid absorption and incretin secretion. The relative difference in the effect of L-81 on the two incretins provides further support that nutrient-stimulation of GIP and GLP-1 is via distinct mechanisms.

show abstract

“…It also brings new opportunities for various excipients that are emerging as bioactive recently in the last decade [76]. Further, excipients such as Cremophor EL and pluronic polymers have been shown to decrease chylomicron production and reduce the P-gp efflux transport of drug molecules [77,78]. One of the versatile excipients in this category is tween 80 which has been found as excellent solubilizer, inhibitor of P-gp efflux and increase chylomicron production [76,79].…”

Section: Lymphatic Transport Of Lipid Carriersmentioning

confidence: 99%

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Desai¹,

Desai²,

Patel³

2023

Drug Formulation Design

View full text Add to dashboard Cite

The drug administered by an oral route has to withstand a harsh environment of gastrointestinal media, absorb through intestinal epithelium and circumvent first-pass metabolism in liver before reaching portal blood circulation. Moreover, hydrophobic drug molecules offer challenges for formulation with respect to their solubility and hence bioavailability. Various approaches have been developed to overcome this barrier. One of them is the use of lipids in formulation. Incorporation of the drug in lipids can result in increased solubility, absorption and thereby enhanced bioavailability. Intestinal lymphatic route of absorption has also been explored for increasing bioavailability of hydrophobic drug moieties. In this chapter, we have discussed the pathway of lipid digestion in the human body as well as the mechanism of lipid particles upon oral administration. The various lipid formulations developed and the excipients used in the formulations have also been described. The importance of lipid chain length and the effect of food in increasing the bioavailability of drug is discussed. The lymphatic pathway of lipid carriers has also been discussed.

show abstract

Untitled

Cited by 64 publications

References 28 publications

Preparation, Characterization and Anti-Ulcer Efficacy of Sanguinarine Loaded Solid Lipid Nanoparticles

Preparation, Characterization and Anti-Ulcer Efficacy of Sanguinarine Loaded Solid Lipid Nanoparticles

Chylomicron Formation and Secretion is Required for Lipid‐Stimulated Release of Incretins GLP‐1 and GIP

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Contact Info

Product

Resources

About