Posted on November 14, 2022 at 12:07 pm

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 Protein and Peptide Oral Delivery Methods Researched

As medical research develops, scientists produce many proteins and peptides (PPs) for use in therapy. Pharmaceutical polymers (PPs) have attracted the pharmaceutical industry’s attention as a promising alternative to small molecular therapies due to their high selectivity, high efficacy, and low toxicity.


Peptides are polypeptide chains, long chains of amino acids linked together by peptide bonds. A peptide is a chain of amino acids that is less than 50 amino acids in length. Polypeptides are bigger than oligopeptides and may include more than fifteen amino acids. Any substance that lacks fifty amino acids cannot be called a protein.


Proper medicine administration improves treatment outcomes and patient adherence. On the other hand, the limited oral bioavailability of peptides necessitates their frequent intravenous administration. Long-term, continual injections may be challenging for patients to adhere to due to pain, intolerance to needles, and local irritation. For this reason, numerous research institutions have been working to develop non-intravenous routes for peptides, including the oral route and nasal, ophthalmic, buccal, and transdermal administration.


Oral insulin administration, as opposed to subcutaneous injection, may also result in better glucose control (sc). Some chronic illness patients may have an easier time if their medications are given orally.


There are several obstacles to oral absorption of PPS.


Although there is considerable interest from pharmaceutical companies and funding agencies in producing oral PPs, there are several challenges in doing so because of the instability of the GI tract and the limited permeability across intestinal epithelia. The major hurdles to oral absorption of PPs are the physiological barriers caused by the GI tract’s intrinsic character as the leading site of food processing and nutrient uptake and the first line of defense against toxins and viruses. In order to overcome obstacles associated with oral administration, knowledge of the physiological and formulation elements is essential.


Innate defenses


In order to reach the small intestine following oral administration, most medications must first survive the harsh environment of the stomach and gastric secretions. However, the stability and absorption of PPs are significantly affected by the differences in pH, enzymes, mucus, and even epithelial permeability between the stomach and intestines.


Inputs that influence the formulation


For the successful commercialization of oral PPs medication, the formulation is as vital as overcoming physiological barriers. The chemical and physical stability of PPs must be considered during formulation to guarantee their durability throughout production, shipping, storage, and dosing. Many excellent papers have outlined the formulation factors that impact stability for parenteral formulations. Compared to small-molecule medicine, PPs rely heavily on interactions, including hydrophobic and hydrophilic forces, hydrogen bonding, and electrostatic repulsion. Some PPs may be altered in surface charge, density, and dispersion depending on the pH of a formulation. PPs’ colloidal stability, which is affected by protein aggregation and degradation rates, is affected by pH. The ionic strength of a solution affects the physical stability of PPs in the same way that pH does; increasing the salt content of the solution may enhance the hydrophobic contacts between proteins. So, professionals utilize solutions to stabilize PPs in solution formation.


Researchers may improve solubility, and protein aggregates avoid using excipients such as arginine, histidine, and glycine in protein formulation. With its ability to inhibit protein accumulation, arginine helps maintain protein structure. Polysorbate is a surfactant that may be used to stabilize proteins by lowering their molecular interactions with surfaces. PPs’ chemical instability impacts the board from inception to decommissioning. Antioxidants such as methionine ascorbic acid may inhibit the oxidation of phenylalanine, tyrosine, phenylalanine, tryptophan, histidine, cysteine, and phenylalanine found in peptide precursors (PPs). The main challenge in protecting PPs under GI circumstances is oral administration, which is complicated by an enzymatic breakdown. The most prevalent ways to shield oral formulations from digestive enzymes include enteric coating, encapsulation, and enzyme inhibitors. Permeation enhancers in oral formulations include sulfosuccinate (SNAC), bile salts (CH3COONa), and nonionic surfactants (NIS).


You can find oral peptides here if you are a researcher interested in further studying the potential of these substances.

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