Recent Advances in Oral Prodrug Discovery

摘要: Publisher Summary A number of new prodrug tactics have been devised to address issues associated with parent drugs or lead compounds, such as solubility, permeability, and tissue distribution. This chapter discusses prodrugs poorly soluble polar targeting active transporters, for targeted delivery. Compounds are considered be when their oral bioavailability is limited by the rate extent dissolution in gastrointestinal (GI) tract. typical strategy cases focuses on chemical derivatization improve water solubility. Highly polar, ionizable promoieties often required obtain an adequate level Prodrug compounds primarily directed toward increasing lipophilicity enhance passive transcellular absorption, while retaining acceptable Accordingly, design involves masking hydrogen-bonding groups appropriate promoieties. Mechanistic studies intestinal transepithelial transport revealed that absorption certain structural classes enhanced membrane-bound transporters. Such proteins include peptide amino acid nucleoside bile monocarboxylic One more recent endeavors field has selectively deliver principles target tissues. For this approach effective, must absorbed intact through mucosa, resistant metabolism enterocytes plasma, taken up reconverted parents