Oral administration, as an ideal drug delivery method, has become a hot topic in the research of protein and peptide drug delivery systems. CD Formulation masters cutting-edge technology and expertise in the development of therapeutic protein and peptide formulations and oral drug delivery systems, and is committed to providing innovative solutions for improving the oral bioavailability and stability of protein and peptide drugs.
Proteins and peptides have gradually become attractive therapeutic molecules due to their high selectivity, good efficacy, and few side effects. However, most protein and peptide drugs are large molecule hydrophilic drugs, which are easily degraded by gastric acid and pepsin under the extreme environment of gastrointestinal stability. At the same time, due to their hydrophilicity, they cannot effectively penetrate physiological barriers such as tight junctions between cells such as the small intestinal mucosa and epithelial layer. This makes the development of oral delivery systems for proteins and peptides face many challenges. It is necessary to fully combine and utilize strategies such as nanotechnology and enteric coating to avoid enzymatic degradation in the digestive system and improve the oral bioavailability of drugs.
Fig. 1 Major barriers to oral delivery of peptide and protein-based drugs.(Cao SJ, et al., 2019)
CD Formulation is an expert in therapeutic protein/peptide science and formulation science, focusing on combining advanced formulation technology with protein/peptide knowledge to develop first-class protein/peptide oral delivery systems. Our scientists deploy a range of strategies, chemical modification, the addition of effective agents, nano-carrier systems, and medical devices to improve the bioavailability and stability of these challenging molecules.
Importantly, our team of scientists has extensive formulation development experience and expertise to design formulations suitable for different protein/peptide compounds, such as spray-dried formulations, lyophilized formulations, tablets, capsules, etc., to support the development of oral delivery systems.
Fig. 2 Our formulation strategies for oral delivery of protein/peptide. (CD Formulation)
The successful development of protein/peptide oral delivery systems lies in protecting these unstable active pharmaceutical ingredients to ensure that they can remain stable in gastric acid and other digestive juices.
1) At CD Formulation, an effective strategy is to stably encapsulate proteins/peptides in nanocarriers. This usually involves selecting suitable carrier materials, such as polymers or liposomes, and using appropriate technologies and methods to encapsulate and protect the active pharmaceutical ingredients.
2) Another key strategy is to introduce some auxiliary substances into the oral delivery system, such as penetration enhancers or enzyme inhibitors, to help improve the absorption rate and stability of proteins/peptides. In addition, targeted delivery systems targeting specific targets can also improve the effectiveness of drugs and reduce dosage.
Published Data
Technology: Orodispersible Films (ODFs)
Journal: Eur J Pharm Biopharm
IF: 4.4
Published: 2018
Results:
The authors prepared protein-loaded orodispersible films (ODFs) based on trehalose/pullulan mixtures by freeze drying. Ovalbumin, lysozyme, and β-galactosidase were selected as model proteins. Ovalbumin was used to study the effects of protein incorporation on the mechanical properties, disintegration time, weight uniformity, and thickness of ODFs, and lysozyme and β-galactosidase were used to evaluate protein stability. The results showed that the addition of ovalbumin had no significant effect on the mechanical properties of freeze-dried ODFs, the trehalose/pullulan ratio had no effect on the stability of lysozyme, while the stability of β-galactosidase increased with the increase of the trehalose/pullulan ratio. This indicates that trehalose/pullulan-based ODFs are promising for oral protein delivery.
Fig. 3 Graphical abstract of trehalose/pullulan-based ODFs. (Tian Y et al., 2018)
CD Formulation is always at the forefront of protein/peptide oral delivery system development, mastering the most cutting-edge technologies and methods. Please don't hesitate to contact us if you are interested in our services.
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