Nanoemulsion-Based Orodispersible Film Formulation of Guava Leaf Oil for Inhibition of Oral Cancer Cells.

Among natural sources, guava leaf oil (GLO) has emerged as a potential anticancer agent. However, its limited water solubility poses a significant challenge for its use. Oil-in-water nanoemulsions are used to address the limitation of water solubility of GLO prior to its incorporation into orodipersible films. Nanoemulsions containing GLO:virgin coconut oil (VCO) at a ratio of 50:50 to 70:30 presented a small droplet size of approximately 50 nm and a relatively low zeta potential. GLO:VCO at a ratio of 70:30 was selected for incorporation into sodium alginate film at various concentrations ranging from 1% to 30% w/w. Tensile strength and elongation at break relied on the concentration of nanoemulsions as well as the internal structure of films. Fourier transform infrared spectroscopy revealed that GLO was compatible with sodium alginate. Film containing 2% w/w of nanoemulsions (2G_ODF) exhibited effective in vitro antioral cancer activity, with an IC50 of 62.49 ± 6.22 mg/mL; furthermore, its anticancer activity showed no significant difference after storage at 25 °C for 1 year. Moreover, 2G_ODF at IC60 arrested colony formation and cell invasion. There is also evidence that cell death occurred via apoptosis, as indicated by nuclear fragmentation and positive Annexin-V staining. These findings highlight the potential of orodispersible films containing GLO nanoemulsions as a prospective oral anticancer agent.

Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles.

Vancomycin hydrochloride (HCl) is a glycopeptide antibiotic used to treat serious or life-threatening infections, and it reduces plaque scores and gingivitis in periodontal patients. In this study, vancomycin HCl was incorporated into rosin in situ forming gel (ISG) and rosin in situ forming microparticles (ISM) to generate a local drug delivery system to treat periodontal disease. The physical properties of the ISG and ISM were measured, including pH, viscosity, injectability, adhesion properties, in-vitro transformation, and drug release. Moreover, the effectiveness of antimicrobial activity was tested using the agar-cup diffusion method against Staphylococcus aureus, Streptococcus mutans, Porphyromonas gingivalis, and Escherichia coli. Vancomycin HCl-loaded rosin-based ISG and ISM had a pH value in the range of 5.02−6.48 and exhibited the ease of injection with an injection force of less than 20 N. Additionally, the lubricity effect of the external oil phase of ISM promoted less work of injection than ISG and 40−60% rosin-based ISM showed good emulsion stability. The droplet size of emulsions containing 40%, 50%, and 60% rosin was 98.48 ± 16.11, 125.55 ± 4.75, and 137.80 ± 16.8 µm, respectively. Their obtained microparticles were significantly smaller in diameter, 78.63 ± 12.97, 93.81 ± 10.53, and 118.32 ± 15.61 µm, respectively, because the particles shrank due to the solvent loss from solvent exchange. Moreover, increasing the concentration of rosin increased the size of microparticles. After phase transformation, all formulations had better plasticity properties than elasticity; therefore, they could easily adapt to the specific shape of a patient's gum cavity. Both developed ISG and ISM presented inhibition zones against S. mutans and P. gingivalis, with ISG presenting significantly more effectively against these two microbes (p < 0.05). The vancomycin HCl-loaded rosin ISG and ISM delayed drug release for 7 days with efficient antimicrobial activities; thus, they exhibit potential as the drug delivery systems for periodontitis treatment.

Borneol-based antisolvent-induced in situ forming matrix for crevicular pocket delivery of vancomycin hydrochloride.

Given its safety and apparent low aqueous solubility, borneol may serve as a matrix forming component of anti-solvent based in situ forming matrixes (ISMs) for crevicular pocket targeting. Drug-free and vancomycin hydrochloride-loaded borneol ISMs were evaluated for pH, density, viscosity, contact angle, surface tension, matrix formation, drug release behavior, in vitro degradability and antimicrobial activities. Density and pH values of borneol-based ISMs decreased with increasing borneol concentration. Given their markedly low viscosity could facilitate better injectability. The contact angles of the drug-free and vancomycin HCl-loaded borneol ISMs increased after being in contact with the agarose gel or the bulge tissue of porcine due to phase inversion. A dense borneol crystal matrix formed after using the highly concentrated ISM corresponded to fast matrix formation. The borneol-based ISM exhibited a sustainable drug release longer than 14 days with a diffusion-controlled release mechanism. Moreover, the developed ISM exhibited strong antimicrobial activities against various microbes. Thus, the vancomycin HCl-loaded borneol-based ISM is a potentially effective local anti-solvent-based ISM for periodontitis treatment via crevicular pocket injection.