Preparation and characterization of layer-by-layer hypoglycemic nanoparticles with pH-sensitivity for oral insulin delivery

2018 ◽  
Vol 6 (45) ◽  
pp. 7451-7461 ◽  
Author(s):  
Li Zhang ◽  
Han Qin ◽  
Jian Li ◽  
Jia-Ni Qiu ◽  
Jing-Min Huang ◽  
...  

We developed an insulin oral delivery system with the combination of pH-sensitive material and structure to avoid intestinal degradation.

Pharmaceutics ◽  
2019 ◽  
Vol 11 (1) ◽  
pp. 40 ◽  
Author(s):  
Ahmed Khames

Because Eplerenone (EPL) is a Biopharmaceutical Classification System (BCS) class-II drug and is prone to extensive liver degradation, it suffers from poor bioavailability after oral administration. This work aimed to prepare liquisolids loaded with EPL-nanoemulsions (EPL-NEs) that have a higher drug release rate and improved bioavailability by the oral route. Based on solubility studies, mixtures of Triacetin (oil) and Kolliphor EL/PEG 400 surfactant/co-surfactant (Smix) in different ratios were used to prepare EPL-NE systems, which were characterized and optimized for droplet size, zeta potential, polydispersity index (PDI), and drug content. Systems were then loaded onto liquisolid formulations and fully evaluated. A liquisolid formulation with better drug release and tableting properties was selected and compared to EPL-NEs and conventional EPL oral tablets in solid-state characterization studies and bioavailability studies in rabbits. Only five NEs prepared at 1:3, 1:2, and 3:1 Smix met the specified optimization criteria. The drug release rate from liquisolids was significantly increased (90% within 45 minutes). EPL-NE also showed significantly improved drug release but with a sustained pattern for four hours. Liquisolid bioavailability reached 2.1 and 1.2 relative to conventional tablets and EPL-NE. This suggests that the EPL-NE liquisolid is a promising oral delivery system with a higher drug release rate, enhanced absorption, decreased liver degradation, and improved bioavailability.


2011 ◽  
Vol 152 ◽  
pp. e184-e186 ◽  
Author(s):  
Li Zhao ◽  
Jianxun Ding ◽  
Pan He ◽  
Chunsheng Xiao ◽  
Zhaohui Tang ◽  
...  

2013 ◽  
Vol 456 (2) ◽  
pp. 459-472 ◽  
Author(s):  
Pierre P.D. Kondiah ◽  
Lomas K. Tomar ◽  
Charu Tyagi ◽  
Yahya E. Choonara ◽  
Girish Modi ◽  
...  

2007 ◽  
Vol 107 (2) ◽  
pp. 863-871 ◽  
Author(s):  
Amit Kumar ◽  
Sitanshu S. Lahiri ◽  
Supriya Punyani ◽  
Harpal Singh

2019 ◽  
Vol 22 ◽  
pp. 102091 ◽  
Author(s):  
Yingfang Fan ◽  
Harkiranpreet Kaur Dhaliwal ◽  
Archita Venugopal Menon ◽  
JuOae Chang ◽  
Jee Eun Choi ◽  
...  

2021 ◽  
Vol 11 (6) ◽  
pp. 194-208
Author(s):  
ADIVA PUJA KRISNA ◽  
Hendri Wahyu Ningrum ◽  
Tamara Laily Fimannuha ◽  
Oktavia Eka Puspita

Diabetes is a metabolic disease characterized by hyperglycemia due to impaired insulin secretion, insulin action, or both. All patients with type 1 diabetes and many type 2 diabetes require insulin therapy to achieve reasonable glycemic control. During this time, insulin is given through the subcutaneous injection route because it can be destroyed by gastric acid when given orally. Until now, many studies have developed oral insulin therapy using various delivery system strategies. This systematic literature review aims to answer several questions about the effect of technique and material on increasing oral insulin bioavailability and the best technique and type of material that can produce the best oral insulin bioavailability. We searched for published articles regarding the development of oral route insulin. Bioavailability parameters were assessed based on plasma insulin levels for relative bioavailability values and/or plasma glucose levels for pharmacological bioavailability values. Conclusion: The manufacturing technique in the delivery system affects insulin stability in maintaining its conformation to provide a therapeutic effect. The type of substance affects insulin bioavailability through its properties in paving the way for insulin across various barriers in the digestive tract. To date, the best results in the development of oral insulin have obtained oral insulin bioavailability of 73.10% achieved by mesoporous silica nanoparticles (MSN) delivery system with layer-by-layer technique coated with [poly (methacrylic acid-co-vinyl triethoxylsilane)] (PMV)]. Keywords: bioavailability, diabetes, insulin, nanoparticles, oral delivery system.


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