Optimum formulation for sustained-release insulin

Takenaga, Mitsuko; Yamaguchi, Yoko; Kitagawa, Aki; Ogawa, Yasuaki; Kawai, Shinichi; Mizushima, Yutaka; Igarashi, Rie

doi:10.1016/j.ijpharm.2003.10.027

Cited by 33 publications

(16 citation statements)

References 10 publications

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“…NIH 3T3 mouse fibroblasts have few endogenous insulin receptors and are insensitive to insulin but express insulin-like growth factor (IGF)-receptors and are responsive to IGF-1. 24 Insulin and IGF regulate certain cellular functions via both overlapping receptor and postreceptor signaling pathways. 25 Therefore, we used these cells to test the biological activity of insulin extracted from Ins-S.O-Comp PLGA NPs and the composite microcapsules compared with that of normal insulin.…”

Section: Biological Activity Of Insulinmentioning

confidence: 99%

pH-sensitive poly(lactide-co-glycolide) nanoparticle composite microcapsules for oral delivery of insulin

Sun¹,

Liang²,

Yamamoto³

et al. 2015

IJN

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This study proposes a new concept of pH-sensitive poly(lactide-co-glycolide) (PLGA) nanoparticle composite microcapsules for oral delivery of insulin. Firstly, insulin–sodium oleate complex was prepared by the hydrophobic ion pairing method and then encapsulated into PLGA nanoparticles by the emulsion solvent diffusion method. In order to reduce the burst release of insulin from PLGA nanoparticles and deliver insulin to specific gastrointestinal regions, hence to enhance bioavailability of insulin, the PLGA nanoparticles were further encapsulated into Eudragit ® FS 30D to prepare PLGA nanoparticle composite microcapsules by organic spray-drying method. The preparation was evaluated in vitro and in vivo, and the absorption mechanism was discussed. The in vitro drug release studies revealed that the drug release was pH dependent, and the in vivo results demonstrated that the formulation of PLGA nanoparticle composite microcapsules was an effective candidate for oral insulin delivery.

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Section: Biological Activity Of Insulinmentioning

confidence: 99%

pH-sensitive poly(lactide-co-glycolide) nanoparticle composite microcapsules for oral delivery of insulin

Sun¹,

Liang²,

Yamamoto³

et al. 2015

IJN

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show abstract

“…NIH 3T3 mouse fibroblasts have few endogenous insulin receptors and are insensitive to insulin, but express IGF receptors and are responsive to IGF-1. 24 Both insulin and IGF regulate certain cellular functions via both overlapping receptor and postreceptor signaling pathways. 25 Therefore, we used these cells to test the biological activity of insulin extracted from Ins-SD-Comp and Ins-SD-Comp-PLGA nanoparticles compared with that of normal insulin.…”

Section: Biological Activity Of Insulinmentioning

confidence: 99%

Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin

Cui¹

2011

IJN

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Insulin was complexed with sodium deoxycholate to form an insulin-sodium deoxycholate complex (Ins-SD-Comp) using an hydrophobic ion pairing method in aqueous phase to enhance the liposolubility of insulin. In order to obtain the maximal complexation efficiency, the molar ratio of sodium deoxycholate to insulin was found. The zeta potential method was used to confirm the optimal ratio for formation of Ins-SD-Comp. The structural characteristics of Ins-SD-Comp were assessed using the Fourier transform infrared method. The apparent partition coefficient of insulin increased upon the formation of Ins-SD-Comp. Based on the preliminary study, Ins-SD-Comp was encapsulated into poly(lactide-co-glycolide) (PLGA) nanoparticles using an emulsion solvent diffusion method. The maximal encapsulation efficiency of Ins-SD-Comp into PLGA nanoparticles was 93.6% ± 2.81%, drug loading was about 4.8% ± 0.32%, and the mean diameter of the nanoparticles was 278 ± 13 nm. Biological activity and in vivo results revealed that the bioactivity of insulin was not destroyed during the preparation process. Ins-SD-Comp-loaded PLGA nanoparticles have the potential to reduce serum glucose levels and increase the oral bioavailability of insulin.

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“…Injectable microparticles from poly(D,L-lactide) (PLA) and poly(D,L-lactide-coglycolide) (PLGA) have been investigated for the delivery of insulin. [5][6][7][8][9] A high initial burst release was observed followed by a slow release over 1-2 weeks period. The release profile was affected by the addition of hydrophilic additives such as water and glycerol.…”

Section: Introductionmentioning

confidence: 95%

Controlled Delivery of Basal Insulin from Phase-Sensitive Polymeric Systems After Subcutaneous Administration: In Vitro Release, Stability, Biocompatibility, In Vivo Absorption, and Bioactivity of Insulin

Al-Tahami

Oak

Singh

2011

Journal of Pharmaceutical Sciences

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Optimum formulation for sustained-release insulin

Cited by 33 publications

References 10 publications

pH-sensitive poly(lactide-co-glycolide) nanoparticle composite microcapsules for oral delivery of insulin

pH-sensitive poly(lactide-co-glycolide) nanoparticle composite microcapsules for oral delivery of insulin

Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin

Controlled Delivery of Basal Insulin from Phase-Sensitive Polymeric Systems After Subcutaneous Administration: In Vitro Release, Stability, Biocompatibility, In Vivo Absorption, and Bioactivity of Insulin

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