Electrospun formulations of bevacizumab for sustained release in the eye

Abstract

Bevacizumab is a potent protein drug which is highly effective in the treatment of degenerative conditions in the eye. To be effective, frequent injections into the eye are required, which is deeply unpleasant for patients and expensive for healthcare providers. Alternative methods of administration are thus highly sought after. In our work, we use the electrospinning technique to prepare fiber-based formulations loaded with bevacizumab. By careful control of the experimental parameters we are able to stabilize the protein during processing and ensure a constant rate of release over more than two months in vitro. These fibers could thus be used to reduce the frequency of dosing required, reducing cost and improving patient outcomes.

Tunable zero-order drug delivery systems created by modified triaxial electrospinning

“…In the development of new drug delivery systems, much effort has been expended to achieve so-called controlled release (for instance, pulsatile, sustained, bi-phasic or targeted release) of active pharmaceutical ingredients (APIs) [42][43][44][45]. In particular, linear drug release (or zero-order release) is much sought after.…”

Electrospun Fibrous Architectures for Drug Delivery, Tissue Engineering and Cancer Therapy

“…Moreover, the interactions between inner and outer solutions were also reported to affect the release kinetics. Angkawinitwong et al discovered that the pH of core solutions could greatly influence the core‐sheath structure and thus the release kinetics when they incorporated bevacizumab into PCL fibers through co‐axial electrospinning. As shown in Figure a, the positively charged bevacizumab could uncontrollably migrate from the core solution to the PCL sheath solution, resulting in the inhomogeneous distribution of drug in both shell and core section, and thus a first order release up to 18 days.…”

“…a) A diagram illustrating the influence of pH of drug solution on the fiber structure, drug distribution, and release kinetics when produced through co‐axial electrospinning. Reproduced with permission . Copyright 2017, Elsevier B.V. b) Thermal responsive fibers using shell‐located nanogels as valve were fabricated through co‐axial electrospinning.…”

“…Drug release using an in vitro eye model showed that the drug residence time (half‐life) was extended to 6 days, which was much greater than the small molecule drug solutions, suggesting that the proposed matrices can be a viable option as intravitreal implant. Angkawinitwong et al encapsulated bevacizumab, a VEGF neutralizing antibody, into the core area in PCL fibers through co‐axial electrospinning to treat age related macular degeneration. This fibrous solid formulation highly prolonged the drug release period over two months, and therefore, reduced the administration frequency and avoided the invasive injection in the eyes.…”

Nanoparticles in an antibiotic-loaded nanomesh for drug delivery

“…38,39 However, it has been shown that in core-shell electrospinning, positively charged drugs are found to migrate to the surface of the bres compared to neutral drugs which remain in the core. 40 This is due to the charge generation of the surface of the polymer during electrospinning. The positively charged drugs are repelled from the inner needle surface and are drawn toward the grounded collector plate.…”