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Enhanced circulation longevity and pharmacodynamics of metformin from surface-modified nanostructured lipid carriers based on solidified reverse micellar solutions

Franklin Chimaobi Kenechukwu, God’spower Tochukwu Isaac, Daniel Okwudili Nnamani, Mumuni A. Momoh, Anthony A. Attama

2022Heliyon27 citationsDOIOpen Access PDF

Abstract

drug release was evaluated in phosphate buffered saline (PBS, pH 7.4). Antidiabetic and pharmacokinetics properties of the NLCs were ascertained in an alloxan-induced diabetic rats model after oral administration. The MTH-loaded NLCs were nanomeric (particle size: 184.8-882.50 nm) with low polydispersity index (0.368-0.687) and zeta potential (26.5-34.2 mV), irregular shape, amorphous nature with reduced crystallinity. The EE% and LC were >90 % and 16%, respectively. The formulations showed >65 % release over 12 h in a greater sustained manner than marketed MTH formulation (Glucophage®) as well as enhanced pharmacokinetics properties and sustained blood glucose lowering effect, even at reduced doses with PEGylated NLCs than Glucophage®. Thus, PEGylated NLC is a promising approach for improved delivery and oral bioavailability of MTH thus encouraging further development of the formulation.

Topics & Concepts

BioavailabilityPharmacokineticsZeta potentialChemistryPoloxamerPharmacologyChromatographyDispersityCrystallinityDrug deliveryMaterials scienceNuclear chemistryNanotechnologyNanoparticleOrganic chemistryMedicinePolymerCopolymerCrystallographyDrug Solubulity and Delivery SystemsAdvancements in Transdermal Drug DeliveryAdvanced Drug Delivery Systems
Enhanced circulation longevity and pharmacodynamics of metformin from surface-modified nanostructured lipid carriers based on solidified reverse micellar solutions | Litcius