Fast-Disintegrating Nanofibrous Web of Pullulan/Griseofulvin-Cyclodextrin Inclusion Complexes.

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery

Background:

• Griseofulvin (GSF) is a widely used antifungal agent with poor water solubility and limited bioavailability.
• Cyclodextrin derivatives, such as hydroxypropyl-beta-cyclodextrin (HPβCD), are known to improve the solubility of poorly soluble drugs.

Purpose of the Study:

• To develop a novel drug delivery system for griseofulvin (GSF) using pullulan nanofibers (NFs) incorporating GSF-HPβCD inclusion complexes (ICs).
• To enhance the physicochemical properties and oral bioavailability of GSF.

Main Methods:

• Molecular modeling was used to predict optimal stoichiometry for GSF-HPβCD inclusion complex formation.
• Griseofulvin-HPβCD inclusion complexes (ICs) were prepared at a 1:2 molar ratio (GSF:HPβCD).
• Pullulan (PULL) nanofibers (NFs) containing the GSF-HPβCD-ICs were fabricated using electrospinning.

Main Results:

• Defect-free pullulan/GSF-HPβCD-IC nanofibers with an average diameter of 805 ± 180 nm were successfully produced.
• The PULL/GSF-HPβCD-IC NFs exhibited a high drug loading efficiency of ~98% (~6.4% w/w drug content), significantly higher than control PULL/GSF NFs (~72% loading, ~4.7% w/w).
• The PULL/GSF-HPβCD-IC NFs demonstrated enhanced aqueous solubility and a ~2.5 times faster drug release profile compared to PULL/GSF NFs, attributed to the inclusion complexation.

Conclusions:

• The developed pullulan/GSF-HPβCD-IC nanofibers represent a promising fast-disintegrating oral dosage formulation for griseofulvin.
• This formulation improves the physicochemical properties of GSF, enhancing its potential for effective oral antifungal therapy.