A novel insulin-sodium oleate complex for oral administration: preparation, characterization and in vivo evaluation

Sun, Song Yung; Cui, Fude; Kawashima, Yasunaru; Liang, Na; Zhang, L.; Shi, Kai; Yu, Yongbo

doi:10.1016/s1773-2247(08)50047-5

Cited by 21 publications

(12 citation statements)

References 20 publications

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“…Researchers have reported shiing the solution pH either up or down from 5.3 to deprotonate insulin's basic residues or protonate its acidic residues, respectively. 42,[49][50][51][52][53] With only one type of charge, the peptide can then be hydrophobically ion paired (Fig. 3).…”

Section: Thermodynamicsmentioning

confidence: 99%

Hydrophobic ion pairing: encapsulating small molecules, peptides, and proteins into nanocarriers

2019

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Section: Thermodynamicsmentioning

confidence: 99%

Hydrophobic ion pairing: encapsulating small molecules, peptides, and proteins into nanocarriers

2019

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“…Ins-S.O complex was prepared by a hydrophobic ion pairing method (Sun et al 2008). Briefly, various amounts of sodium oleate (S.O) were dissolved in 1 ml of HCl solution (pH ¼ 4.0), then the solution was slowly added in a dropwise manner into 4 ml of 1.0 mg/ml insulin solution (pH ¼ 4.0) under magnetic stirring.…”

Section: Preparation and Characterization Of Ins-so Complexmentioning

confidence: 99%

“…Due to the formation of Ins-S.O complex, the apparent solubility of insulin in organic phase evidently increased (Sun et al 2008). So it was much easier to prepare the nanoparticles via an emulsion solvent diffusion method.…”

Section: Preparation and Characterization Of Ins-so Complex-loaded Nmentioning

confidence: 99%

“…In order to encapsulate more insulin in the hydrophobic copolymer, the hydrophobic ion pairing (HIP) technique has been applied to prepare Ins-S.O complex to enhance the hydrophobicity of insulin in our previous work (Sun et al 2008). The technique of HIP is simply performed by the interaction between ionic protein at suitable pH and the opposite ionic head group of fatty acid, surface-active agents or other amphiphilic molecules.…”

Section: Introductionmentioning

confidence: 99%

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Insulin-S.O (sodium oleate) complex-loaded PLGA nanoparticles: Formulation, characterization andin vivoevaluation

Sun

Liang

Piao

et al. 2010

Journal of Microencapsulation

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S.O (sodium oleate) is an anionic surfactant, which is able to forman ionic complex with positively charged insulin at suitable pH. In a previous study, the insulin-S.O (Ins-S.O) complex was prepared by a hydrophobic ion pairing (HIP) method to improve the apparent liposolubility of insulin. The formation of the complex was further confirmed by Zeta potential and X-ray method. Based on the preliminary study, poly(lactide-co-glycolide) (PLGA) nanoparticles harbouring Ins-S.O complex was prepared via an emulsion solvent diffusion method. The effects of key parameters such as concentration of PVA, concentration of PLGA and initial-loaded drug on the properties of the nanoparticles were investigated. The insulin encapsulation efficiency (EE(%)) reached up to 91.2% and mean diameter of the nanoparticles was sized approximately 160 nm under optimal conditions. The pharmacological effects of the nanoparticles made of PLGA (75/25, Av Mw 15,000) were further evaluated to confirm their potential suitability for oral delivery. In order to evaluate hyperglycaemic effect of the nanoparticles for oral administration, Ins-S.O complex-loaded PLGA nanoparticles (20 IU/Kg) were administered orally by force-feeding to diabetic rats. In the case of the nanoparticles, the plasma glucose level reduced to 23.85% from the initial one 12 h post-administration and this continued for 24 h. The results showed that the use of Ins-S.O complex-loaded PLGA nanoparticles is an effective method of reducing plasma glucose levels. The insulin nanoparticles also improved the glycaemic response to an oral glucose challenge.

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“…It was reported that the hydrophobic ion pairing method can be used to enhance the hydrophobicity of protein/peptides. [12][13][14][15] This technique is simply performed by the interaction between ionic protein and the opposite ionic head group of fatty acid, surface-active agents or other amphiphilic molecules at suitable pH. In this study, sodium deoxycholate was chosen as the counterpart of insulin.…”

Section: Introductionmentioning

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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A novel insulin-sodium oleate complex for oral administration: preparation, characterization and in vivo evaluation

Cited by 21 publications

References 20 publications

Hydrophobic ion pairing: encapsulating small molecules, peptides, and proteins into nanocarriers

Hydrophobic ion pairing: encapsulating small molecules, peptides, and proteins into nanocarriers

Insulin-S.O (sodium oleate) complex-loaded PLGA nanoparticles: Formulation, characterization andin vivoevaluation

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

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