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

2016 ◽  
Vol 9 (6) ◽  
pp. 3524-3530 ◽  
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. 

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

2019 ◽  
Vol 7 (5) ◽  
pp. 375-388 ◽  
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.

Preparation, Characterization and in vivo Evaluation of Felodipine Solid-Lipid Nanoparticles for Improved Oral Bioavailability

2015 ◽  
Vol 8 (4) ◽  
pp. 2995-3002
Author(s):  
Kishan V ◽  
Usha Kiranmai Gondrala ◽  
Narendar Dudhipala
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation ◽  
Solid Lipid

Felodipine is an antihypertensive drug with poor oral bioavailability due to the first pass metabolism. For improving the oral bioavailability, felodipine loaded solid lipid nanoparticles (SLNs) were developed using trimyristin, tripalmitin and glyceryl monostearate. Poloxamer 188 was used as surfactant. Lipid excipient compatibilities were confirmed by differential scanning calorimetry. SLN dispersions were prepared by hot homogenization of molten lipids and aqueous phase followed by ultrasonication at a temperature, above the melting point. SLNs were characterized for particle size, zeta potential, drug content, entrapment efficiency and crystallinity of lipid and drug. In vitro release studies were performed in 0.1N HCl and phosphate buffer of pH 6.8 using dialysis method. Pharmacokinetics of felodipine-SLNs after oral admini-stration in male Wistar rats was studied. The bioavailability of felodipine was increased by 1.75 fold when compared to that of a felodipine suspension.  

Solid Lipid Nanoparticles (SLNs) Gels for Topical Delivery of Aceclofenac in vitro and in vivo Evaluation

2013 ◽  
Vol 10 (6) ◽  
pp. 656-666 ◽  
Author(s):  
Sandipan Dasgupta ◽  
Surajit Ghosh ◽  
Subhabrata Ray ◽  
Bhaskar Mazumder
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Topical Delivery ◽  
Lipid Nanoparticles ◽  
In Vivo Evaluation ◽  
Solid Lipid

Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery

2021 ◽  
pp. 97-104
Author(s):  
Kumara Swamy S ◽  
Ramesh Alli
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Sustained Drug Release ◽  
Bioavailability Enhancement ◽  
Solid Lipid

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.

Solid lipid nanoparticles for delivery of andrographolide across the blood-brain barrier: in vitro and in vivo evaluation

2018 ◽  
Vol 161 ◽  
pp. 302-313 ◽  
Author(s):  
Giulia Graverini ◽  
Vieri Piazzini ◽  
Elisa Landucci ◽  
Daniela Pantano ◽  
Pamela Nardiello ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Brain Barrier ◽  
In Vivo Evaluation ◽  
Solid Lipid ◽  
Blood Brain

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

RSC Advances ◽  
2017 ◽  
Vol 7 (53) ◽  
pp. 33314-33326 ◽  
Author(s):  
Hasan Ali ◽  
Priya Ranjan Prasad Verma ◽  
Sunil Kumar Dubey ◽  
Jayachandran Venkatesan ◽  
Youngwan Seo ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Pharmacokinetic Studies ◽  
Solid Lipid ◽  
Pharmacokinetic Evaluation

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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