Evaluation of carvedilol-loaded Eudragit® nanoparticles

Abstract

The objective of present study was to prepare positively charged carvedilol-loaded nanoparticles providing a controlled release formulation by spray dryer technique and was to examine the effect of different derivative of Eudragit ® polymers on entrapment efficiency (EE%), dissolution profile and release kinetics. Two nonbiodegradable positively charged polymers, Eudragit ® RS100 and RL100 were used alone or in combination. The prepared formulations were evaluated for their particle size, polydispersity index, zeta potential, in vitro dissolution and in vitro release kinetics study. Particle sizes of placebo nanoparticles and carvedilol loaded nanoparticles were 418.2±18.5/ 402.3±22.0/ 416.3±12.5 and 535.5±13.8/ 529.4±10.2/ 530.4±10.4 nm, respectively with PDI values of approximately 0.4-0.6 for each. Carvedilol loading was resulted in positive electrical charge on nanoparticles. The drug encapsulation efficiency was 68.45±4.67/ 63.58±2.30/ 65.67±4.21. In vitro cumulative release from the nanoparticles was 80-90 % at 48 hour. Morphology and solid state analyzes were performed also in nanoparticles. The results of this research indicate that spray dryer technique is suitable for carvedilol loaded Eudragit ® nanoparticles and no burst effect but a prolonged drug release was observed from formulations.

The Exploitation of pH-Responsive Eudragit-Coated Mesoporous Silica Nanostructures in the Repurposing of Terbinafine Hydrochloride for Targeted Colon Cancer Inhibition: Design Optimization, In Vitro Characterization, and Cytotoxicity Assessment

“…In addition, TER was released from the coated formulas in a controlled manner, taking around 24 h to complete. The controllable release of TER might be attributable to the presence of the second layer of Eud RL-100, which demonstrated a sustained release of TER with no burst effect [ 40 ]. The hydrophobic property of the Eud RL-100 coat minimized the water penetration into the matrix, delaying the TER release process where the molecules diffused through the polymer coating and were then released slowly into the dissolving medium [ 41 ].…”

Brain Targeted Delivery of Levetiracetam Loaded Nanosphere

“…The results of gelation temperatures of all in situ gel formulation showed in table (4). The temperature of gel formation was observed between (28.6°C ± 0.51 and 34°C ± 0.6) for the batches (NG1 to NG6).…”

“…A solution of 100 µg/mL of levetiracetam (LEV) in Phosphate Buffer Solution (PBS) (pH 6.4) was prepared as stock solution. Aliquots of 0.2, 0.4, 0.6, 0.8, 1, 1.2, 1.4, 1.6, 1.8, 2, 2.2, 2.4, 2.6 and 2.8 mL were separately put in a suitable measuring flask (10 mL) then diluted with PBS (pH 6.4) to produce a concentration of 2,4,6,8,10,12,14,16,18,20,22, 24, 26 and 28 µg/mL, respectively. The absorbance was measured spectrophotometrically at the predetermined λmax (210 nm) using PBS (pH 6.4) as a blank 13 .…”

Formulation and Evaluation of Baclofen Polymeric Nanoparticles for Transdermal Delivery In-vitro and Ex-vivo Optimization

“…RE is more accurate as it reflects both the rate and the extent of drug release. The slow release of the drug from the NPs is due to the strong ionic interaction between baclofen and ERL 30 . This explained why RE of formula B9 (6% ERL) was significantly (P<0.001) lower than both formulae B3 (2% ERL) and B6 (4%ERL).…”