Optimization of Linagliptin-loaded polymersomes via response surface methodology: A repurposed therapeutic strategy for hepatic encephalopathy prevention

dc.AffiliationOctober University for modern sciences and Arts MSA
dc.contributor.authorNabila M. Sweed
dc.contributor.authorHeba T. Elbalkiny
dc.contributor.authorEslam Magdy
dc.contributor.authorMahitab Ramadan
dc.contributor.authorShahin Mahmoud
dc.contributor.authorToka Mohamed
dc.contributor.authorIslam S. Mannaa
dc.contributor.authorMai A. Zaafan
dc.date.accessioned2025-04-12T08:29:01Z
dc.date.available2025-04-12T08:29:01Z
dc.date.issued2025-03-28
dc.descriptionSJR 2024 0.817 Q1 H-Index 89
dc.description.abstractThis study aims to prepare linagliptin-loaded polymersomes in order to enhance its stability, bioavailability, and to investigate its potential in the prophylaxis against hepatic encephalopathy (HE). Polymersomes were formulated using solvent injection technique and optimized using D-optimal design, where the effect of drug to polymer ratio (X1) and polymer type, whether Poly (D, L-lactic-co-glycolide) or polycaprolactone (X2) were studied. Fifteen formulae were prepared and evaluated for entrapment efficiency % (Y1), particle size (Y2), and zeta potential (Y3). The optimized formula was prepared using polycaprolactone polymer with a drug to polymer ratio of 1:8.9. The optimized formula showed an entrapment efficiency % of 73 ± 1.04 %, a particle size of 184.1 ± 1.45 nm, and a zeta potential of − 21.2 ± 0.97 mV. In-vitro drug release showed remarkable sustained release profile for linagliptin-loaded polymersomes as compared to the standard linagliptin. In-vivo pharmacokinetic studies in rats showed a 262 % increase in bioavailability of linagliptin-loaded polymersomes. Moreover, linagliptin-loaded polymersomes showed promising results in a rat model of hepatic encephalopathy, with marked improvement in markers such as alanine transaminase (ALT), aspartate aminotransferase (AST), ammonia levels, and hippocampus brain-derived neurotrophic factor levels (BDNF). Our results showed that the optimized linagliptin-loaded polymersomes formula is a promising drug delivery system for enhancing linagliptin bioavailability, offering potential therapeutic benefits for managing HE and other diseases requiring sustained release and enhanced bioavailability.
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=22204&tip=sid&clean=0#google_vignette
dc.identifier.citationSweed, N. M., Elbalkiny, H. T., Magdy, E., Ramadan, M., Mahmoud, S., Mohamed, T., Mannaa, I. S., & Zaafan, M. A. (2025). Optimization of Linagliptin-Loaded polymersomes via response surface Methodology: A Repurposed therapeutic Strategy for Hepatic encephalopathy Prevention. Journal of Drug Delivery Science and Technology, 106855. https://doi.org/10.1016/j.jddst.2025.106855
dc.identifier.doihttps://doi.org/10.1016/j.jddst.2025.106855
dc.identifier.otherhttps://doi.org/10.1016/j.jddst.2025.106855
dc.identifier.urihttps://repository.msa.edu.eg/handle/123456789/6376
dc.language.isoen_US
dc.publisherEditions de Sante
dc.relation.ispartofseriesJournal of Drug Delivery Science and Technology ; Volume 108 , June 2025 , Article number 106855
dc.subjectHepatic encephalopathy
dc.subjectLinagliptin
dc.subjectPolymersomes
dc.titleOptimization of Linagliptin-loaded polymersomes via response surface methodology: A repurposed therapeutic strategy for hepatic encephalopathy prevention
dc.typeArticle

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