Design and In Vitro Evaluation of a Slow-Release Intraocular Implant of Betamethasone

AAPS PharmSciTech. 2021 Jun 10;22(5):174. doi: 10.1208/s12249-021-02048-0.

Abstract

Posterior eye diseases are a common cause of vision problems in developing countries, which have encouraged the development of new treatment models for these degenerative diseases. Intraocular implants are one of the drug delivery systems to the posterior region of the eye. Using these implants, the blood-eye barrier can be bypassed; the complications caused by repeated in vitro administrations can be eliminated, and smaller amounts of the drug would be used during the treatment process. Meanwhile, biodegradable implants have received more attention due to their biodegradable structure and the lack of need for re-surgery to remove the rest of the system from the eye. The aim of this study is to employ biodegradable implants composed of polyethylene glycol (PEG) and 3-hydroxybutyrate-co-3-hydroxyvalerat (PHBV) to deliver betamethasone to the back of the eye in the treatment of retinopathy. PHBV polymer has been selected as the main polymer with a certain ratio of drug to polymer for fabrication of enamel and different amounts of PEG with three molecular weights used as pore generators to control drug release over a period of time. Based on the analysis of the results of differential scanning calorimetry (DSC) and FTIR spectroscopy, none of the polymers were degraded in the temperature range of the manufacturing process, and among betamethasone derivatives, the best option for implant preparation is the use of its basic form. Drug release studies over a period of three months showed that implants containing PHBV HV2% and PEG 6000 had a more appropriate release profile.

Keywords: PEG; PHBV; betamethasone; biodegradable; ophthalmic drugs; ophthalmic implants; retinopathy.

MeSH terms

  • Absorbable Implants*
  • Anti-Inflammatory Agents / chemical synthesis
  • Anti-Inflammatory Agents / pharmacokinetics
  • Betamethasone / analogs & derivatives
  • Betamethasone / chemical synthesis
  • Betamethasone / pharmacokinetics*
  • Delayed-Action Preparations / chemical synthesis
  • Delayed-Action Preparations / pharmacokinetics
  • Drug Design*
  • Drug Implants
  • Drug Liberation
  • Polyesters / chemical synthesis
  • Polyesters / pharmacokinetics*
  • Polyethylene Glycols / chemical synthesis
  • Polyethylene Glycols / pharmacokinetics

Substances

  • Anti-Inflammatory Agents
  • Delayed-Action Preparations
  • Drug Implants
  • Polyesters
  • poly(3-hydroxybutyrate)-co-(3-hydroxyvalerate)
  • Polyethylene Glycol 6000
  • Polyethylene Glycols
  • Betamethasone