Galactose decorated PLGA nanoparticles for hepatic delivery of acyclovir

Abstract

The present study explores prospective of surface tailored nanoparticles for targeted delivery of acyclovir along with the interception of minimal side effects. Acyclovir loaded plain and galactosylated poly lectic co glycolic acid (PLGA) nanoparticles were efficiently prepared and characterized by Fourier transform infrared spectroscopy, scanning electron microscopy (SEM), size, polydispersity index, zeta potential, and entrapment efficiency. The formulations were evaluated for in vitro drug release and hemolysis. Further, biodistribution study and fluorescent microscopic studies were carried out to determine the targeting potential of formulations. SEM revealed smooth morphology and spherical shape of the nanoparticles. In vitro, the galactosylated nanoparticles were found to be least hemolytic and exhibited a sustained release pattern. In vivo studies exhibited an augmented bioavailability, increased residence time and enhanced delivery of acyclovir to the liver upon galactosylation. It may therefore be concluded that galactose conjugated PLGA nanoparticles can be used suitably as vehicles for delivery of bioactives specifically to the hepatic tissues and may be thus exploited in the effective management of various liver disorders.

Formulation and evaluation of tacrolimus-loaded galactosylated Poly(lactic-co-glycolic acid) nanoparticles for liver targeting

“…Biodistribution studies were performed to assess the targeting ability of galactosylated nanoparticles to deliver tacrolimus to the hepatic tissues. The concentration of tacrolimus in liver was significantly higher in nanoparticle formulations than plain drug, which may be due to uptake of nanoparticles by mono‐nuclear phagocytic system [11]. However, the concentration in nanoparticles was significantly less than galactosylated PLGA nanoparticles ( P < 0.05) that might be due to non‐specific entry in the absence of specific receptors.…”

“…The concentration of tacrolimus in liver was significantly higher in nanoparticle formulations than plain drug, which may be due to uptake of nanoparticles by mono-nuclear phagocytic system. [11] However, the concentration in nanoparticles was significantly less than galactosylated PLGA nanoparticles (P < 0.05) that might be due to non-specific entry in the absence of specific receptors. At 24 h, there was an increase in tacrolimus concentration from Tac-Gal-PLGA NPs by 4.83 fold and 11.72 fold from Tac-PLGA NPs and plain drug solution respectively.…”

“…Blood samples of 0.5 ml were collected from retro‐orbital plexus of rats at 0 h, 1 h, 3 h, 8 h, 24 h time intervals in 2 ml preheparinized tubes. The samples were centrifuged at 5000 rpm for 10 min at 4°C to separate red blood cells and supernatant plasma was collected [11]. Plasma of 0.2 ml was treated with 0.6 ml methanol: 2% zinc sulphate in water (80:20) (protein precipitating agent),[19] vortexed for 10 min and then centrifuged at 9000 rpm for 10 min at 4°C.…”

“…The samples were centrifuged at 5000 rpm for 10 min at 4°C to separate red blood cells and supernatant plasma was collected. [11] Plasma of 0.2 ml was treated with 0.6 ml methanol: 2% zinc sulphate in water (80:20) (protein precipitating agent), [19] vortexed for 10 min and then centrifuged at 9000 rpm for 10 min at 4°C. The supernatant was collected, filtered through 0.22μ filter and the filtrate was injected into LC-MS to analyse tacrolimus concentration.…”

Nanomedicine-Based Neuroprotective Strategies in Patient Specific-iPSC and Personalized Medicine

“…Additionally, it protects the drug molecule from degradation and exhibits sustained release [36]. Most importantly, PLGA-based NPs are able to target particles to specific organs or cells [37,38], and have been widely used as drug delivery systems for the treatment of different pathologies. A large number of studies have demonstrated applications of PLGA-based delivery nanosystems in vaccination [39,40], cancer treatment [41,42], inflammation [43], and regenerative medicine [44].…”