PLGA Biodegradable Nanoparticles Containing Perphenazine or Chlorpromazine Hydrochloride: Effect of Formulation and Release

Abstract

In our study, poly(dl-lactide-co-glycolide) (PLGA) nanoparticles loaded with perphenazine (PPH) and chlorpromazine hydrochloride (CPZ-HCl) were formulated by emulsion solvent evaporation technique. The effect of various processing variables, including PLGA concentration, theoretical drug loading, poly(vinyl alcohol) (PVA) concentration and the power of sonication were assessed systematically to obtain higher encapsulation efficiency and to minimize the nanoparticles size. By the optimization formulation process, the nanoparticles were obtained in submicron size from 325.5 ± 32.4 to 374.3 ± 10.1 nm for nanoparticles loaded with PPH and CPZ-HCl, respectively. Nanoparticles observed by scanning electron microscopy (SEM) presented smooth surface and spherical shape. The encapsulation efficiency of nanoparticles loaded with PPH and CPZ-HCl were 83.9% and 71.0%, respectively. The drug loading were 51.1% and 39.4% for PPH and CPZ-HCl, respectively. Lyophilized nanoparticles with different PLGA concentration 0.8%, 1.3% and 1.6% (w/v) in formulation process were evaluated for in vitro release in phosphate buffered saline (pH = 7.4) by using dialysis bags. The release profile for both drugs have shown that the rate of PPH and CPZ-HCl release were dependent on a size and amount of drugs in the nanoparticles.

Polymeric Nanoparticles for Improved Bioavailability of Cilnidipine

“…In our study, we observed decrease in PDI with high concentration of PVA (trial 1, 7) which is also reported by Hylayqa [12] where high concentration of PVA showed decrease in PDI values for the same amount of PLGA, but the effect in our case is due to high volume of organic solvent used which assured the complete solubility of the polymer. …”

“…An increase in the mean particle size was observed when increasing concentration of PLGA was used for all the amount of PVA in the formulation (1-3%). It was reported that an increase in the amount of PVA in the formulation may lead to the smaller particle size due to tight surface that is formed from PVA macromolecular chains at high concentration [12].…”

Development and characterisation of disulfiram-loaded PLGA nanoparticles for the treatment of non-small cell lung cancer

“…This is due to the size of the nanoparticles decreasing with an increase in PVA loading ( Figure 2A). The smaller the size of the nanoparticles the less DSF they can encapsulate and thus the lower the encapsulation efficiency [59]. Furthermore, increasing the loading of PVA increases the concentration of residual PVA [60], which binds to the DSF limiting it's encapsulation in the PLGA [61].…”

Interaction of Solid Lipid Nanoparticles and Specific Proteins of the Corona Studied by Surface Plasmon Resonance

“…The polydispersity index of the obtained nanoparticles ranged between 0.14 and 0.23, verifying in all cases the small polydispersity of the SLN solutions. It is well known that size influences both cell uptake and drug release kinetics in nanoparticles and other particulate systems [31][32][33]. Accordingly, it is desirable to attain low polydispersity since this is expected to result in a more predictable and homogeneous behavior within the targeted biological system.…”