Biologic excipients: Importance of clinical awareness of inactive ingredients

PLoS One. 2020 Jun 25;15(6):e0235076. doi: 10.1371/journal.pone.0235076. eCollection 2020.

Abstract

Due to the complexity and fragility of biological drug products, several challenges exist in their formulation development. Excipients are added to increase product stability, maintain tonicity, and facilitate drug delivery. The potential implications of these additive substances merit clinical consideration. We assessed the safety risk of excipients on the basis of their type and variability through an assessment framework, which quantifies excipient complexity in 230 biological formulations, and identifies excipient-related adverse events through published case reports. A biologic on average contained 4.45 excipients, half of that found in oral medications. The frequency distribution was heavily skewed towards the most commonly occurring excipients: water (40.4%), sodium chloride (38.3%), polysorbate 80 (28.7%), sucrose (24.4%), and mannitol (20.9%), with 44.4% of formulations not listing the concentration of the most commonly occurring inactive ingredients. A literature search revealed only 17 case reports of excipient-related adverse events, suggesting the need for more clarity for clinicians on the safety of chemical additives. These cases included injection site reactions, anaphylaxis, hyperglycemia, and acute renal failure. With the expansion of the biopharmaceutical market, it is important to consider the safety data of biologic excipients, so that therapy can be tailored appropriately for a specific patient.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acute Kidney Injury / chemically induced*
  • Anaphylaxis / chemically induced*
  • Chemistry, Pharmaceutical
  • Excipients / adverse effects*
  • Excipients / therapeutic use
  • Humans
  • Hyperglycemia / chemically induced*
  • Mannitol / adverse effects
  • Mannitol / therapeutic use
  • Polysorbates / adverse effects
  • Polysorbates / therapeutic use
  • Sodium Chloride / adverse effects
  • Sodium Chloride / therapeutic use
  • Sucrose / adverse effects
  • Sucrose / therapeutic use
  • Water / adverse effects

Substances

  • Excipients
  • Polysorbates
  • Water
  • Mannitol
  • Sodium Chloride
  • Sucrose

Grants and funding

This work was funded by a grant from U.S. Pharmacopeia, who participated in the design and conduct of the study, analysis and interpretation of the data, and review of the final manuscript, although the decision to submit the manuscript for publication was the authors’ alone.