Proteins and peptides are inherently unstable and susceptible to degradation by a variety of physical and chemical degradation mechanisms. Therefore, a variety of excipients are required to stabilize them during processing and storage. As a professional pharmaceutical technology company, CD Formulation provides customers with a variety of excipient solutions for stabilizing proteins and peptides. With our unique technology and professional team, we provide customers with customized excipient formulas to ensure product stability and activity during production and storage.

The Importance of Stable Excipients Screening

Biomolecules, such as peptides, proteins, monoclonal antibodies, etc., are inherently less stable than small molecules. Moreover, formulation development is often hampered by strict product development timelines. Additionally, the limited availability of drug substances forces formulation scientists to rely heavily on the use of forced degradation studies that often result in suboptimal formulation development, ultimately leading to stability and manufacturing challenges during clinical and commercial manufacturing processes. In other words, complex molecular structures, lack of clear stability-indicating assays, and multiple degradation mechanisms pose major obstacles to the formulation development of therapeutic proteins and peptides. These characteristics determine the need to screen suitable stable excipients and understand their interactions with active molecules in the pre-formulation research stage to rationally design stable formulations of therapeutic proteins and peptides, especially high-concentration protein formulations.

Explore Our Stable Excipients Screening Services

The study of excipients to stabilize therapeutic proteins and peptides is critical to successful formulation strategies. Through proper selection of excipients, the forces affecting the conformational stability of the molecule, such as electrostatic interactions, van der Waals interactions, hydrogen bonding, and hydrophobicity, can be targeted to improve the stability of therapeutic proteins and peptides.

At CD Formulation, we provide you with unparalleled excipient screening services to facilitate your product's smooth entry into the formulation development stage. For native conformations in therapeutic proteins and peptides, our scientists specialize in stabilization with high concentrations of sugars (e.g., sucrose, trehalose, lactose, etc.) and polyols (e.g., sorbitol, mannitol, polyethylene glycol, etc.), due to they are preferentially excluded from protein surfaces.

Our services include but are not limited to:

Solubilizing Agent Screening

For proteins and peptides, solubility can usually be increased by adding moderate concentrations of salt. However, salt excipients may negatively affect the conformational stability of some proteins and peptides. In this case, we will screen for you the best counterions and their concentrations to change your product stability, including:

• Use different buffer types with different compositions (i.e. different ionic strengths) to obtain the same pH conditions to change protein stability.
• Maintain the native state of the protein by binding to ligands.

Surfactant Screening

Surfactants help inhibit the adsorption, denaturation, and aggregation of proteins at interfaces (air-water and solid-water), as well as may also affect stability through differential binding to the native or denatured state of the protein.

We will conduct a series of stirring and freeze-thaw stress studies to analyze the effect of different surfactants, such as polysorbate 20, polysorbate 80, Pluronic F6, or others, on your therapeutic proteins and peptides to effectively reduce the formation of soluble and insoluble aggregates.

Antibacterial Preservative Screening

For products in multi-dose forms, we also offer excipient screening services for antimicrobial preservatives. Our scientists typically screen various preservatives, including m-cresol, benzyl alcohol or phenol, phenoxyethanol, and chlorobutanol, individually or in combination before selection.

It should be noted that for multidose formulations since the protein is unstable in aqueous conditions, we will be conducting studies by forcing lyophilization without preservatives and reconstitution with BWFI (bacteriostatic water for injection).

Lyophilizing Protectants Screening

For lyophilized formulations, proteins can be denatured in the frozen concentrate state, at the frozen surface interface, and during freezing.

We will fully consider the impact of excipients, such as local concentrations of salts and buffers and pH changes caused by buffer crystallization, on the stability of proteins and peptides. Comprehensive consideration and screen additional lyoprotectants, such as sucrose and trehalose, to maximize protein and peptide stability. This includes testing and optimizing parameters such as drying rate, temperature, and pressure under different freeze-drying conditions.

Why Choose Us for Stable Excipients Screening of Protein & Peptide Formulation?

• Our team of experts has extensive experience in stable excipients screening for protein and peptide formulation, ensuring that we use the most effective methods and techniques to optimize stability.
• Comprehensive stabilizing excipient portfolio, including buffers, amino acids, stabilizers, bulking agents, surfactants, cyclodextrin based, salts, etc.
• Equipped with state-of-the-art facilities and equipment allows for conducting thorough and precise stability studies to determine the best excipients.
• A variety of testing options are available to meet any type of protein and peptide, including monoclonal antibodies, recombinant proteins, therapeutic peptides, etc.
• Prioritize customer satisfaction and ensure regular communication with our clients throughout the screening process to ensure they are informed and involved every step of the way.
• Provides flexible testing design and customized solutions.

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