Nanocrytals-Mediated Oral Drug Delivery: Enhanced Bioavailability of Amiodarone

Abstract

The aim of this study was to improve the saturation solubility, dissolution profile and oral bioavailability of amiodarone hydrochloride (AMH), a highly lipophilic drug. Stabilizer (Pluronic F-127)-coated AMH nanocrystals (AMH-NCs) were developed by a combination of antisolvent precipitation and homogenization techniques. The optimized formulation comprised pluronic F-127 and AMH at the concentration of 4% and 2% w/v, respectively. The particle size (PS), zeta potential (ZP) and polydispersity index (PDI) of the optimized formulation was found to be 221 ± 1.2 nm, 35.3 mV and 0.333, respectively. The optimized formulation exhibited a rough surface morphology with particles in colloidal dimensions and a significant reduction in crystallinity of the drug. AMH-NCs showed a marked increase in the saturation solubility as well as rapid dissolution rate when compared with the AMH and marketed product. The stability study displayed that the formulation was stable for 3 months, with no significant change in the PS, ZP and PDI. The in vivo pharmacokinetic study demonstrated the ability of AMH-NCs to significantly (p < 0.05) improve the oral bioavailability (2.1-fold) of AMH in comparison with AMH solution, indicating that the production of AMH-NCs using a combination of antisolvent precipitation and homogenization techniques could enhance the bioavailability of the drug.

Preparation and In Vitro Evaluation of Controlled-Release Matrices of Losartan Potassium Using Ethocel Grade 10 and Carbopol 934P NF as Rate-Controlling Polymers

“…Therefore, several losartan potassium sustained-release matrices have been designed, often prepared by the direct compression method by using polymers such as Eudragit RLPO, Eudragit RSPO, and ethylcellulose, either alone or associated with each other, observing an extension of the drug release up to 12 h when using Eudragit polymers in combination with ethylcellulose [ 10 , 11 ], following an anomalous non-Fickian drug release mechanism [ 11 ]. Similarly, other authors devised and prepared losartan potassium sustained release matrix tablets by the direct compression method using Kollidon SR [ 12 ] and methylcellulose [ 13 ] as rate-retarding polymers. Another explored possibility was the preparation of matrix tablets by wet granulation composed of Carbopol 934P and xanthan gum with chitosan, obtaining 99% release of the drug in 24 h [ 14 ].…”

Development and Evaluation of Apocynin Loaded pH-sensitive Nanoparticle Based Hydrogel for the Management of Rheumatoid Arthritis

“…APO-NPs were evaluated by Zetasizer (Malvern Instrument, Worcestershire, UK) for physicochemical properties like PS, PDI and ZP [21].…”

“…There was no observed phase separation and color change in APO-NPs based hydrogel. However, pH of hydrogel was slightly increased, but this increase is not significant whereas drug content was decreased which shows that hydrogel is stable during observed period [57][58][59].…”

Comparative evaluation on the effect of different cavity disinfectant nano gels; Chlorohexidine, Propolis, Liquorice versus Diode Laser in terms of composite microleakage

“…Pharmaceutical scientists use various methods to enhance the dissolution and bioavailability of poorly soluble drugs such as; micronization, self-emulsi cation, salt formation, solid lipid nanoparticles nanocrystallization, and others. 13,14 Awan et al, 2022 14 stated that nanocrystallization enhances solubility and loading of the drug as well as increases its bioavailability.…”