Nanoparticles and microparticles, as well as pharmaceutical preparations thereof, have been designed to contain conjugates of active substances, such as therapeutic agents, prophylactics, or diagnostic agents, which are connected to a targeted part, such as a somatostatin receptor binding part, via a connector. These nanoparticles and microparticles can provide improved space-time delivery of active substances and / or improved biological distribution. Methods for preparing conjugates, granules and preparations thereof are provided. Methods for administering preparations to subjects in need, for example, to treat or prevent cancer or infectious diseases, are provided.已設計含有經由接頭連接至靶向部分(諸如生長激素抑制素受體結合部分)的活性物質(諸如治療劑、預防劑或診斷劑)的綴合物的納米顆粒和微粒及其藥物製劑。此類納米顆粒和微粒可提供改善的活性物質時空遞送和/或改善的生物分佈。提供製備綴合物、顆粒及其製劑的方法。提供向有需要的受試者施用製劑例如以治療或預防癌症或感染性疾病的方法。