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

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 effect...

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Main Authors: Susbin Raj Wagle, Bozica Kovacevic, Daniel Walker, Corina Mihaela Ionescu, Melissa Jones, Goran Stojanovic, Sanja Kojic, Armin Mooranian, Hani Al-Salami
Format: Article
Language:English
Published: MDPI AG 2020-07-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/12/8/708
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author Susbin Raj Wagle
Bozica Kovacevic
Daniel Walker
Corina Mihaela Ionescu
Melissa Jones
Goran Stojanovic
Sanja Kojic
Armin Mooranian
Hani Al-Salami
author_facet Susbin Raj Wagle
Bozica Kovacevic
Daniel Walker
Corina Mihaela Ionescu
Melissa Jones
Goran Stojanovic
Sanja Kojic
Armin Mooranian
Hani Al-Salami
author_sort Susbin Raj Wagle
collection DOAJ
description 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 <i>in vitro</i> (formulation study), and showed a promising effect in <i>ex vivo</i> study (<i>p</i> < 0.05), suggesting that ULCA can optimize the oral delivery of PB and support its potential application in diabetes treatment.
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spelling doaj.art-680e5aaa8bc54d529a5dc2a1caef4f672023-11-20T08:17:29ZengMDPI AGPharmaceutics1999-49232020-07-0112870810.3390/pharmaceutics12080708Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting FormulationsSusbin Raj Wagle0Bozica Kovacevic1Daniel Walker2Corina Mihaela Ionescu3Melissa Jones4Goran Stojanovic5Sanja Kojic6Armin Mooranian7Hani Al-Salami8Biotechnology and Drug Development Research Laboratory, School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth WA 6102, AustraliaBiotechnology and Drug Development Research Laboratory, School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth WA 6102, AustraliaBiotechnology and Drug Development Research Laboratory, School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth WA 6102, AustraliaBiotechnology and Drug Development Research Laboratory, School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth WA 6102, AustraliaBiotechnology and Drug Development Research Laboratory, School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth WA 6102, AustraliaFaculty of Technical Sciences, University of Novi Sad, Trg Dositeja Obradovica 6, 21000 Novi Sad, SerbiaFaculty of Technical Sciences, University of Novi Sad, Trg Dositeja Obradovica 6, 21000 Novi Sad, SerbiaBiotechnology and Drug Development Research Laboratory, School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth WA 6102, AustraliaBiotechnology and Drug Development Research Laboratory, School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth WA 6102, AustraliaBile 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 <i>in vitro</i> (formulation study), and showed a promising effect in <i>ex vivo</i> study (<i>p</i> < 0.05), suggesting that ULCA can optimize the oral delivery of PB and support its potential application in diabetes treatment.https://www.mdpi.com/1999-4923/12/8/708bile acidsdiabetes mellitusformulation sciencesinflammationprobucolunconjugated lithocholic acid
spellingShingle Susbin Raj Wagle
Bozica Kovacevic
Daniel Walker
Corina Mihaela Ionescu
Melissa Jones
Goran Stojanovic
Sanja Kojic
Armin Mooranian
Hani Al-Salami
Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations
Pharmaceutics
bile acids
diabetes mellitus
formulation sciences
inflammation
probucol
unconjugated lithocholic acid
title Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations
title_full Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations
title_fullStr Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations
title_full_unstemmed Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations
title_short Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations
title_sort pharmacological and advanced cell respiration effects enhanced by toxic human bile nano pharmaceuticals of probucol cell targeting formulations
topic bile acids
diabetes mellitus
formulation sciences
inflammation
probucol
unconjugated lithocholic acid
url https://www.mdpi.com/1999-4923/12/8/708
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