Abstract
Till recent, injections remained the most common means for administering therapeutic proteins and peptides because of their poor oral bioavailability. However, oral route would be preferred to any other route because of its high levels of patient acceptance and long term compliance, which increases the therapeutic value of the drug. Designing and formulating a polypeptide drug delivery through the gastro intestinal tract has been a persistent challenge because of their unfavorable physicochemical properties, which includes enzymatic degradation, poor membrane permeability and large molecular size. The main challenge is to improve the oral bioavailability from less than 1% to at least 30-50%. Consequently, efforts have intensified over the past few decades, where every oral dosage form used for the conventional small molecule drugs has been used to explore oral protein and peptide delivery. Various strategies currently under investigation include chemical modification, formulation vehicles and use of enzyme inhibitors, absorption enhancers and mucoadhesive polymers. This review summarizes different pharmaceutical approaches which overcome various physiological barriers that help to improve oral bioavailability that ultimately achieve formulation goals for oral delivery.
Highlights
Till recent, injections remained the most common means for administering therapeutic proteins and peptides because of their poor oral bioavailability
Since the liver is a signiÞcant participant in the control of blood glucose, it is believed that successfully activating the liver with oral insulin may provide a mechanism to potentially reestablish normal glucose control in the diabetic patient and turn on a number of metabolic activities that can help mitigate complications of diabetes[17]
Numerous classes of compounds with diverse chemical properties, including detergents, surfactants, bile salts, Ca2+ chelating agents, fatty acids, medium chain glycerides, acyl carnitine, alkanoyl cholines, N-acetylated α-amino acids, N-acetylated non-αamino acids, chitosans, mucoadhesive polymers, and phospholipids have been reported to enhance the intestinal absorption of large polypeptide drugs[24,25]
Summary
Injections remained the most common means for administering therapeutic proteins and peptides because of their poor oral bioavailability. Designing and formulating a polypeptide drug delivery through the gastro intestinal tract has been a persistent challenge because of their unfavorable physicochemical properties, which includes enzymatic degradation, poor membrane permeability and large molecular size. Injections (i.e. intravenous, intramuscular or subcutaneous route) remain the most common means for administering these protein and peptide drugs. Oral administration presents a series of attractive advantages towards other drug delivery These advantages are relevant for the treatment of pediatric patients and include the avoidance of pain and discomfort associated with injections and the elimination of possible infections www.ijpsonline.com caused by inappropriate use or reuse of needles.
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