Self-injectable extended release formulation of Remdesivir (SelfExRem): A potential formulation alternative for COVID-19 treatment

Int J Pharm. 2021 Mar 15:597:120329. doi: 10.1016/j.ijpharm.2021.120329. Epub 2021 Feb 2.

Abstract

There has been a growing and evolving research to find a treatment or a prevention against coronavirus 2019 (COVID-19). Though mass vaccination will certainly help in reducing number of COVID-19 patients, an effective therapeutic measure must be available too. Intravenous remdesivir (RDV) was the first drug receiving Food and Drug Administration (FDA) approval for the treatment of COVID-19. However, in a pandemic like COVID-19, it is essential that drug formulations are readily available, affordable and convenient to administer to every patient around the globe. In this study, we have developed a Self-injectable extended release subcutaneous injection of Remdesivir (SelfExRem) for the treatment of COVID-19. As opposed to intravenous injection, extended release subcutaneous injection has the benefits of reducing face-to-face contact, minimizing hospitalization, reducing dosing frequency and reducing overall health care cost. SelfExRem was developed using a biodegradable polymer, poly(lactic-co-glycolic acid) (PLGA), dissolved in a biocompatible vehicle. Six different batches were formulated using 2 different grades of low molecular weight PLGA and 3 different PLGA concentration. The force of injection of various polymeric solutions through 23-30-gauge needles were analyzed using a TA.XTplus texture analyzer. The time required for injection was evaluated both manually and by using an autoinjector. In vitro release of all the batches were carried out in 1% v/v tween 80 in phosphate buffer saline. The study indicated that SelfExRem developed with15% w/v PLGA(75:25) provided a steady release of drug for 48 h and may be a breakthrough approach for the treatment of COVID-19.

Keywords: Covid19; In situ depot formulations; Long-acting injectables; Remdesivir; SARS-CoV2.

MeSH terms

  • Adenosine Monophosphate / analogs & derivatives*
  • Adenosine Monophosphate / pharmacology
  • Alanine / analogs & derivatives*
  • Alanine / pharmacology
  • Antiviral Agents / pharmacology
  • COVID-19 Drug Treatment*
  • COVID-19* / epidemiology
  • COVID-19* / prevention & control
  • Delayed-Action Preparations / pharmacology*
  • Drug Evaluation, Preclinical
  • Humans
  • Injections, Subcutaneous / methods
  • Prodrugs / pharmacology
  • SARS-CoV-2

Substances

  • Antiviral Agents
  • Delayed-Action Preparations
  • Prodrugs
  • remdesivir
  • Adenosine Monophosphate
  • Alanine