Gastrointestinal Responsive Polymeric Nanoparticles for Oral Delivery of Insulin: Optimized Preparation, Characterization, and In Vivo Evaluation

Research output: Contribution to journal › Journal article › Research › peer-review

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Gastrointestinal Responsive Polymeric Nanoparticles for Oral Delivery of Insulin: Optimized Preparation, Characterization, and In Vivo Evaluation. / Fang, Yan; Wang, Qi; Lin, Xiaojie; Jin, Xuechao; Yang, Dongjuan; Gao, Shan; Wang, Xiyan; Yang, Mingshi; Shi, Kai.

In: Journal of Pharmaceutical Sciences, Vol. 108, No. 9, 01.09.2019, p. 2994–3002.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Fang, Y, Wang, Q, Lin, X, Jin, X, Yang, D, Gao, S, Wang, X, Yang, M & Shi, K 2019, 'Gastrointestinal Responsive Polymeric Nanoparticles for Oral Delivery of Insulin: Optimized Preparation, Characterization, and In Vivo Evaluation', Journal of Pharmaceutical Sciences, vol. 108, no. 9, pp. 2994–3002. https://doi.org/10.1016/j.xphs.2019.04.020

APA

Fang, Y., Wang, Q., Lin, X., Jin, X., Yang, D., Gao, S., Wang, X., Yang, M., & Shi, K. (2019). Gastrointestinal Responsive Polymeric Nanoparticles for Oral Delivery of Insulin: Optimized Preparation, Characterization, and In Vivo Evaluation. Journal of Pharmaceutical Sciences, 108(9), 2994–3002. https://doi.org/10.1016/j.xphs.2019.04.020

Vancouver

Fang Y, Wang Q, Lin X, Jin X, Yang D, Gao S et al. Gastrointestinal Responsive Polymeric Nanoparticles for Oral Delivery of Insulin: Optimized Preparation, Characterization, and In Vivo Evaluation. Journal of Pharmaceutical Sciences. 2019 Sep 1;108(9):2994–3002. https://doi.org/10.1016/j.xphs.2019.04.020

Author

Fang, Yan ; Wang, Qi ; Lin, Xiaojie ; Jin, Xuechao ; Yang, Dongjuan ; Gao, Shan ; Wang, Xiyan ; Yang, Mingshi ; Shi, Kai. / Gastrointestinal Responsive Polymeric Nanoparticles for Oral Delivery of Insulin: Optimized Preparation, Characterization, and In Vivo Evaluation. In: Journal of Pharmaceutical Sciences. 2019 ; Vol. 108, No. 9. pp. 2994–3002.

Bibtex

@article{f830fc0b8dad47d3a51d9d70df87ff15,
title = "Gastrointestinal Responsive Polymeric Nanoparticles for Oral Delivery of Insulin: Optimized Preparation, Characterization, and In Vivo Evaluation",
abstract = "Gastrointestinal responsive polymeric nanospheres (NPs) based on hydroxypropyl methylcellulose phthalate were prepared using spontaneous emulsification solvent diffusion method for improved oral administration of insulin. The NPs prepared under optimized conditions have an encapsulation efficiency of 90% and a particle size of about 200 nm. In vitro drug release experiments demonstrated that the NPs exhibited a gradient release profile of loaded drug when the pH value gradually increased from 3.0 to 7.4. Enzyme resistance experiments showed that under simulated gastrointestinal conditions, the NPs protected more than 60% of the drug from being degraded by trypsin. The oral hypoglycemic experiments revealed that insulin-loaded NPs could significantly reduce blood glucose levels in diabetic rats with a relative bioavailability of 8.6%. Ex vivo imaging investigation of rat tissues showed that the drug-loaded NPs could promote the absorption of insulin in the ileum and colon. The work described here suggests that the gastrointestinal responsive polymeric NPs may be promising candidates for improving gastrointestinal tract delivery of hydrophilic biomacromolecules. Accordingly, the results indicated that hydroxypropyl methylcellulose phthalate NPs with gastrointestinal stimuli responsiveness could be a promising candidate for oral insulin delivery.",
keywords = "absorption, insulin, nanospheres, oral drug delivery, physical characterization",
author = "Yan Fang and Qi Wang and Xiaojie Lin and Xuechao Jin and Dongjuan Yang and Shan Gao and Xiyan Wang and Mingshi Yang and Kai Shi",
year = "2019",
month = sep,
day = "1",
doi = "10.1016/j.xphs.2019.04.020",
language = "English",
volume = "108",
pages = "2994–3002",
journal = "Journal of Pharmaceutical Sciences",
issn = "0022-3549",
publisher = "Elsevier",
number = "9",

}

RIS

TY - JOUR

T1 - Gastrointestinal Responsive Polymeric Nanoparticles for Oral Delivery of Insulin: Optimized Preparation, Characterization, and In Vivo Evaluation

AU - Fang, Yan

AU - Wang, Qi

AU - Lin, Xiaojie

AU - Jin, Xuechao

AU - Yang, Dongjuan

AU - Gao, Shan

AU - Wang, Xiyan

AU - Yang, Mingshi

AU - Shi, Kai

PY - 2019/9/1

Y1 - 2019/9/1

N2 - Gastrointestinal responsive polymeric nanospheres (NPs) based on hydroxypropyl methylcellulose phthalate were prepared using spontaneous emulsification solvent diffusion method for improved oral administration of insulin. The NPs prepared under optimized conditions have an encapsulation efficiency of 90% and a particle size of about 200 nm. In vitro drug release experiments demonstrated that the NPs exhibited a gradient release profile of loaded drug when the pH value gradually increased from 3.0 to 7.4. Enzyme resistance experiments showed that under simulated gastrointestinal conditions, the NPs protected more than 60% of the drug from being degraded by trypsin. The oral hypoglycemic experiments revealed that insulin-loaded NPs could significantly reduce blood glucose levels in diabetic rats with a relative bioavailability of 8.6%. Ex vivo imaging investigation of rat tissues showed that the drug-loaded NPs could promote the absorption of insulin in the ileum and colon. The work described here suggests that the gastrointestinal responsive polymeric NPs may be promising candidates for improving gastrointestinal tract delivery of hydrophilic biomacromolecules. Accordingly, the results indicated that hydroxypropyl methylcellulose phthalate NPs with gastrointestinal stimuli responsiveness could be a promising candidate for oral insulin delivery.

AB - Gastrointestinal responsive polymeric nanospheres (NPs) based on hydroxypropyl methylcellulose phthalate were prepared using spontaneous emulsification solvent diffusion method for improved oral administration of insulin. The NPs prepared under optimized conditions have an encapsulation efficiency of 90% and a particle size of about 200 nm. In vitro drug release experiments demonstrated that the NPs exhibited a gradient release profile of loaded drug when the pH value gradually increased from 3.0 to 7.4. Enzyme resistance experiments showed that under simulated gastrointestinal conditions, the NPs protected more than 60% of the drug from being degraded by trypsin. The oral hypoglycemic experiments revealed that insulin-loaded NPs could significantly reduce blood glucose levels in diabetic rats with a relative bioavailability of 8.6%. Ex vivo imaging investigation of rat tissues showed that the drug-loaded NPs could promote the absorption of insulin in the ileum and colon. The work described here suggests that the gastrointestinal responsive polymeric NPs may be promising candidates for improving gastrointestinal tract delivery of hydrophilic biomacromolecules. Accordingly, the results indicated that hydroxypropyl methylcellulose phthalate NPs with gastrointestinal stimuli responsiveness could be a promising candidate for oral insulin delivery.

KW - absorption

KW - insulin

KW - nanospheres

KW - oral drug delivery

KW - physical characterization

UR - http://www.mendeley.com/research/gastrointestinal-responsive-polymeric-nanoparticles-oral-delivery-insulin-optimized-preparation-char

U2 - 10.1016/j.xphs.2019.04.020

DO - 10.1016/j.xphs.2019.04.020

M3 - Journal article

C2 - 31047941

VL - 108

SP - 2994

EP - 3002

JO - Journal of Pharmaceutical Sciences

JF - Journal of Pharmaceutical Sciences

SN - 0022-3549

IS - 9

ER -

ID: 229562163