Abstract
Purpose: With the increase of population aging and the proportion of overweight and obese, a growing number of people are suffering from diabetes. Insulin (INS) as the most widely used hypoglycemic agent was always chosen as the most effective treatment method of diabetes. In this study, fumaryl diketopiperazine (FDKP) was used as a carrier for the pulmonary delivery of insulin.Patients and methods: The INS-loaded FDKP microspheres (INS@FDKP-MPs) were prepared by spray drying and physicochemical properties (drug loading, particle size, flowability, moisture content, morphology, and crystalline state) were further investigated. Pharmacodynamics was investigated on diabetic model rats administrated by intratracheal insufflation.Results: The INS-loaded FDKP microspheres show satisfied flowability and in vitro deposition with FPF 50.2% and MMAD 3.45 ± 0.13 μm, and the blood glucose level was significantly decreased. Moreover, no inflammatory reaction was observed during the safety study.Conclusion: To sum up, the aim was to develop a non-injection system for insulin, INS@FDKP-MPs powder inhalation with high dose, low toxicity, and good lung deposition inhalation could rapidly decrease the blood glucose level without immune stimulation, which shows remarkably potential on diabetes treatment by pulmonary delivery route.
Highlights
Diabetes mellitus is a common endocrine and metabolic disease caused by the lack of insulin secretion in the body, leading to disorders of protein and fat metabolism caused by hyperglycemia (Olivera et al, 1996)
Compared with AfrezzaVR, this paper aims to optimize the preparation process of INS@fumaryl diketopiperazine (FDKP)-MPs by adopting a simpler and more convenient synthesis method to reduce the production cost, and by evaluating the properties of INS@FDKP-MPs, it is intended to construct an inhalable insulin preparation that is qualified in particle size, drug loading, hypoglycemic effect, and safety
The preparation process of INS@FDKP-MPs was optimized and the insulin entrapment rate was higher than 95% with drug loading about 13%, which indicate that FDKP has a large enough loading capacity as a drug carrier for inhalation
Summary
Diabetes mellitus is a common endocrine and metabolic disease caused by the lack of insulin secretion in the body, leading to disorders of protein and fat metabolism caused by hyperglycemia (Olivera et al, 1996). Patients with type 1 or type 2 diabetes mellitus always require insulin therapy to control the Supplemental data for this article can be accessed here.
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