A novel ophthalmic delivery system utilizing levofloxacin-loaded, preservative-free, nanofiber-based inserts was investigated. Polyvinyl alcohol (PVA) and Poloxamer 407 (Polox)were employed as matrix materials, while hydroxypropyl-beta-cyclodextrin (HP-β-CD) was a solubilizer. The formulations were prepared via electrospinning and characterized for fiber morphology, drug dissolution, cytotoxicity, and antimicrobial activity. Scanning electron microscopy confirmed uniform fibrous structures. Fourier Transform Infrared spectroscopy and X-ray diffraction analyses demonstrated the amorphous state of levofloxacin within the fibers. In vitro dissolution studies revealed a rapid (within 2 min) and complete drug release, with higher HP-β-CD levels slightly delaying the release. Cytotoxicity tests showed increased HP-β-CD concentrations induced irritation, that was mitigated by sodium hyaluronate. The antimicrobial efficacy of the nanofibers was comparable to conventional eye drops, with lower minimum inhibitory concentrations for most tested strains. The nanofibrous formulation prepared from a PVA–Polox-based viscous solution of the drug:CD 1:1 mol ratio, containing 0.4% (w/w) sodium hyaluronate) was identified as a particularly promising alternative formulation due to its rapid and complete dissolution, good biocompatibility, and effective antimicrobial properties. Its gelling properties indicate that the residence time on the eye surface can be increased, potentially reducing discomfort and enhancing therapeutic outcomes. The nanofibrous formulations enhanced antimicrobial efficacy, providing a preservative-free alternative that minimizes the potential eye irritation that might occur because of the preservative agent and reduces the administrated dose frequency by extending the drug’s retention time on the eye’s surface. Subsequently, it improves patients’ adherence, which would reflect positively on the bioavailability. The levofloxacin-HP-β-CD nanofibers demonstrate promise as an alternative to traditional eye drops, offering advantages in solubility, stability, and patient compliance for ocular infection treatment.

Background/Objectives: Fungal keratitis remains a vision-threatening infection, and current amphotericin B (AmphB) eye drops suffer from low corneal residence time, poor aqueous solubility, and the need for frequent dosing. This study develops electrospun nanofiber-based ophthalmic inserts combining polyvinyl alcohol (PVA), gamma-cyclodextrin (γ-CD), and sodium taurocholate (STC) to enhance AmphB solubility and provide a non-invasive, rapidly dissolving ophthalmic dosage form. Methods: γ-CD and STC-enhanced AmphB-loaded PVA nanofiber-based ophthalmic inserts with varying γ-CD and STC concentrations were prepared by electrospinning and characterized by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Drug content, in vitro release (Weibull modeling), antifungal activity against Candida albicans, Fusarium solani, and Aspergillus fumigatus, ocular cytocompatibility using the Hen’s Egg Test on Chorioallantoic Membrane (HET-CAM), and accelerated stability (40 ± 2 °C, 75 ± 5% relative humidity, 4 weeks) were evaluated. Results: Bead-free nanofibers with mean diameters between 216 ± 33 nm and 310 ± 35 nm were obtained, and XRD confirmed complete amorphization of AmphB within the PVA nanofiber matrix, forming an amorphous solid dispersion. All formulations showed rapid and nearly complete AmphB release (≈100% within 60 min), with Weibull β values < 0.75, indicating Fickian diffusion-controlled release. AmphB-loaded PVA nanofiber-based ophthalmic inserts produced inhibition zones and broth susceptibility profiles comparable to AmphB in dimethyl sulfoxide (DMSO), demonstrating preserved antifungal activity. HET-CAM scores (0–0.9) classified the inserts as practically non-irritant, and SEM/FTIR after accelerated storage showed no relevant morphological or physicochemical changes. Conclusions: These γ-CD and STC-enhanced AmphB-loaded PVA nanofiber-based ophthalmic inserts provide a non-invasive, rapidly dissolving ophthalmic dosage form that combines amorphous AmphB, immediate drug availability, and good ocular tolerance, supporting their further development as a patient-friendly treatment option for fungal keratitis.

Background/Objectives: The melt-spinning process has seen limited application in the pharmaceutical industry. However, nano- and microfibrous structures show significant potential for novel drug delivery systems, due to their high specific surface area. To facilitate broader adoption in pharmaceutical technology, critical parameters influencing fiber quality and yield must be investigated. In this study, we aimed to develop an isomalt-based microfibrous carrier system for active pharmaceutical ingredients. Methods: The effects of different isomalt compositions—specifically, varying ratios of GPS (6-O-α-d-glucopyranosyl-d-sorbitol) and GPM (1-O-α-d-glucopyranosyl-d-mannitol)—as well as key process parameters, were systematically investigated to optimize fiber formation. The prepared fibers underwent different treatments. Morphological changes were monitored with a microscope, and microstructural changes were studied using a differential scanning calorimeter and X-ray diffractometer. The macroscopic behavior of the fibers was evaluated by image analysis under monitored conditions. Results: Statistical analysis was used to determine the optimal setting to produce isomalt-based fibers. We found that storage over ethanol vapor has a positive effect on the stability of the fibers. We successfully prepared ibuprofen sodium-containing fibers that remained stable after alcohol treatment and enabled drug release within 15 s. Conclusions: It was found that the applied GPS:GPM isomalt ratio significantly influenced fiber formation and that storage over ethanol positively influenced the processability and stability of the fibrous structure. An isomalt-based microfibrous system with advantageous physicochemical and structural properties was successfully developed as a potential drug carrier. The system is also resistant to the destructive effects of ambient humidity, enabling preparation of suitable dosage forms.

Background/Objectives: To improve the potential therapeutic efficacy of albendazole (ABZ), its low solubility in alkaline environments should be addressed. Spray drying has been widely applied to increase the solubility of poorly soluble drugs. Eudragit^® E PO (EudE) has previously been used to increase the solubility of weakly basic drugs, alone and in combination with organic acids. In the present work, we aimed to demonstrate that EudE and tartaric acid (TA) significantly increase the solubility of ABZ via spray drying. Furthermore, a colon-delivery formulation was applied to deliver ABZ at pH 7.2. Methods: This study developed spray-dried formulations of ABZ-TA-EudE. The formulation with the best solubility profile was selected and loaded into the EUDRACAP^® colon to achieve colon-delivery of the ABZ formulation with enhanced solubility at basic pH. The physicochemical characteristics and in vitro drug release were evaluated and compared with those of the respective physical mixtures. Results: The addition of TA further enhanced the solubility of ABZ-EudE formulations. Both EudE and TA significantly increase ABZ solubility. The ternary ABZ-TA-EudE formulation with the best solubility, when delivered into the EUDRACAP^® colon, showed enhanced ABZ release at pH 7.2. Enhanced in vitro drug release at basic pH and physicochemical characteristics were observed for the spray-dried formulation of ABZ-TA-EudE compared with the corresponding physical mixture and the ABZ powder. Conclusions: TA and EudE significantly enhance the solubility of the weakly basic drug, ABZ, in a spray-dried formulation. Furthermore, the application of EUDRACAP^® colon is effective for colon-delivery of ABZ, as it ensures ABZ release at pH 7.2, thereby providing enhanced formulation’s solubility at its site of action.