Folate targeted PEGylated liposomes for the oral delivery of insulin: In vitro and in vivo studies

被引：58

作者：

Yazdi, Jafar Rahnama ^{[1
,2
,3
]}

Tafaghodi, Mohsen ^{[2
,4
]}

Sadri, Kayvan ^{[5
]}

Mashreghi, Mohammad ^{[2
,4
]}

Nikpoor, Amin Reza ^{[6
]}

Nikoofal-Sahlabadi, Sara ^{[7
]}

Chamani, Jamshidkhan ^{[8
]}

Vakili, Rahim ^{[9
]}

Moosavian, Seyedeh Alia ^{[2
,4
]}

Jaafari, Mahmoud Reza ^{[1
,2
,4
]}

机构：

[1] Mashhad Univ Med Sci, Biotechnol Res Ctr, Pharmaceut Technol Inst, Mashhad 917751365, Razavi Khorasan, Iran

[2] Mashhad Univ Med Sci, Nanotechnol Res Ctr, Pharmaceut Technol Inst, Mashhad, Razavi Khorasan, Iran

[3] Mashhad Univ Med Sci, Sch Pharm, Dept Pharmaceut Biotechnol, Mashhad 917751365, Razavi Khorasan, Iran

[4] Mashhad Univ Med Sci, Sch Pharm, Dept Pharmaceut Nanotechnol, Mashhad 917751365, Razavi Khorasan, Iran

[5] Mashhad Univ Med Sci, Nucl Med Res Ctr, Mashhad, Razavi Khorasan, Iran

[6] Hormozgan Univ Med Sci, Mol Med Res Ctr, Hormozgan Hlth Inst, Bandar Abbas, Iran

[7] Hormozgan Univ Med Sci, Fac Pharm, Dept Pharmaceut, Bandar Abbas, Iran

[8] Islamic Azad Univ, Fac Sci, Dept Biol, Mashhad Branch, Mashhad 9187147578, Razavi Khorasan, Iran

[9] Mashhad Univ Med Sci, Imam Reza Hosp, Sch Med, Dept Pediat Endocrinol & Metab, Mashhad, Razavi Khorasan, Iran

来源：

COLLOIDS AND SURFACES B-BIOINTERFACES | 2020年 / 194卷

关键词：

Insulin; Liposomes; Targeted oral delivery; Folic acid; DRUG-DELIVERY; VITAMIN-B-12; PATHWAY; NANOPARTICLES; ABSORPTION; STABILITY; PROTEIN; BIOAVAILABILITY; PEPTIDE;

D O I：

10.1016/j.colsurfb.2020.111203

中图分类号：

Q6 [生物物理学];

学科分类号：

071011 ;

摘要：

In this study using phospholipids with high transition temperature and taking advantage of PEGylation, we designed liposomal formulation targeted with folic acid (FA) to improve the stability of liposomes with high penetration efficiency at the same time. The results of characterization demonstrated that liposomal formulations are in range of 150-210 nm size with negative surface charge. The results of cell uptake indicated that FA conjugation resulted in the more uptake of insulin. However, the results of transepithelial electrical resistance (TEER) showed no statistical differences among the formulations. The results of biodistribution also demonstrated that PEGylated liposome targeted with FA had more residence time in stomach and intestine along with higher amounts in blood and liver. The anti-diabetic effects of formulation in vivo indicated the efficacy of PEGylated liposome targeted with FA had promising results in decreasing blood glucose and increasing insulin levels. The results of this study indicated that using phospholipids with high Tm along with PEGylation and using targeting ligand could improve efficiency of oral delivery of liposomes which merit further investigation.

引用

页数：11

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