Abstract
The oral route is the most common route for drug administration. It is the most preferred route, due to its advantages, such as non-invasiveness, patient compliance and convenience of drug administration. Various factors govern oral drug absorption including drug solubility, mucosal permeability, and stability in the gastrointestinal tract environment. Attempts to overcome these factors have focused on understanding the physicochemical, biochemical, metabolic and biological barriers which limit the overall drug bioavailability. Different pharmaceutical technologies and drug delivery systems including nanocarriers, micelles, cyclodextrins and lipid-based carriers have been explored to enhance oral drug absorption. To this end, this review will discuss the physiological, and pharmaceutical barriers influencing drug bioavailability for the oral route of administration, as well as the conventional and novel drug delivery strategies. The challenges and development aspects of pediatric formulations will also be addressed.
Highlights
Reviewed by: Urjita Sheth, Uka Tarsadia University, India Amit Kumar Nayak, Seemanta Institute of Pharmaceutical Sciences (SIPS), India
Several transporters belonging to the adenosine triphosphate (ATP) binding cassette transporters (ABC transporters) superfamily and solute carrier (SLC) transporters are expressed in the apical and basolateral membranes of the GI tract for the influx or efflux of endogenous substances and xenobiotics
The NPs were suggested to enhance the epithelial permeability and are efficient for oral drug delivery Reported the development of biodegradable NPs containing streptomycin with high loading efficiency of 50% or higher for tuberculosis treatment
Summary
Polysaccharidase – Proteases, lipases Polysaccharidase, oligosaccharidases, proteases, peptidases, lipases Oligosaccharidases, peptidases, lipases Broad spectrum of bacterial enzymes. Food affects the GI functions such as gastric emptying, intestinal transit time, bile acid secretion, stomach pH change, and liver blood flow increase It can alter the physiochemical characteristics of drugs, such as solubility, intestinal permeability, size, and dissolution profile. Several transporters belonging to the adenosine triphosphate (ATP) binding cassette transporters (ABC transporters) superfamily and solute carrier (SLC) transporters are expressed in the apical and basolateral membranes of the GI tract for the influx or efflux of endogenous substances and xenobiotics The absorption via this pathway is an energy-consuming process requiring ATP hydrolysis and can occur against a concentration gradient, that is, from a region of lower drug concentration to that of higher concentration. Dosage form changes that significantly increase the solubility of BDDCS class 2 drugs might decrease or eliminate the effect of high-fat meals and mostly minimize other drug transporter interactions.
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