Mono-lithocholated exendin-4-loaded glycol chitosan nanoparticles with prolonged antidiabetic effects

Sohee Son; Sung Mook Lim; Su Young Chae; Kwangmeyung Kim; Eun Ji Park; Kang Choon Lee; Dong Hee Na

doi:10.1016/j.ijpharm.2015.08.084

Mono-lithocholated exendin-4-loaded glycol chitosan nanoparticles with prolonged antidiabetic effects

Sohee Son, Sung Mook Lim, Su Young Chae, Kwangmeyung Kim, Eun Ji Park, Kang Choon Lee, Dong Hee Na

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

13 Scopus citations

Abstract

Hydrophobically modified glycol chitosan (HGC) nanoparticles loaded with mono-lithocholic acid-conjugated exendin-4 at the Lys²⁷ residue (LAM1-Ex4) were prepared and characterized by particle size measurement, proteolytic stability, in vitro drug-release profile, and in vivo antidiabetic effects in a db/db diabetic mouse model. Compared with Ex-4-loaded HGC nanoparticles (Ex4/HGC NPs) prepared as a control, LAM1-Ex4-loaded HGC nanoparticles (LAM1-Ex4/HGC NPs) showed improved drug-loading efficiency, small particle size, enhanced resistance against proteolytic digestion, and an extended in vitro drug release profile. These findings may be attributable to the strong hydrophobic interaction between LAM1-Ex4 and the inner core of HGC. Furthermore, LAM1-Ex4/HGC NPs showed prolonged hypoglycemic efficacy in db/db mice, lasting 1 week after a single subcutaneous administration. The present study demonstrated that LAM1-Ex4/HGC NPs have considerable potential as a long-acting sustained-release antidiabetic system for type 2 diabetes.

Original language	English
Pages (from-to)	81-86
Number of pages	6
Journal	International Journal of Pharmaceutics
Volume	495
Issue number	1
DOIs	https://doi.org/10.1016/j.ijpharm.2015.08.084
State	Published - 10 Nov 2015

Bibliographical note

Publisher Copyright:
© 2015 Elsevier B.V. All rights reserved.

Keywords

Antidiabetic effects
Exendin-4
Glycol chitosan
Lithocholic acid
Nanoparticles

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.ijpharm.2015.08.084

Cite this

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title = "Mono-lithocholated exendin-4-loaded glycol chitosan nanoparticles with prolonged antidiabetic effects",

abstract = "Hydrophobically modified glycol chitosan (HGC) nanoparticles loaded with mono-lithocholic acid-conjugated exendin-4 at the Lys27 residue (LAM1-Ex4) were prepared and characterized by particle size measurement, proteolytic stability, in vitro drug-release profile, and in vivo antidiabetic effects in a db/db diabetic mouse model. Compared with Ex-4-loaded HGC nanoparticles (Ex4/HGC NPs) prepared as a control, LAM1-Ex4-loaded HGC nanoparticles (LAM1-Ex4/HGC NPs) showed improved drug-loading efficiency, small particle size, enhanced resistance against proteolytic digestion, and an extended in vitro drug release profile. These findings may be attributable to the strong hydrophobic interaction between LAM1-Ex4 and the inner core of HGC. Furthermore, LAM1-Ex4/HGC NPs showed prolonged hypoglycemic efficacy in db/db mice, lasting 1 week after a single subcutaneous administration. The present study demonstrated that LAM1-Ex4/HGC NPs have considerable potential as a long-acting sustained-release antidiabetic system for type 2 diabetes.",

keywords = "Antidiabetic effects, Exendin-4, Glycol chitosan, Lithocholic acid, Nanoparticles",

author = "Sohee Son and Lim, {Sung Mook} and Chae, {Su Young} and Kwangmeyung Kim and Park, {Eun Ji} and Lee, {Kang Choon} and Na, {Dong Hee}",

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AU - Son, Sohee

AU - Lim, Sung Mook

AU - Chae, Su Young

AU - Kim, Kwangmeyung

AU - Park, Eun Ji

AU - Lee, Kang Choon

AU - Na, Dong Hee

PY - 2015/11/10

Y1 - 2015/11/10

N2 - Hydrophobically modified glycol chitosan (HGC) nanoparticles loaded with mono-lithocholic acid-conjugated exendin-4 at the Lys27 residue (LAM1-Ex4) were prepared and characterized by particle size measurement, proteolytic stability, in vitro drug-release profile, and in vivo antidiabetic effects in a db/db diabetic mouse model. Compared with Ex-4-loaded HGC nanoparticles (Ex4/HGC NPs) prepared as a control, LAM1-Ex4-loaded HGC nanoparticles (LAM1-Ex4/HGC NPs) showed improved drug-loading efficiency, small particle size, enhanced resistance against proteolytic digestion, and an extended in vitro drug release profile. These findings may be attributable to the strong hydrophobic interaction between LAM1-Ex4 and the inner core of HGC. Furthermore, LAM1-Ex4/HGC NPs showed prolonged hypoglycemic efficacy in db/db mice, lasting 1 week after a single subcutaneous administration. The present study demonstrated that LAM1-Ex4/HGC NPs have considerable potential as a long-acting sustained-release antidiabetic system for type 2 diabetes.

AB - Hydrophobically modified glycol chitosan (HGC) nanoparticles loaded with mono-lithocholic acid-conjugated exendin-4 at the Lys27 residue (LAM1-Ex4) were prepared and characterized by particle size measurement, proteolytic stability, in vitro drug-release profile, and in vivo antidiabetic effects in a db/db diabetic mouse model. Compared with Ex-4-loaded HGC nanoparticles (Ex4/HGC NPs) prepared as a control, LAM1-Ex4-loaded HGC nanoparticles (LAM1-Ex4/HGC NPs) showed improved drug-loading efficiency, small particle size, enhanced resistance against proteolytic digestion, and an extended in vitro drug release profile. These findings may be attributable to the strong hydrophobic interaction between LAM1-Ex4 and the inner core of HGC. Furthermore, LAM1-Ex4/HGC NPs showed prolonged hypoglycemic efficacy in db/db mice, lasting 1 week after a single subcutaneous administration. The present study demonstrated that LAM1-Ex4/HGC NPs have considerable potential as a long-acting sustained-release antidiabetic system for type 2 diabetes.

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KW - Glycol chitosan

KW - Lithocholic acid

KW - Nanoparticles

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Mono-lithocholated exendin-4-loaded glycol chitosan nanoparticles with prolonged antidiabetic effects

Abstract

Bibliographical note

Keywords

UN SDGs

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