Microparticles of Sericin-Dextran Conjugate for Improving the Solubility of Antiviral Drug

Abstract

A novel sericin-dextran conjugate (SDC) and self-assembled microparticles has been prepared for improving solubility of atazanavir. Microparticles of SDC were assembled by the reprecipitation method. The size and morphology of SDC microparticles could be adjusted by the concentration and solvents. Low concentration was conducive to the preparation of microspheres. Heterogeneous microspheres could be prepared in ethanol with the range of 85–390 nm, and hollow mesoporous microspheres in propanol with an average particle size of 2.5–22 µm. The aqueous solubility of atazanavir was improved to 2.22 mg/mL in buffer solutions at pH 2.0 and 1.65 mg/mL at pH 7.4 by SDC microspheres. In vitro release of atazanavir from hollow microspheres of SDC exhibited a slower release, had the lowest linear cumulative release in basic buffer (pH 8.0), and the most rapid double exponential diphase kinetic cumulative release in acid buffer (pH 2.0).

Sustainable Silk-Based Particulate Systems for the Controlled Release of Pharmaceuticals and Bioactive Agents in Wound Healing and Skin Regeneration

“…Delivery of antiviral drugs by using soluble SS microparticles was proposed in the investigation carried out by Chen et al [ 99 ]. Antiviral drugs can play a crucial role in the wound-healing process, especially in wounds that are at risk of viral infections or are already infected [ 9 ].…”

“…At pH 8.0, the release of atazanavir was the slowest, with 51.2% of the drug released after 120 h. In contrast, the release rates increased in more acidic environments, with 99.2%, 97.8%, and 94.8% of atazanavir released at pH 7.4, 6.5, and 2.0, respectively, over the same period. This pH-dependent release behavior indicates the microparticles’ potential for targeted drug delivery, leveraging the pH variations within different body compartments to optimize therapeutic effectiveness [ 99 ].…”