In vitro–in vivo and pharmacokinetic evaluation of solid lipid nanoparticles of furosemide using Gastroplus™

In this work, we conducted pharmacokinetic studies and established the in vitro and in vivo correlation (IVIVC) of furosemide (FRS) loaded solid lipid nanoparticles (FSLN).

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Lacidipine Loaded Solid Lipid Nanoparticles for Oral Delivery: Preparation, Characterization and In vivo Evaluation

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2016.9.6.2 ◽

2016 ◽

Vol 9 (6) ◽

pp. 3524-3530 ◽

Cited By ~ 1

Author(s):

Kishan V. ◽

Sandeep V ◽

Narendar D ◽

Arjun N

Keyword(s):

Solid Lipid Nanoparticles ◽

Oral Bioavailability ◽

Oral Delivery ◽

Lipid Nanoparticles ◽

Pharmacokinetic Studies ◽

Electron Microscopic ◽

In Vivo Evaluation ◽

Solid Lipid

The objective of this study was to develop and evaluate lacidipine (LD) loaded solid lipid nanoparticles (LD-SLNs) for improving the oral bioavailability. LD-SLNs were prepared in two steps. First step was hot homogenization and next by ultrasonication method, using triglycerides (tripalmitin and tristearin), monoglyceride and surfactants (Poloxamer 188 and egg lecithin E80). The prepared LD-SLNs were characterized for particle size, PDI, zeta potential, drug content, entrapment efficiency (EE %). In vitro drug release studies using a dialysis bag method in 0.1N HCl and pH 6.8 phosphate buffer were conducted. In addition, long-term physical stability of the optimized SLNs was investigated at refrigerated and room temperature for 60 days. FTIR and DSC studies revealed that no interaction between the drug and lipids. LD-SLNs prepared with Dynasan-116 (F3), having the size of 141.86nm, PDI of 0.293, ZP of -22.3 m with 94.75% of EE was optimized and was stable for 60days. Scanning electron microscopic studies showed nearly spherical shaped particles. Further, pharmacokinetic studies were conducted in wistar rats. The relative bioavailability of LD in SLNs was 2.03 times when compared with that of the LD suspension. The results are indicative of SLNs as suitable lipid based carrier system for improving the oral bioavailability of LD.

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Cytotoxicity and Biological Efficacy of Exendin-4-Encapsulated Solid Lipid Nanoparticles in INS-1 Cells

Journal of Nanomaterials ◽

10.1155/2015/753569 ◽

2015 ◽

Vol 2015 ◽

pp. 1-6 ◽

Cited By ~ 3

Author(s):

Hee-Sook Jun ◽

Gongdeuk Bae ◽

Young Tag Ko ◽

Yoon Sin Oh

Keyword(s):

Solid Lipid Nanoparticles ◽

Biological Effects ◽

Lipid Nanoparticles ◽

Pharmacokinetic Studies ◽

Mrna Levels ◽

Solid Lipid ◽

Vehicle Treatment ◽

Glucagon Like Peptide 1

Exendin-4 (Ex-4), a peptide of glucagon-like peptide-1 receptor agonist, is a potent insulinotropic agent and alternative drug delivery systems to increase therapeutic utility have been explored. We developed exendin-4-encapsulated solid lipid nanoparticles (Eudragit Ex-4 SLNs) and compared the effects of Eudragit Ex-4 SLNs with those of native Ex-4 on INS-1 cells. We observed no significant toxic effects of nanoparticles at concentrations from 1 nM to 100 nM. Similar to Ex-4, Eudragit Ex-4 SLNs stimulated the production of cyclic AMP at 10 nM. Moreover, unlike treatment with the vehicle, treatment with 10 nM Eudragit Ex-4 SLNs increased insulin mRNA levels and insulin secretion. These insulinotropic effects of Eudragit Ex-4 SLNs were comparable to those of Ex-4. Thus, ourin vitroresults suggest that the biological effects of Eudragit Ex-4 SLNs are similar to those of Ex-4, and furtherin vivopharmacokinetic studies are required to propose an alternative sustained release drug system.

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Solid Lipid Nanoparticles of Dronedarone Hydrochloride for Oral Delivery: Optimization, In Vivo Pharmacokinetics and Uptake Studies

Pharmaceutical Nanotechnology ◽

10.2174/2211738507666190802140607 ◽

2019 ◽

Vol 7 (5) ◽

pp. 375-388 ◽

Cited By ~ 2

Author(s):

Vaishali M. Gambhire ◽

Makarand S. Gambhire ◽

Nisharani S. Ranpise

Keyword(s):

Particle Size ◽

Solid Lipid Nanoparticles ◽

Oral Bioavailability ◽

Oral Delivery ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Pharmacokinetic Studies ◽

Solid Lipid

Background: Dronedarone HCl (DRD), owing to its poor aqueous solubility and extensive presystemic metabolism shows low oral bioavailability of about 4% without food, which increases to approximately 15% when administered with a high fat meal. Objective: Solid lipid nanoparticles (SLN) were designed with glyceryl monstearate (GMS) in order to improve oral bioavailability of DRD. Methods: Hot homogenization followed by probe sonication was used to prepare SLN dispersions. Box-Behnken design was used to optimize manufacturing conditions. SLN were characterized for particle size, zeta potential, entrapment efficiency, physical state and in vitro drug release. Pharmacokinetics and intestinal uptake study of dronedarone HCl loaded solid lipid nanoparticles (DRD-SLN) in the presence and absence of endocytic uptake inhibitor, chlorpromazine (CPZ) was performed with conscious male Wistar rats. Results: Optimized formulation of SLN showed particle size of 233 ± 42 nm and entrapment efficiency of 87.4 ± 1.29%. Results of pharmacokinetic studies revealed enhancement of bioavailability of DRD by 2.68 folds from SLN as compared to DRD suspension. Significantly reduced bioavailability of DRD-SLNs in the presence of chlorpromazine, demonstrated the role of endocytosis in uptake of SLN formulation. Conclusion: These results indicated that dronedarone HCl loaded SLN could potentially be exploited as a delivery system for improving oral bioavailability by minimizing first pass metabolism.

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