Abstract: A controlled release pharmaceutical formulation which comprises cyclosporin entrapped in a biodegradable polymer to form microspheres or nanospheres such that the cyclosporin is substantially in an amorphous state and the biodegradable polymer comprises greater than 12.5% w/w poly(lactide). The biodegradable polymer is suitably poly-D,L-lactide or a blend of poly-D,L-lactide and poly-D,L-lactide-co-glycolide. Additionally, an enteric coating can be applied to the microspheres or nanospheres or to the oral dosage form incorporating the microspheres or nanospheres to protect the formulation while it passes through the stomach. A particularly suitable formulation comprises 50% w/w cyclosporin-loaded 80:20 blend of poly-D,L-lactide-co-glycolide to poly-D,L-lactide micro- and/or nanospheres. This formulation has the combined properties of nearly complete but relatively slow release of cyclosporin within 8 hours and is useful for targeting cyclosporin to the small intestine when administered orally.

Abstract: A controlled release pharmaceutical formulation comprises nanoparticles formed of a biodegradable polycyanoacrylate polymer in which insulin is entrapped, the insulin being complexed to the polycyanoacrylate. These particles are capable of releasing bioactive insulin in vivo at a slower release rate than nanoparticles in which the insulin is free. The formulation may comprise a mixture of nanoparticles in which the insulin is free and nanoparticles in which it is complexed, so as to obtain the desired release profile. The nanoparticles have a preferred loading of 15-25% w/v insulin and a preferred size of 100-400 nm. Administration may be oral or parenteral, and for oral administration, an enteric coating may be provided to target release to the small intestine. Complexing of the insulin is achieved by the polymerisation of cyanoacrylate monomer in the presence of insulin at a low pH, preferably at about pH=2.

Abstract: An intradermal drug delivery device for delivering a liquid drug to a subject via the subject's skin includes a housing having a lower surface provided with an adhesive coating for adhering the housing to the subject's skin. An expansible-contractible chamber within the housing defines a reservoir which is expanded upon being filled with the drug and contracted to dispense the drug. A hollow needle extends through the lower surface of the housing and has an inner end which communicates with the reservoir and an outer end which projects outwardly of the housing a short distance to penetrate through the epidermis and into the dermis of the subject's skin when the housing is adhered thereto. The device permits delivery of drugs of relatively large molecular size and at slow rates which can be precisely controlled.

Abstract: An improved controlled release tablet formulation for the release of potassium chloride through a differentially permeable membrane from which the release of potassium chloride can be accurately controlled to minimize the likelihood of producing high localized concentrations of potassium within the gastrointestinal tract.