Enhanced oral absorption of insulin from desolvated fatty acid-sodium glycocholate emulsions

Mesiha, Mounir S.; Plakogiannis, Fotios M.; Vejosoth, Suttida

doi:10.1016/0378-5173(94)90343-3

Cited by 61 publications

(20 citation statements)

References 9 publications

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“…Significant improvements of oral insulin absorption were already attained by masking the hydrophilic surface of its molecule. Moreover, chemical modification of the molecule by optimizing the fatty acid chain length with palmitic acid achieved an enhanced oral absorption of insulin [56][57][58].…”

Section: Future Research Pathsmentioning

confidence: 99%

Oral Antidiabetic Therapy in Patients with Heart Disease

Fisman

Tenenbaum

Motro

et al. 2004

Herz

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Five types of oral antihyperglycemic drugs are currently approved for the treatment of diabetes: biguanides, sulfonylureas, meglitinides, glitazones, and alpha-glucosidase inhibitors. The cardiovascular effects of the most commonly used antidiabetic drugs in these groups are briefly reported, in an attempt to improve knowledge and awareness regarding their influences and potential risks when treating patients with coronary artery disease (CAD). Regarding biguanides, gastrointestinal disturbances such as diarrhea are frequent, and the intestinal absorption of group B vitamins and especially folate is impaired during chronic therapy. This deficiency may lead to increased plasma homocysteine levels which, in turn, accelerate the progression of vascular disease due to adverse effects on platelets, clotting factors, and endothelium. The existence of a graded association between homocysteine levels and overall mortality in patients with CAD is well established. In addition, metformin may lead to lethal lactic acidosis, especially in patients with clinical conditions that predispose to this complication, such as heart failure or recent myocardial infarction. Sulfonylureas avoid ischemic preconditioning. During myocardial ischemia, they may prevent the opening of the ATP-dependent potassium channels, impeding the necessary hyperpolarization that protects the cell by blocking calcium influx. Meglitinides may exert similar effects, due to their analogous mechanism of action. During treatment with glitazones, edema has been reported in 5% of patients, and these drugs are contraindicated in diabetics with NYHA class III or IV cardiac status. The long-term effects of alpha-glucosidase inhibitors on morbidity and mortality rates and on diabetic micro- and macrovascular complications are yet unknown. The combined sulfonylurea/metformin therapy reveals additive effects on mortality. It is concluded that(1) four of the five oral antidiabetic drug groups present proven or potential cardiac hazards;(2) these hazards are not mere "side effects", but are deeply rooted in the drugs' mechanism of action;(3) current data indicate that the combined glibenclamide/metformin therapy seems to present special risk and should be avoided in the long-term management of type 2 diabetics with proven CAD; and(4) customized antihyperglycemic pharmacological approaches should be investigated for optimal treatment of diabetic patients with heart disease.

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Section: Future Research Pathsmentioning

confidence: 99%

Oral Antidiabetic Therapy in Patients with Heart Disease

Fisman

Tenenbaum

Motro

et al. 2004

Herz

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“…Early steps in improving oral absorption involved co-administration/co-formulation of proteins with protease inhibitors, such as sodium glycocholate, aprotinin, bacitracin, soybean trypsin inhibitor, camostat mesilate [54,55] and absorption enhancers such as bile salts, salicylates, surfactants and chelating agents [56,57]. However, these were found to have deleterious effects on the GI tract wall, on normal digestion and the pancreas itself [1,3-7,9,10].…”

Section: Technologies To Facilitate Oral Protein Deliverymentioning

confidence: 99%

The Oral Delivery of Proteins Using Interpolymer Polyelectrolyte Complexes

Thompson¹,

Ibie

2011

Therapeutic Delivery

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In spite of the numerous barriers inherent in the oral delivery of therapeutically active proteins, research into the development of functional protein-delivery systems is still intense. The effectiveness of such oral protein-delivery systems depend on their ability to protect the incorporated protein from proteolytic degradation in the GI tract and enhance its intestinal absorption without significantly compromising the bioactivity of the protein. Among these delivery systems are polyelectrolyte complexes (PECs) which are composed of polyelectrolyte polymers complexed with a protein via coulombic and other interactions. This review will focus on the current status of PECs with a particular emphasis on the potential and limitations of multi- or inter-polymer PECs used to facilitate oral protein delivery.

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“…Another strategy for permeation enhancement involves the co-delivery of detergent-like or lipid-based molecules, such as the salts of fatty acids, pluronic acid, or small molecule hydrophobic compounds [98][99][100][101]. These agents can act either by directly increasing the permeability of cell membranes, thus enhancing epithelial cell uptake of the biologic, or by destabilizing the tight junctions between cells in the epithelial layer, thus increasing paracellular absorption of the drug.…”

Section: Co-delivery Of Modulatory Agents To Improve Absorption From mentioning

confidence: 99%

Routes of Delivery for Biological Drug Products

Irvine¹,

Su²,

Kwong³

2013

Pharmaceutical Sciences Encyclopedia

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Unlike conventional small‐molecule drugs, many of which can be formulated effectively with excipients to avoid degradation in the stomach and which exhibit reasonably efficient uptake through the gastrointestinal tract, biological drugs may exhibit lower stability and a greater sensitivity to enzymatic degradation, making oral delivery problematic. Thus, the majority of biologics are currently administered through subcutaneous/intramuscular injection or via intravenous infusion. Recent advances in delivery of traditional biologics include methods to increase the acceptable volume of drug solutions that can be administered subcutaneously.In addition, a number of alternative routes of administration for biologic drug products are being intensively investigated at the preclinical and clinical stages, such as intranasal, pulmonary, transcutaneous, and other routes, with some first examples of products recently licensed.This chapter will review current methods in use for marketed biologics and advanced approaches undergoing clinical testing.

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Enhanced oral absorption of insulin from desolvated fatty acid-sodium glycocholate emulsions

Cited by 61 publications

References 9 publications

Oral Antidiabetic Therapy in Patients with Heart Disease

Oral Antidiabetic Therapy in Patients with Heart Disease

The Oral Delivery of Proteins Using Interpolymer Polyelectrolyte Complexes

Routes of Delivery for Biological Drug Products

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