[Drug discovery by formulation design and innovative drug delivery systems (DDS)]

Hiroaki Okada, Okada H
Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan · 2011 · doi:10.1248/yakushi.131.1271 · PMID:21881300
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This review highlights drug discovery advancements using formulation design and drug delivery systems for peptides and nucleotides, achieving sustained release and enhanced cellular delivery for various therapeutic applications.

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This review examines drug discovery strategies utilizing rational formulation design and innovative drug delivery systems for biomaterials like therapeutic peptides and nucleotides. It highlights the development of PLGA microcapsules containing the LH-RH superagonist leuprorelin acetate, which enables long-term sustained release over one to six months through a novel in-water drying method. The authors note that this technology significantly improves patient quality of life and clinical utility for treating hormone-dependent conditions by facilitating easier administration. Relevance to endometriosis: listed as one indication for GnRH agonists via sustained-release microcapsules, though the paper's main focus is broader drug delivery innovations.

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Abstract

This review describes studies on drug discovery using a rational formulation design and innovative, drug delivery systems (DDS) for biomaterials such as therapeutic peptides and nucleotides. The microcapsules of the LH-RH superagonist leuprorelin acetate prepared using the new in-water drying method and biodegradable polymers, such as PLGA and PLA, could achieve a long-term sustained release for 1-6 months thereby facilitating easily treatment of hormone-dependent diseases, prostate cancer, endometriosis, and precocious puberty. This DDS technology showed an improvement in patient QOL and highly promoted the clinical value of the agonist. Moreover, PLGA microcapsules of siRNAs against VEGF, cFLIP, Raf-1, and Int6 have also been developed to treat various cancers and arteriosclerosis obliterans. To develop therapeutic nucleotides, a particle design is created using functional peptides, such as cell penetrating peptides (CPP), nuclear localizing signals (NLS), tight junction reversible openers (AT1002), bombesin, and dynein light chain-associated sequences. siRNA use should lead to a paradigm shift in drug discovery against various diseases. Tat analog with NLS could enhance the potency of a vaginal DNA vaccine. The artificial Tat CPP of STR-CH(2)R(4)H(2)C synthesized in our laboratory could efficiently deliver siRNAs into many types of cells and enhance the therapeutic effects for treating sarcoma, atopic dermatitis, allergic rhinitis, and asthma by intratumor injection and inhalation of the nanoparticles. Tat and AT1002 analogs used to treat atopic dermatitis in mice increased cell membrane permeability to siRelA, a siRNA against a subclass of NF-κB, and exhibited striking therapeutic and preventive effects.
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総説 製剤設計及び革新的薬物送達システム（DDS）による創薬 2011 年 131 巻 9 号 p. 1271-1287 詳細 抄録 This review describes studies on drug discovery using a rational formulation design and innovative, drug delivery systems (DDS) for biomaterials such as therapeutic peptides and nucleotides. The microcapsules of the LH-RH superagonist leuprorelin acetate prepared using the new in-water drying method and biodegradable polymers, such as PLGA and PLA, could achieve a long-term sustained release for 1-6 months thereby facilitating easily treatment of hormone-dependent diseases, prostate cancer, endometriosis, and precocious puberty. This DDS technology showed an improvement in patient QOL and highly promoted the clinical value of the agonist. Moreover, PLGA microcapsules of siRNAs against VEGF, cFLIP, Raf-1, and Int6 have also been developed to treat various cancers and arteriosclerosis obliterans. To develop therapeutic nucleotides, a particle design is created using functional peptides, such as cell penetrating peptides (CPP), nuclear localizing signals (NLS), tight junction reversible openers (AT1002), bombesin, and dynein light chain-associated sequences. siRNA use should lead to a paradigm shift in drug discovery against various diseases. Tat analog with NLS could enhance the potency of a vaginal DNA vaccine. The artificial Tat CPP of STR-CH2R4H2C synthesized in our laboratory could efficiently deliver siRNAs into many types of cells and enhance the therapeutic effects for treating sarcoma, atopic dermatitis, allergic rhinitis, and asthma by intratumor injection and inhalation of the nanoparticles. Tat and AT1002 analogs used to treat atopic dermatitis in mice increased cell membrane permeability to siRelA, a siRNA against a subclass of NF-κB, and exhibited striking therapeutic and preventive effects. © 2011 by the PHARMACEUTICAL SOCIETY OF JAPAN

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Condition tags

endometriosis

MeSH descriptors

Chemistry, Pharmaceutical Drug Delivery Systems Drug Delivery Systems Drug Design Drug Discovery Drug Discovery Drug Discovery Nucleotides Peptides Animals Capsules Delayed-Action Preparations Humans Leuprolide Mice Nanoparticles Nuclear Localization Signals Oligopeptides RNA, Small Interfering

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