LAPSE:2021.0313
Published Article
LAPSE:2021.0313
Insulin Release from NPH Insulin-Loaded Pluronic® F127 Hydrogel in the Presence of Simulated Tissue Enzyme Activity
Muhammad H. Sultan, Wael A. Mahdi, Young M. Kwon
April 30, 2021
Background: Despite the widespread use of newer basal insulins, Natural Protamine Hagedorn (NPH) insulin still represents a well-established basal formulation with its long history of use, featuring the native form of human insulin. However, NPH insulin exhibits an undesirable peak within hours after a single subcutaneous (s.c.) injection, which may lead to hypoglycemia followed by insufficient basal insulin delivery. This may be attributed to the s.c. enzyme activities degrading the protamine in NPH microcrystals. Methods: A thermogelling block copolymer Pluronic® F127 (PF127) was utilized as a protective carrier for NPH microcrystals and as a modulator for insulin release from NPH. NPH insulin-loaded PF127 gel was prepared with varying concentrations of the polymer (15−25%) under mild conditions. The formulations were characterized for their gelling temperature, morphology, gel erosion, and in vitro insulin release, with trypsin concentrations up to 5 U/mL. Results: Scanning electron microscopy (SEM) showed that the integrity of NPH microcrystals was maintained after preparation. The burst release of insulin from NPH was significantly attenuated over the course of ~16h in the presence of PF127 with or without enzyme activity. Conclusion: NPH-PF127 successfully resisted the acceleration of NPH crystal dissolution and insulin release in vitro in the presence of protamine-degrading enzyme activity, warranting further testing.
Keywords
drug release, insulin, protein delivery, thermosensitive polymers, tissue enzymes
Subject
Suggested Citation
Sultan MH, Mahdi WA, Kwon YM. Insulin Release from NPH Insulin-Loaded Pluronic® F127 Hydrogel in the Presence of Simulated Tissue Enzyme Activity. (2021). LAPSE:2021.0313
Author Affiliations
Sultan MH: Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan 45142, Saudi Arabia; Department of Pharmaceutical Sciences, College of Pharmacy, Nova Southeastern University, Fort Lauderdale, FL 33314, USA
Mahdi WA: Department of Pharmaceutical Sciences, College of Pharmacy, Nova Southeastern University, Fort Lauderdale, FL 33314, USA; Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
Kwon YM: Department of Pharmaceutical Sciences, College of Pharmacy, Nova Southeastern University, Fort Lauderdale, FL 33314, USA
Journal Name
Processes
Volume
8
Issue
10
Article Number
E1320
Year
2020
Publication Date
2020-10-21
Published Version
ISSN
2227-9717
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Original Submission
Other Meta
PII: pr8101320, Publication Type: Journal Article
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LAPSE:2021.0313
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doi:10.3390/pr8101320
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Apr 30, 2021
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CC BY 4.0
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Apr 30, 2021
 
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Apr 30, 2021
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https://psecommunity.org/LAPSE:2021.0313
 
Original Submitter
Calvin Tsay
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