Long-acting injection is a controlled release agent, which was designed that stable blood concentration is provided by giving it once in two to four weeks. Schizophrenia treatment is essential to long-term medication. So, LAI is one of the useful therapeutic strategies. Although traditional LAI had the strong negative impression to be forcibly used for the patients with the refusing medication and the lack of insight into disease, LAI of second-generation antipsychotics are expected to maintenance therapy for the outpatients with Schizophrenia. While psychiatric medical care is shifting from hospitalization to outpatient department, and a role of LAI is important in social rehabilitation. Here, we outline to the clinical importance, characteristic, and future challenge of LAI in psychiatric treatment.

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Considering the pathophysiology of inflammatory bowel disease (IBD), it would be ideal to develop drug delivery system (DDS) regulating mucosal immune system as therapeutic strategy for IBD.Development of DDS with polymeric materials such as biodegradable microspheres, which could carry drugs, anti-inflammatory cytokines and growth factors to targeted gastrointestinal tracts, would contribute to future treatment for IBD.

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Use of technologies on the skin-penetration enhancement is very important to apply many therapeutic drugs to transdermal drug delivery systems (TDDS). In addition, controlled release ability is also needed in the TDDS fabrication to have predetermined bioavailability and absorption rate of drugs. In this review, I introduce about 4 decades-history on TDDS and overall research on the chemical penetration-enhancers and physical means like iontophoresis and microneedles to increase skin permeation of drugs. Use of such penetration-enhancement methods leads to develop new TDDS having real controlled release ability of drugs. I also introduce new concept on the TDDS with internet of things (IoT). Such new TDDS IoT may be responsible for the center of the pharmaceutical formulations in the near future.

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Drug products with oral drug controlled release technology play a center role in the market of Drug Delivery System (DDS) and greatly contribute to drug therapy. Drug product functions from medical practices are being diversified. Therefore, demands for development of a wide variety of products in small quantities will be forecasted in the pharmaceutical sector. With advance in science, oral drug controlled release technology is being transformed from specialty to commodity. A variety type of oral drug controlled release technologies are found in the world. Bioequivalence to original oral drug controlled release products can be shown with the technologies. In the past, oral drug controlled release technologies have provided not only functional values based on pharmaceutical technologies but also customer values from user needs. Prolongation of pharmacological effect, reduction of dose frequency, prevention of the risk of adverse effects with steep drug absorption, and so on, have been considered as the conventional product values of oral drug controlled release technologies. For the future, novel product values should be alternatively created for oral drug controlled release technology in order to continue contribution to the drug therapy. In this report, current development of the oral drug controlled release formulations is overviewed. New product value creation with oral controlled release technology will be introduced in terms of drug abuse protection, adherence improvement, drug repositioning, and reformulation.

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Regenerative medicine is defined as an advanced medicine technology to enhance the natural-healing potential of body itself. The natural-healing potential is based on the cell ability for proliferation and differentiation. This cell-based regenerative medicine can be achieved only by enhancing the cell ability. Regenerative medicine is composed of two scientific fields, regenerative therapy and stem cell biology (regenerative research) which scientifically supports the therapy of next generation. For both the fields, it is practically indispensable to develop controlled release technology which can create the local environment of cells to enhance their tissue regeneration activity. This paper introduces the definition of drugs and their large contribution to advanced medicine.

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Cedartolen^® is the first product for sublingual immunotherapy in Japan. It was approved in 2014 as an allergen immunotherapy product which would provide cure for allergic patients. It has some characteristics such as sublingual administration rout, dose escalation manner for reducing allergic reaction and so on. Furthermore we achieved the development of the container to store allergen extract solution stable and to administrate it with dose escalation manner. We expect that much more Japanese cedar pollinosis patients receive Cedartolen^® treatment and they become relieved although three to five years treatment is required.

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We have developed the 3rd generation drug-eluting stent (DES), the Ultimaster sirolimus eluting coronary stent, in order to reduce the risk of late stent thrombosis and subsequently to shorten the dual anti-platelet therapy (DAPT) duration, because the DAPT is a critical issue on high bleeding risk patients or non-cardiac surgery. The mechanisms behind late stent thrombosis are multi-factorial, varying from factors such as stent malapposition to delayed endothelialization or endothelial dysfunction due to inflammation induced by polymer excipients. The Ultimaster DES is distinguished by the very flexible stent platform having thin-strut, in order to avoid stent malapposition, and also distinguished by the unique abluminal gradient coating which leaves the abluminal surface of the curves and link parts of the stent free from the drug and biodegradable polymer coating by gradually decreasing the coating layer thickness toward the hinge area, in order to accelerate endothelialization on the luminal surface and to avoid coating delamination. The biodegradable polymer, poly (D,L-lactide-co-caprolactone) was newly designed and developed as the excipients and adhesives, considering the drug release profile and the coating integrity. The drug, sirolimus, is released from the Ultimaster DES after implantation till 3 months, and the polymer is degraded and metabolized within 3-4 months, consequently only a bare metal stent leaves in the artery and the risk of late stent thrombosis can be minimized. The clinical trial data demonstrate the efficacy and safety of Ultimaster DES with non-inferiority to the 2nd generation DES and also corroborates the possibility of shortening the DAPT duration, with high endothelialization rate at 3 months after. The issue of the stent thrombosis will be solved in the near future by being introduced such 3rd generation DES and new anti-platelet agents into daily clinical practices. A new challenge to the remaining issue in DES, i.e. improvement of the long-term clinical outcomes, has already started with the development of bio-resorbable scaffolds.

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