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Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations

Susbin Raj Wagle, Božica Kovačević, Daniel P. Walker, Corina Mihaela Ionescu, Melissa Jones, Goran M. Stojanović, Sanja Kojić, Armin Mooranian, Hani Al‐Salami

2020Pharmaceutics33 citationsDOIOpen Access PDF

Abstract

Bile acids have recently been studied for potential applications as formulation excipients and enhancers for drug release; however, some bile acids are not suitable for this application. Unconjugated lithocholic acid (ULCA) has recently shown drug formulation-stabilizing and anti-inflammatory effects. Lipophilic drugs have poor gut absorption after an oral dose, which necessitates the administration of high doses and causes subsequent side effects. Probucol (PB) is a highly lipophilic drug with poor oral absorption that resulted in restrictions on its clinical prescribing. Hence, this study aimed to design new delivery systems for PB using ULCA-based matrices and to test drug formulation, release, temperature, and biological effects. ULCA-based matrices were formulated for PB oral delivery by applying the jet-flow microencapsulation technique using sodium alginate as a polymer. ULCA addition to new PB matrices improved the microcapsule’s stability, drug release in vitro (formulation study), and showed a promising effect in ex vivo study (p < 0.05), suggesting that ULCA can optimize the oral delivery of PB and support its potential application in diabetes treatment.

Topics & Concepts

ProbucolPharmacologyChemistryDrugDrug deliveryIn vivoEx vivoAbsorption (acoustics)BioavailabilityIn vitroCholesterolBiochemistryMedicineMaterials scienceBiologyOrganic chemistryBiotechnologyComposite materialDrug Solubulity and Delivery SystemsNatural Antidiabetic Agents StudiesDrug Transport and Resistance Mechanisms
Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations | Litcius