Mechanistic insights into acyclovir-polyethylene glycol 20000 binary dispersions

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Acyclovir (ACY) exhibits poor aqueous solubility, limiting its therapeutic efficacy.
• Developing strategies to enhance ACY solubility and dissolution is crucial for improving oral bioavailability.

Purpose of the Study:

• To elucidate the mechanism behind solubility and dissolution enhancement of acyclovir (ACY) using polyethylene glycol 20000 (PEG20000).
• To evaluate the impact of PEG20000 on ACY's solid-state properties and in vitro performance.

Main Methods:

• Preparation of acyclovir-PEG20000 solid dispersions at various ratios.
• Characterization using phase solubility, in vitro release, kinetic analysis, in situ perfusion, and in vitro permeation studies.
• Solid-state analysis via PXRD, DSC, FT-IR, PMI, SEM, AFM, and NMR.

Main Results:

• PEG20000 significantly increased acyclovir's aqueous solubility and dissolution rate.
• Solid dispersions formed solid solutions with reduced crystallinity and no drug-carrier interactions.
• Enhanced drug permeation and stability were observed in the solid dispersions.

Conclusions:

• The study provides mechanistic insights into how PEG20000 enhances acyclovir solubility and dissolution.
• This solid dispersion approach offers a promising platform for improving the delivery of other poorly water-soluble drugs.