Multivesicular Liposomes for Glucose-Responsive Insulin Delivery

An intelligent insulin delivery system is highly desirable for diabetes management. Herein, we developed a novel glucose-responsive multivesicular liposome (MVL) for self-regulated insulin delivery using the double emulsion method. Glucose-responsive MVLs could effectively regulate insulin release i...

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Main Authors: Guangqu Liu, Suping He, Yu Ding, Cai Chen, Qingchun Cai, Wei Zhou
Format: Article
Language:English
Published: MDPI AG 2021-12-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/14/1/21
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author Guangqu Liu
Suping He
Yu Ding
Cai Chen
Qingchun Cai
Wei Zhou
author_facet Guangqu Liu
Suping He
Yu Ding
Cai Chen
Qingchun Cai
Wei Zhou
author_sort Guangqu Liu
collection DOAJ
description An intelligent insulin delivery system is highly desirable for diabetes management. Herein, we developed a novel glucose-responsive multivesicular liposome (MVL) for self-regulated insulin delivery using the double emulsion method. Glucose-responsive MVLs could effectively regulate insulin release in response to fluctuating glucose concentrations in vitro. Notably, in situ released glucose oxidase catalyzed glucose enrichment on the MVL surface, based on the combination of (3-fluoro-4-((octyloxy)carbonyl)phenyl)boronic acid and glucose. The outer MVL membrane was destroyed when triggered by the local acidic and H<sub>2</sub>O<sub>2</sub>-enriched microenvironment induced by glucose oxidase catalysis in situ, followed by the further release of entrapped insulin. Moreover, the Alizarin red probe and molecular docking were used to clarify the glucose-responsive mechanism of MVLs. Utilizing chemically induced type 1 diabetic rats, we demonstrated that the glucose-responsive MVLs could effectively regulate blood glucose levels within a normal range. Our findings suggest that glucose-responsive MVLs with good biocompatibility may have promising applications in diabetes treatment.
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spelling doaj.art-187163d0c90742cd8ebb55833ec00b5b2023-11-23T15:02:35ZengMDPI AGPharmaceutics1999-49232021-12-011412110.3390/pharmaceutics14010021Multivesicular Liposomes for Glucose-Responsive Insulin DeliveryGuangqu Liu0Suping He1Yu Ding2Cai Chen3Qingchun Cai4Wei Zhou5Department of Pharmaceutics, China Pharmaceutical University, Nanjing 211198, ChinaDepartment of Pharmaceutics, China Pharmaceutical University, Nanjing 211198, ChinaDepartment of Pharmaceutics, China Pharmaceutical University, Nanjing 211198, ChinaDepartment of Pharmaceutics, China Pharmaceutical University, Nanjing 211198, ChinaDepartment of Pharmaceutics, China Pharmaceutical University, Nanjing 211198, ChinaDepartment of Pharmaceutics, China Pharmaceutical University, Nanjing 211198, ChinaAn intelligent insulin delivery system is highly desirable for diabetes management. Herein, we developed a novel glucose-responsive multivesicular liposome (MVL) for self-regulated insulin delivery using the double emulsion method. Glucose-responsive MVLs could effectively regulate insulin release in response to fluctuating glucose concentrations in vitro. Notably, in situ released glucose oxidase catalyzed glucose enrichment on the MVL surface, based on the combination of (3-fluoro-4-((octyloxy)carbonyl)phenyl)boronic acid and glucose. The outer MVL membrane was destroyed when triggered by the local acidic and H<sub>2</sub>O<sub>2</sub>-enriched microenvironment induced by glucose oxidase catalysis in situ, followed by the further release of entrapped insulin. Moreover, the Alizarin red probe and molecular docking were used to clarify the glucose-responsive mechanism of MVLs. Utilizing chemically induced type 1 diabetic rats, we demonstrated that the glucose-responsive MVLs could effectively regulate blood glucose levels within a normal range. Our findings suggest that glucose-responsive MVLs with good biocompatibility may have promising applications in diabetes treatment.https://www.mdpi.com/1999-4923/14/1/21MVLglucose-responsiveinsulinin situ catalysisAlizarin red probemolecular docking
spellingShingle Guangqu Liu
Suping He
Yu Ding
Cai Chen
Qingchun Cai
Wei Zhou
Multivesicular Liposomes for Glucose-Responsive Insulin Delivery
Pharmaceutics
MVL
glucose-responsive
insulin
in situ catalysis
Alizarin red probe
molecular docking
title Multivesicular Liposomes for Glucose-Responsive Insulin Delivery
title_full Multivesicular Liposomes for Glucose-Responsive Insulin Delivery
title_fullStr Multivesicular Liposomes for Glucose-Responsive Insulin Delivery
title_full_unstemmed Multivesicular Liposomes for Glucose-Responsive Insulin Delivery
title_short Multivesicular Liposomes for Glucose-Responsive Insulin Delivery
title_sort multivesicular liposomes for glucose responsive insulin delivery
topic MVL
glucose-responsive
insulin
in situ catalysis
Alizarin red probe
molecular docking
url https://www.mdpi.com/1999-4923/14/1/21
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AT yuding multivesicularliposomesforglucoseresponsiveinsulindelivery
AT caichen multivesicularliposomesforglucoseresponsiveinsulindelivery
AT qingchuncai multivesicularliposomesforglucoseresponsiveinsulindelivery
AT weizhou multivesicularliposomesforglucoseresponsiveinsulindelivery