The solid-state modification for solubility enhancement of practically insoluble glimepiride: A systematic review

Context: Solubility is a crucial physicochemical property of pharmaceuticals that directly influences the absorption and bioavailability of drugs within the human body. Glimepiride, an oral anti-diabetic agent included in the Biopharmaceutics Classification System (BCS) class II, is practically insoluble in water. Various solid-state modification techniques have been implemented to improve the solubility of glimepiride, namely by the formation of co-crystals, co-amorphous, inclusion complexes, and solid dispersions. Aims: To systematically review the enhancement of glimepiride solubility after solid-state modifications, including co-crystals, co-amorphous, inclusion complexes, and solid dispersions. Methods: This review followed the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) 2020 statement. The citation searches for records published in the last ten years from reputable journals. The eligibility criteria of the identified study are as follows: Population (P): Glimepiride is practically insoluble in water; Intervention (I): Solid-state modification of glimepiride includes co-crystals, co-amorphous, inclusion complexes, and solid dispersions; (C): Glimepiride raw material before solid-state modification; and Outcome (O): Solubility and dissolution enhancement. ADA tool was used to assess the quality of the records. Results: A total of 5,220 records were found. The duplicates and undesired articles were excluded. 14 relevant records were further identified through citation searching. The screening and exclusion of records based on the inclusion and exclusion criteria left 13 eligible studies. The studies show that solid-state modification, including co-crystals, amorphous, inclusion complexes, and solid dispersions, can enhance the solubility of practically insoluble glimepiride. Conclusions: Solid-state modification could improve the solubility and dissolution of glimepiride.