Proteins & Peptides Microspheres Delivery System Development

Biodegradable microspheres composed of biocompatible polymers have been extensively studied for controlled release systems of proteins and peptides. Benefiting from decades of successful project experience and expertise in the development of microsphere delivery systems, CD Formulation specializes in encapsulating peptides and proteins in microspheres to meet the growing demand for advanced therapeutic solutions.

Potential Advantages of Microspheres Delivery of Protein/Peptide

As potential drug carriers for various routes of administration of biomacromolecules such as proteins/peptides, microspheres have the following advantages over other dosage forms.

• Supports controlled release of protein/peptide drugs to specific target sites and enables manipulation of the drug's in vivo effects, pharmacokinetic (PK) characteristics, tissue distribution, and cellular interactions.
• Improves stability, protects proteins/peptides from degradation by the body's internal environment, and maintains their structural integrity and biological activity.
• Reduces dosing frequency.
• Reduces dosing doses and reduces the likelihood of adverse events.
• Improves bioavailability and eliminates fluctuations in drug serum concentrations.

Fig. 1 General structure of microspheres. (CD Formulation)

Explore Our Proteins & Peptides Microspheres Delivery System Development Services

Although the application of microspheres in protein/peptide drug delivery has made significant progress, challenges still exist. Disadvantages of microspheres include difficulty in large-scale production, drug inactivation during the manufacturing process, and poor control of the drug release rate.

As an expert in protein/peptide science and formulation science, CD Formulation has the most advanced industry knowledge and technology in protein and peptide delivery and is committed to providing you with comprehensive, innovative, and efficient microsphere delivery system development solutions.

With advanced manufacturing technology and a professional team, we can customize the microsphere delivery system using a variety of biodegradable polymers such as PLA, PCL, polyanhydrides, and poly(orthoesters) to meet your specific needs.

Our expertise in microsphere development covers:

• Porous Microspheres

Proteins/peptides are in contact with the external environment through the gaps formed by polymerization without gradual dissolution, and they are continuously dissolved and diffused to exert their drug effects. The number of pores on the sphere determines the surface area and drug loading of the microsphere, and the two together affect the release of the drug. Our science usually adjusts the pore size of the microsphere by selecting appropriate solvents to achieve optimal drug release.

• Double-layer Microspheres

Double-layer microspheres have a core-shell structure. Our scientists mix a biodegradable polymer material with the drug as the core of the microsphere, and another biodegradable polymer material as the shell. Unlike porous microspheres, the release of double-layer microspheres mainly depends on the core-shell structure.

Magnetic Microspheres

Magnetic microspheres are modified on the basis of the first two types of microspheres. Our science makes magnetic metals or metal oxides into ultrafine powders, disperses them in polymer materials or drugs, and obtains a mixture of drugs, metals, and polymer-degradable materials, namely magnetic microspheres.

Our Microsphere Preparation Method

Fig. 2 Categorization of methods for preparing protein/peptide microsphere. (CD Formulation)

Emulsification-Solvent Evaporation Method

This method generally involves the formation of a single emulsion (O/W) or double emulsion (W/O/W).

1) For poorly soluble molecules, we use the O/W method. The main steps include:

• Dissolving the insoluble drug in an organic solvent containing a polymer.
• Emulsifying the organic phase or dispersed phase in an aqueous phase or continuous phase.
• Extracting the solvent from the dispersed phase with the continuous phase.
• Converting the droplets of the dispersed phase into solid particles.
• Collecting and drying the microspheres to eliminate the residual solvent.

2) For highly hydrophilic molecules, we use the W/O/W double emulsion method. The main steps include:

• Adding an aqueous solution containing a hydrophilic molecule to a polymer solution previously dissolved in a water-immiscible organic solvent (e.g., dichloromethane, chloroform, ethyl acetate) to form a primary emulsion.
• Adding an aqueous emulsifier to the primary emulsion to form a double emulsion.
• The double emulsion is then transferred to an aqueous medium to evaporate the organic solvent to form microspheres.

The double emulsification method can produce microspheres with high encapsulation efficiency and high yield, which is suitable for temperature-sensitive drugs.

Coacervation/Phase Separation Method

This method is a process of separating a polymer solution into two immiscible equilibrium liquid phases. The main steps include phase separation of the coating polymer solution, adsorption of the coacervate around the protein molecules, and solidification of the microparticles.

Spray Drying Method

This method improves the stability of proteins/peptides by encapsulating them. The main steps include:

• Dispersing an aqueous solution of the protein or peptide in an organic phase containing the polymer to form a primary emulsion.
• This primary emulsion is atomized in a heated air stream with appropriate inlet/outlet temperatures,
• The solvent is evaporated instantaneously from the formed droplets, resulting in microspheres with a size range of 1 to 100 µm (depending on the atomization conditions).

Supporting Microspheres Analysis and Testing Services

Physicochemical characterization is one of the key steps to ensure the success of microsphere formulation. It can confirm the quality and quantity of drug encapsulated in the microspheres (including drug loading, absence of incompatibility, stability, and crystallinity), the quality of the microspheres (such as particle size, shape, and encapsulation efficiency), and the quality of the microencapsulation process (including yield, encapsulation efficiency, and particle size distribution).

We provide a full range of microsphere characterization services to support the successful implementation of your microsphere project, including but not limited to:

Why Choose Us for Proteins & Peptides Microspheres Delivery System Development?

• Extensive expertise and experience in executing protein/peptide microsphere delivery system development.
• We have a flexible team of experts responsible for protein/peptide microsphere formulation feasibility, process development, and commercial manufacturing.
• Scalable microsphere manufacturing process.
• Comprehensive analytical testing capabilities, including surface photomorphology, drug loading percentage, residual solvent testing, etc.
• We provide flexible and tailored solutions to meet our customers' specific needs and requirements.
• Fast and efficient services ensure that our customers' projects are delivered on time.

Publication

CD Formulation is continually researching and developing new technologies to improve protein/peptide aqueous microsphere delivery systems. Our scientists stay up to date on the latest advances in the field to provide innovative solutions that can enhance protein and peptide delivery. Please don't hesitate to contact us if you are interested in our services.

How It Works

STEP 1

Submit a service request describing your specific research or development need.

STEP 2

We'll email you to provide your quote and confirm order details if applicable.

STEP 3

Execute the project with real-time communication, and deliver the final report promptly.