Excipients in parenteral formulations: selection considerations and effective utilization with small molecules and biologics

  title={Excipients in parenteral formulations: selection considerations and effective utilization with small molecules and biologics},
  author={Bindhu Madhavi Rayaprolu and Jonathan J Strawser and Gopal Anyarambhatla},
  journal={Drug Development and Industrial Pharmacy},
  pages={1565 - 1571}
Abstract Excipients form a major component of pharmaceutical formulations and are classified as any ingredient other than the active ingredient which is included within the product formulation to improve drug product performance. Functional uses of excipients include improving solubility and stability, safety and efficacy, as bulking agents in lyophilized formulations, tonicity agents, and aiding in controlled or prolonged drug delivery. Parenteral formulations are sterile, pyrogen-free; free… Expand
Excipients in freeze-dried biopharmaceuticals: contributions toward formulation stability and lyophilisation cycle optimisation.
The main aim of the present review is to define the most important groups of biopharmaceutical excipients, based on their roles in formulations and the mechanism(s) through which they support the lyophilisation process, to provide products with the required protein efficiency and product characteristics. Expand
Rational design to biologics development: the polysorbates point of view.
Polysorbates are the most widely used surfactants in the pharmaceutical industry, and are presented in >80% of commercial monoclonal antibody formulations, and the characteristics that have to be taken into account during formulation development are provided. Expand
Cyclodextrins in parenteral formulations.
  • T. Loftsson
  • Medicine, Chemistry
  • Journal of pharmaceutical sciences
  • 2020
The physiochemical and biological properties of CDs are reviewed as well as their pharmacokinetics after intravenous administration, and some examples are given of how CDs are applied in aqueous parenteral formulations, how their solubilizing effect has been enhanced and how their target concentration is determined. Expand
Lyophilized liposome-based parenteral drug development: Reviewing complex product design strategies and current regulatory environments.
This review provides an overview of liposome formulation-specific lyophilization approaches for parenteral use, excipients used exclusively in liposomal parenTERal products, lyophilsome formulation design and process development, long-term storage, and current regulatory guidance for liposom drug products. Expand
Fabrication of advanced parenteral drug-delivery systems
This chapter summarizes the historical development of the field, including colloidal dispersions ideas, biodegradable polymer approaches, surface-releasing systems, liposomes, niosomes, nanoscale systems, implantable drug-delivery system, infusion devices, short-interfering RNA, and microRNA delivery system along with Food and Drug Administration–approved parenteral products for the management of several diseases. Expand
Lyophilization of Small-Molecule Injectables: an Industry Perspective on Formulation Development, Process Optimization, Scale-Up Challenges, and Drug Product Quality Attributes.
A general overview of the lyophilization process is provided and several key considerations and product development aspects of formulation, process optimization, container closure system, scale-up principles, and drug product quality attributes from the industrial viewpoint are discussed. Expand
Subcutaneous delivery of biotherapeutics: challenges at the injection site
This review provides an overview of the factors affecting subcutaneous absorption with a focus on transient effects at the injection site following administration of biotherapeutics and the subsequent impact on absorption and stability. Expand
Formulation strategies in immunotherapeutic pharmaceutical products
A concise and contemporary review of ongoing formulation strategies and excipients used in approved antibodies and cellular therapeutic products is provided. Expand
Evaluating parameters affecting drug fate at the intramuscular injection site.
The purpose of this article is to propose "critical parameters" of the IM environment that could be examined in hypothesis-driven studies that might ultimately be useful in predicting and improving in vivo PK performance of IM injected drugs. Expand
Self-Assembled, Dilution-Responsive Hydrogels for Enhanced Thermal Stability of Insulin Biopharmaceuticals
This work reports the utilization of a cellulose-based supramolecular hydrogel formed from polymer–nanoparticle (PNP) interactions to encapsulate and stabilize insulin, an important biotherapeutic used widely to treat diabetes. Expand


Excipient Selection In Parenteral Formulation Development
. Excipients are the integral part of pharmaceutical products development to achieve desired product profile (stability and efficacy). This review deals with understanding of the physicochemicalExpand
Pharmaceutical excipients - quality, regulatory and biopharmaceutical considerations.
  • D. Elder, M. Kuentz, R. Holm
  • Medicine
  • European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2016
Exipients can have an impact on the absorption, distribution, metabolism and elimination (ADME) processes of the co-administered drug, which is important information when selecting excipients for any new formulation. Expand
Pharmaceutical Excipients: A review
Excipients play an important role in formulating a dosage form. These are the ingredients which along with Active Pharmaceutical Ingredients make up the dosage forms. Excipients act as protectiveExpand
Handbook of Pharmaceutical Excipients
The Handbook of Pharmaceutical Excipients has been conceived as a systematic, comprehensive resource of information ​ on all of the physical and chemical properties of these materials and the growth of novel forms of delivery has resulted in an increase in the number of excipients being used and suppliers ofexcipients have developed novel coprocessed excipient mixtures and new physical forms to improve their properties. Expand
Drug-excipient interaction and its importance in dosage form development
Excipients are included in dosage forms to aid manufacture, administration or absorption. Although considered pharmacologically inert, excipients can initiate, propagate or participate in chemical orExpand
An Overview of Pharmaceutical Excipients: Safe or Not Safe?
This review is intended to address the general status of the pharmaceutical excipients and to describe the safety assessment, and suggests the interest of simplifying the formulations as much as possible and of reducing the number ofexcipients necessary to strictly meet the required functions. Expand
Protein-excipient interactions: mechanisms and biophysical characterization applied to protein formulation development.
Key mechanisms of protein-excipient interactions such as electrostatic and cation-pi interactions, preferential hydration, dispersive forces, and hydrogen bonding are presented in the context of different physical states of the formulation. Expand
Drug-Excipient Interactions: Case Studies and Overview of Drug Degradation Pathways
The objective of the current research article is to provide a comprehensive review of excipients impact on the stability of the drug product and their implications during the product development.Expand
Interactions of formulation excipients with proteins in solution and in the dried state.
A number of mechanisms by which the excipients interact with proteins in solution and with various interfaces, and their effects on the physical properties of the dried protein structure are described, and how the various interaction forces are related to their observed effects on protein stability are explained. Expand
Excipient hydrolysis and ester formation increase pH in a parenteral solution over aging.
The physicochemical stability of an injectable solution of conivaptan hydrochloride salt was investigated and the pH of the solution was found to increase gradually over time, thereby ensuring product quality through the prevention of precipitate formation due to reduced solubility. Expand