Enhancement of oral bioavailability of pentoxifylline by solid lipid nanoparticles

2009 ◽  
Vol 00 (00) ◽  
pp. 090820062440031-9 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Mohsen Minayian ◽  
Elaheh Moazen
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Lipid Nanoparticles ◽  
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.

Development of Lipid-Based Nanocarriers for Increasing Gastrointestinal Absorption of Lupinifolin

Planta Medica ◽  
2020 ◽  
Vol 86 (05) ◽  
pp. 364-372 ◽  
Author(s):  
Jidapa Musika ◽  
Nuannoi Chudapongse
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Medium Chain Triglyceride ◽  
Lipid Nanoparticles ◽  
Delivery Systems ◽  
Nanostructured Lipid Carriers ◽  
Gastrointestinal Absorption ◽  
Prolonged Release ◽  
Solid Lipid ◽  
Lipid Nanocarriers

AbstractLupinifolin, a plant flavonoid, has been reported to possess various pharmacological effects. It most likely exerts low oral bioavailability because of poor water solubility. The objective of this study was to develop lipid nanocarriers as drug delivery systems to increase the gastrointestinal absorption of lupinifolin extracted from Albizia myriophylla. Three types of nanocarriers, lupinifolin-loaded solid lipid nanoparticles, lupinifolin-loaded nanostructured lipid carriers, and lupinifolin-loaded nanoemulsions, were prepared by an emulsification-sonication technique. All three types of nanocarriers loaded with lupinifolin, lupinifolin-loaded solid lipid nanoparticles, lupinifolin-loaded nanostructured lipid carriers, and lupinifolin-loaded nanoemulsions, were successfully synthesized. The lipid components chosen to formulate nanocarriers were tripalmitin and/or medium chain triglyceride. Physicochemical characterizations along with releasing profiles of lupinifolin-loaded lipid nanocarriers were compared. It was found that the best lipid nanocarrier for lupinifolin was lupinifolin-loaded nanostructured lipid carriers, which demonstrated the particle size of 151.5 ± 0.1 nm, monodispersity distribution with a polydispersity index of 0.24, negative surface charge at − 41.2 ± 0.7 mV, high encapsulation (99.3%), and high loading capacity (5.0%). The obtained lupinifolin-loaded nanostructured lipid carriers exhibited prolonged release in a simulated circulatory system but produced a low release in gastrointestinal conditions (3.7%). Intestinal permeability of the nanocarriers was further evaluated in everted intestinal sacs. The results from the ex vivo study indicated that lupinifolin-loaded nanostructured lipid carriers significantly increased the absorption of lupinifolin compared to the native form. In conclusion, lupinifolin-loaded lipid nanocarriers were successfully formulated as delivery systems to enhance its oral bioavailability. Further in vivo experiments are needed to validate the results from this study.

Implications of designing clarithromycin loaded solid lipid nanoparticles on their pharmacokinetics, antibacterial activity and safety

RSC Advances ◽  
2016 ◽  
Vol 6 (80) ◽  
pp. 76621-76631 ◽  
Author(s):  
Manu Sharma ◽  
Namita Gupta ◽  
Sumeet Gupta
Keyword(s):  
Antibacterial Activity ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Half Life ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Short Half Life ◽  
Intracellular Infections

The major obstacles for treatment of intracellular infections with clarithromycin are poor gastrointestinal solubility, short half-life (3–4 h), low oral bioavailability and hepatotoxicity.

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.

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