Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation

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 dik...

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Main Authors: Yun Xia, Yipeng Su, Qiyue Wang, Chen Yang, Baoqiang Tang, Yue Zhang, Jiasheng Tu, Yan Shen
Format: Article
Language:English
Published: Taylor & Francis Group 2019-01-01
Series:Drug Delivery
Subjects:
Online Access:http://dx.doi.org/10.1080/10717544.2019.1631408
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author Yun Xia
Yipeng Su
Qiyue Wang
Chen Yang
Baoqiang Tang
Yue Zhang
Jiasheng Tu
Yan Shen
author_facet Yun Xia
Yipeng Su
Qiyue Wang
Chen Yang
Baoqiang Tang
Yue Zhang
Jiasheng Tu
Yan Shen
author_sort Yun Xia
collection DOAJ
description 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.
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spelling doaj.art-57f7fac78be043a8929053c75c70c8e92022-12-22T00:05:29ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642019-01-0126165066010.1080/10717544.2019.16314081631408Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalationYun Xia0Yipeng Su1Qiyue Wang2Chen Yang3Baoqiang Tang4Yue Zhang5Jiasheng Tu6Yan Shen7China Pharmaceutical UniversityChina Pharmaceutical UniversityChina Pharmaceutical UniversityChina Pharmaceutical UniversityChina Pharmaceutical UniversityChina Pharmaceutical UniversityChina Pharmaceutical UniversityChina Pharmaceutical UniversityPurpose: 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.http://dx.doi.org/10.1080/10717544.2019.1631408insulinfdkpdiabeticinhalationpharmacodynamic
spellingShingle Yun Xia
Yipeng Su
Qiyue Wang
Chen Yang
Baoqiang Tang
Yue Zhang
Jiasheng Tu
Yan Shen
Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation
Drug Delivery
insulin
fdkp
diabetic
inhalation
pharmacodynamic
title Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation
title_full Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation
title_fullStr Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation
title_full_unstemmed Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation
title_short Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation
title_sort preparation characterization and pharmacodynamics of insulin loaded fumaryl diketopiperazine microparticle dry powder inhalation
topic insulin
fdkp
diabetic
inhalation
pharmacodynamic
url http://dx.doi.org/10.1080/10717544.2019.1631408
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