Development of the Composition and Technology for Obtaining a Model of an Injection Form of an Indolocarbazole Derivative

The indolocarbazole derivative LCS-1269 has a multitarget mechanism of action on tumors and blocks vasculogenic mimicry. The hydrophobic character of LCS-1269 hampers the development of an injectable dosage form (IDF), the need for which was determined in series of in vitro and in vivo biological experiments. The purpose of this study was to select an excipient composition for creating a model IDF of LCS-1269 with high antitumor activity and low toxicity and to develop the technology for LCS-1269 IDF production. Acomposition of a model IDF of LCS-1269 including EtOH (95%), Kollidon 17 PF, and polysorbate 80 and the technology for obtaining a true solution were developed during preliminary experimental studies. The selected model was lyophilized to exclude EtOH from the composition and to increase the shelf life of the compound.

Automated summary

The study aimed to select an excipient composition for creating an injectable dosage form (IDF) of LCS-1269 with high antitumor activity and low toxicity, and developed the technology for LCS-1269 IDF production.