Acyclovir-Polyethylene Glycol 6000 Binary Dispersions: Mechanistic Insights

Abstract

The dissolution and subsequent oral bioavailability of acyclovir (ACY) is limited by its poor aqueous solubility. An attempt has been made in this work to provide mechanistic insights into the solubility enhancement and dissolution of ACY by using the water-soluble carrier polyethylene glycol 6000 (PEG6000). Solid dispersions with varying ratios of the drug (ACY) and carrier (PEG6000) were prepared and evaluated by phase solubility, in vitro release studies, kinetic analysis, in situ perfusion, and in vitro permeation studies. Solid state characterization was done by powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analysis, and surface morphology was assessed by polarizing microscopic image analysis, scanning electron microscopy, atomic force microscopy, and nuclear magnetic resonance analysis. Thermodynamic parameters indicated the solubilization effect of the carrier. The aqueous solubility and dissolution of ACY was found to be higher in all samples. The findings of XRD, DSC, FTIR and NMR analysis confirmed the formation of solid solution, crystallinity reduction, and the absence of interaction between the drug and carrier. SEM and AFM analysis reports ratified the particle size reduction and change in the surface morphology in samples. The permeation coefficient and amount of ACY diffused were higher in samples in comparison to pure ACY. Stability was found to be higher in dispersions. The results suggest that the study findings provided clear mechanical insights into the solubility and dissolution enhancement of ACY in PEG6000, and such findings could lay the platform for resolving the poor aqueous solubility issues in formulation development.

Improved Hygroscopicity and Bioavailability of Solid Dispersion of Red Ginseng Extract with Silicon Dioxide

“…The hydrophilic carriers were selected on the basis of their high dispersibility, increased solubility, and low hygroscopicity [ 11 ]. Saccharides (i.e., mannitol, sucrose, lactose, and trehalose), cellulose derivatives (i.e., HPC), polymers (i.e., PVP, and cross-linked PVP (PVPc)), and polyethylene glycols (i.e., P1500 and P6000) [ 11 , 27 , 28 , 29 , 30 ] were used in the preparation of solid dispersion formulations of RGE with low hygroscopicity and increased oral permeability. We began by determining the ginsenoside content in the solid dispersion formulations of RGE and whether the solid dispersion formulation process modified the ginsenoside content.…”