Preparation of Nano-vesicles for Encapsulating Protein Drugs

The half-life of most proteins in the body is about 10 minutes on average, and proteins entering the body are rapidly cleared by various proteases in the body. In particular, the complex tertiary and quaternary structures of protein drugs are easily denatured and inactivated during preparation and in vivo administration, and have very short half-lives. Facing the obstacles of enzymatic degradation in the gastrointestinal tract and the first-pass effect in the liver, the protein conformation is easily affected by the microenvironment such as acid-base and charge in the body, and after the conformation change, it not only loses its original activity, but also completely changes the nature of the protein, and even induces harmful immune reaction, making it change from a good drug to a poison. CD Formulation can customize the vesicles that encapsulate protein drug molecules to avoid the technical problems of drug rupture and leakage during in vivo delivery. Our technical team will perform a full range of analytical tests to ensure that the product meets your requirements and helps you develop your drug.

How to Prepare Nano-vesicles for Encapsulating Protein Drugs

• Mix glycidyl methacrylate dextran solution with polyethylene glycol solution to form a suspension.
• Add tri-block polymers to the suspension and emulsify for a certain time, followed by the addition of protein macromolecule drugs and emulsify for a certain time to form nano-vesicles encapsulating protein macromolecule drugs dispersed in two phases of polyethylene glycol and glycidyl methacrylate dextran.
• A cross-linking agent is added to the nano-vesicle emulsion, cross-linked for a certain period of time, followed by dialysis through a dialysis bag, and the water is removed after lyophilization to obtain polymeric nano-vesicles wrapped with protein macromolecule drug.

Among them, the protein macromolecule drug can be selected from one or more of B-galactosidase, FITC-BSA, calf serum protein, interferon or erythropoietin.

Protein Nano-vesicles Analysis Testing

• Protein nanovesicles morphology test
• Particle size analysis of protein nanovesicles
• MTT toxicity of protein nanovesicles
• Stability testing of protein nanovesicles

The Advantages of Nano-vesicles Preparation Technology

• The preparation method of nanovesicles encapsulating protein macromolecules is based on internal aqueous cross-linking, which can avoid the rupture of the vesicles and the leakage of the drug after the change of osmotic pressure during the in vivo delivery.
• Nano-vesicles can maintain the activity of protein macromolecule drug, the surface of vesicle composition is smooth and round, the particles are regular and non-adhesive, the particle size can be adjusted according to the need, its lyophilized powder is micro-white and delicate, good homogeneity, loose, will not collapse and good dispersibility.
• With the selection of polyethylene glycol solution and glycidyl methacrylate dextran solution with suitable concentration and ratio, the protein has an active encapsulation mechanism to enter the internal aqueous phase more easily, which improves the encapsulation rate of vesicles and avoids the disadvantages of the conventional W/O and W/O/W encapsulation rates.
• The method of encapsulating proteins, which can avoid the effect of the preparation method on the therapeutic effect of the drug, especially the drugs with unstable physicochemical properties and sensitive to the oil-water interface.
• In the present invention, the tri-block polymer is distributed on the surface of the internal water phase according to the phase orientation to form vesicles, which not only reduce the surface tension in the preparation (which can adjust the vesicle particle size), but also provide a platform for the targeting groups to be linked.
• In the preparation method, the cross-linking agent allows the vesicles to be delivered in vivo without rupture due to osmotic pressure, which improves the mechanical strength of the vesicles.

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