Development, optimization and characterization of glycyrrhetinic acid–chitosan nanoparticles of atorvastatin for liver targeting

Abstract

Glycyrrhetinic acid-modified chitosan (mGA-suc-CTS) is used as liver-targeted carrier for drug delivery. In this study, nanoparticles were prepared by ionic gelation process, and glycyrrhetinic acid act as the targeting ligand. The structure of the product was confirmed by IR and NMR techniques. The main aim of this study was to deliver atorvastatin directly to the liver by using same conjugate and reduce the associated side-effects, i.e. hepatotoxicity at high dose. Characterization of the developed formulation was performed by differential scanning calorimetry, particle size measurements and cellular uptake studies. Release profile, pharmacokinetics studies and organ distribution studies showed that developed formulation shows a relative higher liver uptake. The optimized formulation showed increased plasma concentration than the CTS nanoparticles as well as plain drug and the accumulation in the liver was nearly 2.59 times more than that of obtained with the CTS nanoparticles. Pharmaceutical and pharmacological indicators suggested that the proposed strategy can be successfully utilized for liver targeting of therapeutics.

Biochemical and histopathological assessment of atorvastatin-loaded nanoemulsion effectiveness in Rats

“…20 The particle sizes of ATV-LNE ranged from 38.12±6.71 to 119.2±16.17nm which was similar to the results observed by Kumar who reported the particle size of ATV loaded solid lipid nanoparticles was ranged from 50.0±4.12 to 125.1±6.12 nm. 21 The particle size of 20% ATV-LNE has the smallest size with z-average diameter of 38.12±6.71nm and has the largest zeta negative potential of -26.8±4.16mV.…”

“…23 this was in agreement with Rohilla et al who found the PDI of ATV loaded in glycyrrhetinic acid-chitosan nanoparticles was 0.126. 20 When investigating the lipid profile, it was noticed that the cholesterol and LDL levels were decreased in all treated groups slightly. 20% ATV-LNE and Blank-NE groups have the least level of CHO and LDL compared to the control group.…”

Liver-targeting self-assembled hyaluronic acid-glycyrrhetinic acid micelles enhance hepato-protective effect of silybin after oral administration

“…The difference between HA-adh-DOCA 10 and HAadh-GA 20 micelles was ascribed to the different hydrophobic moiety. Studies have described that GA-modified drug delivery systems accumulated particularly in the rat liver and maintained at a high level, because of the abundant receptors for GA on hepatocyte membranes Rohilla et al, 2014). In this study, although most of the hydrophobic GA molecules were embedded in the inner core of micelles, some GA molecules were still present on the surface of HA-adh-GA 20 micelles, serving as liver-targeting ligands.…”

Archaeosomes: an excellent carrier for drug and cell delivery

“…The risk of transmission of the disease is high because the infection has been detected in nonendemic areas of the Americas and Europe due to largescale migrations. It is essential to develop new strategies for the prevention and control of Chagas disease (Rohilla et al, 2014a). At present, vaccines and immune therapies targeted at T. cruzi infection are practically nonexistent.…”