Abstract: Atrial naturiuretic factor (ANF) is encapsulated within hollow acidic proteinoid microspheres which are stable and protective in the acidic stomach of a mammal but which dissolve at the near neutral pH of the blood. Microspheres having diameters of less than about 10 microns readily penetrate the gastrointestinal mucosa and release the ANF in the bloodstream in physiologically active form. Such gastric administration significantly extends the period of effectiveness of ANF as a diuretic and blood pressure suppressant.

Abstract: Substantially anhydrous pharmacological agents microencapsulated within protective hollow proteinoid microspheres are produced by contacting an aqueous mixture of such agent with an insoluble proteinoid and lyophilizing the resulting microspheres. Such encapsulation and dehydration results in a free flowing powder that has a long shelf life under naturally occurring temperature conditions and that quickly reabsorbs water without damage to the capsular wall. Gastrointestinally labile or poorly absorbed agents, such as insulin, heparin or dopamine redox carrier system, which are so microencapsulated in protective microspheres are rapidly rehydrated by body fluids in the gastrointestinal tract. Those microspheres having a diameter of about 10 microns or less penetrate the gastrointestinal mucosa and release the agent into the bloodstream in physiologically active form.

Abstract: Methods are described for targeting the release of an active pharmacological agent in an animal by administering that agent encapsulated in proteinoid microspheres which are stable to the environment encountered from the point of introduction until they migrate to the targeted body organs, fluids or cells and are there unstable. Orally administered delivery systems for insulin, heparin and physostigmine utilize encapsulating microspheres which are predominantly of less than about 10 microns in diameter and pass readily through the gastrointestinal mucosa and which are made of an acidic proteinoid that is stable and unaffected by stomach enzymes and acid, but which releases the microencapsulated agent in pharmacologically active form in the near neutral blood stream. Basic proteinoid microspheres encapsulating a dopamine redox carrier system are administered in the weakly basic, where they are stable, and then enter the blood stream, where the encapsulated agent is similarly released.

Abstract: Microcapsules containing oil-based biologically active compounds which are stable over extended time periods for release of the encapsulated compound in the intestine. There are a number of biologically active compounds having an oil base which must be orally ingested in order to have a beneficial effect. An example of one such biologically active oil-based compound is a fish oil having a high content of polyunsaturated omega-3 fatty acids which has been demonstrated to reduce plasma levels of triglycerides, very low density lipoprotein, low density lipoproteins and cholesterol in normal and hyperlipidemic subjects. The disclosed microcapsules eliminate the unfortunate problems of the unpleasant taste and smell of the fish oil, as well as the aftertaste, particularly when ingested in large quantities, and provide a palatable and practical means of ingesting efficacious quantities of fish oil. In addition, the normal oxidation of polyunsaturated fatty acids is inhibited.