Elucidation of intestinal absorption mechanism of carvedilol-loaded solid lipid nanoparticles using Caco-2 cell line as an in-vitro model

  title={Elucidation of intestinal absorption mechanism of carvedilol-loaded solid lipid nanoparticles using Caco-2 cell line as an in-vitro model},
  author={Mansi K. Shah and Parshotam L. Madan and Senshang Lin},
  journal={Pharmaceutical Development and Technology},
  pages={877 - 885}
Abstract Enhanced oral bioavailability of poorly aqueous soluble drugs encapsulated in solid lipid nanoparticles (SLNs) via lymphatic delivery has been documented. Since no in-vitro lymphoid tissue is currently available, human excised Caco-2 cell monolayer could be alternative tissue for development of an in-vitro model to be used as a screening tool before animal studies are undertaken. Therefore, optimized carvedilol-loaded SLNs (FOPT-SLNs) were prepared, characterized, and evaluated using… 

Fabrication of solid lipid nanoparticles of lurasidone HCl for oral delivery: optimization, in vitro characterization, cell line studies and in vivo efficacy in schizophrenia

It was concluded that oral administration of LH-SLNs in rats improved the bioavailability of LH via lymphatic uptake along with improved therapeutic effect in MK-801 induced schizophrenia model in rats.

Enhanced intestinal absorption of asenapine maleate by fabricating solid lipid nanoparticles using TPGS: elucidation of transport mechanism, permeability across Caco-2 cell line and in vivo pharmacokinetic studies

Effectiveness of SLNs are demonstrated to improve therapeutic efficacy of AM in the treatment of schizophrenia by demonstrating non-toxicity of the carriers and drug.

Self microemulsifying drug delivery system of lurasidone hydrochloride for enhanced oral bioavailability by lymphatic targeting: In vitro, Caco-2 cell line and in vivo evaluation.

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  • Biology, Chemistry
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2019

Improved uptake and bioavailability of cinnamaldehyde via solid lipid nanoparticles for oral delivery.

CA-SLNs improved the absorption across Caco-2 cell model and improved the oral administration bioavailability of CA in rats, and were taken up by an energy-dependent, endocytic mechanism mediated by caveolae mediated endocytosis across Cco-2 cells.

Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles

Gal-BSA NPs could improve the intestinal absorption capacity and oral bioavailability of curcumin through the double absorption mechanisms of the clathrin-mediated endocytosis and the passive transport.

Development and In Vitro Characterization of Paclitaxel Loaded Solid Lipid Nanoparticles

In vitro release studies showed a sustained release profile for PSLN over a period of 48 hours, and SLNs loaded with PTX were found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.

Improved brain delivery of pueraria flavones via intranasal administration of borneol-modified solid lipid nanoparticles.

PTF-Bo-SA-SLNs are a promising therapeutic carrier for brain disease after intranasal administration and their brain delivery effects were evaluated in vitro and in vivo.

Rosuvastatin calcium-loaded Solid Lipid Nanoparticles (SLN) using design of experiment approach for oral delivery

Quality-by-design approach was used to develop the Rosuvastatin Calcium (Rst)-loaded solid lipid nanoparticles (SLN) and it was observed that interplay of formulation variables had significant effect on particle size, %EE and In vitro release.



Preparation, in vitro evaluation and statistical optimization of carvedilol-loaded solid lipid nanoparticles for lymphatic absorption via oral administration

Higher carvedilol uptake from SLNs compared to drug solution in the Caco-2 cell line exhibited a potential prolonged drug release and upon cellular uptake, SLNs could then enter the lymphatic system which will avoid first pass metabolism and hence higher oral bioavailability.

Improvement of digoxin oral absorption in rabbits by incorporation into solid lipid nanoparticles.

Results indicate that DG absorption is enhanced significantly by employing SLN formulations and SLNs are a potential as an oral delivery carrier for poorly water soluble drugs.

Preparation and in vitro, in vivo evaluations of norfloxacin-loaded solid lipid nanopartices for oral delivery

NFX-SLN resulted in significantly higher plasma drug concentration than native NFX and increased the relative bioavailability of NFX by 12 folds, prolonged the plasma drug level above the average minimum inhibition concentration from 14 to 168 h.

Body Distribution of Camptothecin Solid Lipid Nanoparticles After Oral Administration

SLN could be a promising sustained release and targeting system for camptothecin or other lipophilic antitumor drugs after oral administration and show significant changes in body distribution through incorporation into solid lipid nanoparticles by peroral route.

Localization and quantification of biodegradable particles in an intestinal cell model: the influence of particle size.

  • M. GaumetR. GurnyF. Delie
  • Materials Science, Biology
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2009

Effect of poloxamer 188 on lymphatic uptake of carvedilol-loaded solid lipid nanoparticles for bioavailability enhancement

Findings augur well with the possibility of enhancement of the oral bioavailability of drug, via the lymphatic system bypassing hepatic first pass metabolism, via a combination of particle size as well as reduction in hydrophobicity of SLNs.

Formulation and optimization of solid lipid nanoparticles of buspirone HCl for enhancement of its oral bioavailability

It was found that the relative bioavailability of the drug in SLNs was significantly increased, compared to that of theDrug solution, and the percentage of drug entrapment, mean particle-size diameter, and zeta potential were studied as the responses.

In vitro assessment of oral lipid based formulations.

Lipid--an emerging platform for oral delivery of drugs with poor bioavailability.