New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion Temperature Method

Quercetin (QCT), a natural flavonoid, is of research interest owing to its pharmacological properties. However, its pharmacokinetic limitations could hinder its widespread therapeutic use. Nanocarriers, especially solid lipid nanoparticles (SLNs), might overcome this constraint. This study aimed to...

Full description

Bibliographic Details
Main Authors: Yotsanan Weerapol, Suwisit Manmuan, Nattaya Chaothanaphat, Sontaya Limmatvapirat, Jitnapa Sirirak, Poomipat Tamdee, Sukannika Tubtimsri
Format: Article
Language:English
Published: MDPI AG 2022-09-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/14/10/1984
_version_ 1797470377763405824
author Yotsanan Weerapol
Suwisit Manmuan
Nattaya Chaothanaphat
Sontaya Limmatvapirat
Jitnapa Sirirak
Poomipat Tamdee
Sukannika Tubtimsri
author_facet Yotsanan Weerapol
Suwisit Manmuan
Nattaya Chaothanaphat
Sontaya Limmatvapirat
Jitnapa Sirirak
Poomipat Tamdee
Sukannika Tubtimsri
author_sort Yotsanan Weerapol
collection DOAJ
description Quercetin (QCT), a natural flavonoid, is of research interest owing to its pharmacological properties. However, its pharmacokinetic limitations could hinder its widespread therapeutic use. Nanocarriers, especially solid lipid nanoparticles (SLNs), might overcome this constraint. This study aimed to investigate QCT-loaded SLNs prepared via a new approach using a volatile oil. The phase-inversion temperature method was used to incorporate rosemary oil (RMO) into SLNs prepared using solid lipids possessing different chemical structures. Among the solid lipids used in the formulations, trilaurin (TLR) exhibited the smallest particle size and good stability after a temperature cycling test. SLNs prepared with a ratio of RMO to TLR of 1:3 could load QCT with an entrapment efficiency of >60% and drug loading of ~2% <i>w</i>/<i>w</i>. The smallest particle size was achieved using the polyoxyethylene-hydrogenated castor oil RH40, and the particle size depended on the concentration. The drug-release profile of QCT_TLR exhibited prolonged biphasic release for >24 h. QCT_TLR was a safe formulation, as indicated by a cell viability percentage of >75% at <2% <i>v</i>/<i>v</i>. In a computer simulation, the system with RMO enabled smaller sized SLNs than those without RMO. This new discovery shows great promise for producing SLNs via the phase-inversion temperature method with incorporation of volatile oil, particularly for delivering compounds with limited water solubility.
first_indexed 2024-03-09T19:36:40Z
format Article
id doaj.art-8765a89be0e34112bf1a7d0af02e6e29
institution Directory Open Access Journal
issn 1999-4923
language English
last_indexed 2024-03-09T19:36:40Z
publishDate 2022-09-01
publisher MDPI AG
record_format Article
series Pharmaceutics
spelling doaj.art-8765a89be0e34112bf1a7d0af02e6e292023-11-24T01:53:06ZengMDPI AGPharmaceutics1999-49232022-09-011410198410.3390/pharmaceutics14101984New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion Temperature MethodYotsanan Weerapol0Suwisit Manmuan1Nattaya Chaothanaphat2Sontaya Limmatvapirat3Jitnapa Sirirak4Poomipat Tamdee5Sukannika Tubtimsri6Faculty of Pharmaceutical Sciences, Burapha University, Chonburi 20131, ThailandFaculty of Pharmaceutical Sciences, Burapha University, Chonburi 20131, ThailandFaculty of Pharmaceutical Sciences, Burapha University, Chonburi 20131, ThailandDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, ThailandDepartment of Chemistry, Faculty of Science, Silpakorn University, Nakhon Pathom 73000, ThailandDepartment of Chemistry, Faculty of Science, Silpakorn University, Nakhon Pathom 73000, ThailandFaculty of Pharmaceutical Sciences, Burapha University, Chonburi 20131, ThailandQuercetin (QCT), a natural flavonoid, is of research interest owing to its pharmacological properties. However, its pharmacokinetic limitations could hinder its widespread therapeutic use. Nanocarriers, especially solid lipid nanoparticles (SLNs), might overcome this constraint. This study aimed to investigate QCT-loaded SLNs prepared via a new approach using a volatile oil. The phase-inversion temperature method was used to incorporate rosemary oil (RMO) into SLNs prepared using solid lipids possessing different chemical structures. Among the solid lipids used in the formulations, trilaurin (TLR) exhibited the smallest particle size and good stability after a temperature cycling test. SLNs prepared with a ratio of RMO to TLR of 1:3 could load QCT with an entrapment efficiency of >60% and drug loading of ~2% <i>w</i>/<i>w</i>. The smallest particle size was achieved using the polyoxyethylene-hydrogenated castor oil RH40, and the particle size depended on the concentration. The drug-release profile of QCT_TLR exhibited prolonged biphasic release for >24 h. QCT_TLR was a safe formulation, as indicated by a cell viability percentage of >75% at <2% <i>v</i>/<i>v</i>. In a computer simulation, the system with RMO enabled smaller sized SLNs than those without RMO. This new discovery shows great promise for producing SLNs via the phase-inversion temperature method with incorporation of volatile oil, particularly for delivering compounds with limited water solubility.https://www.mdpi.com/1999-4923/14/10/1984solid lipid nanoparticlesquercetinphase-inversion temperaturemolecular dynamics studyvolatile oil
spellingShingle Yotsanan Weerapol
Suwisit Manmuan
Nattaya Chaothanaphat
Sontaya Limmatvapirat
Jitnapa Sirirak
Poomipat Tamdee
Sukannika Tubtimsri
New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion Temperature Method
Pharmaceutics
solid lipid nanoparticles
quercetin
phase-inversion temperature
molecular dynamics study
volatile oil
title New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion Temperature Method
title_full New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion Temperature Method
title_fullStr New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion Temperature Method
title_full_unstemmed New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion Temperature Method
title_short New Approach for Preparing Solid Lipid Nanoparticles with Volatile Oil-Loaded Quercetin Using the Phase-Inversion Temperature Method
title_sort new approach for preparing solid lipid nanoparticles with volatile oil loaded quercetin using the phase inversion temperature method
topic solid lipid nanoparticles
quercetin
phase-inversion temperature
molecular dynamics study
volatile oil
url https://www.mdpi.com/1999-4923/14/10/1984
work_keys_str_mv AT yotsananweerapol newapproachforpreparingsolidlipidnanoparticleswithvolatileoilloadedquercetinusingthephaseinversiontemperaturemethod
AT suwisitmanmuan newapproachforpreparingsolidlipidnanoparticleswithvolatileoilloadedquercetinusingthephaseinversiontemperaturemethod
AT nattayachaothanaphat newapproachforpreparingsolidlipidnanoparticleswithvolatileoilloadedquercetinusingthephaseinversiontemperaturemethod
AT sontayalimmatvapirat newapproachforpreparingsolidlipidnanoparticleswithvolatileoilloadedquercetinusingthephaseinversiontemperaturemethod
AT jitnapasirirak newapproachforpreparingsolidlipidnanoparticleswithvolatileoilloadedquercetinusingthephaseinversiontemperaturemethod
AT poomipattamdee newapproachforpreparingsolidlipidnanoparticleswithvolatileoilloadedquercetinusingthephaseinversiontemperaturemethod
AT sukannikatubtimsri newapproachforpreparingsolidlipidnanoparticleswithvolatileoilloadedquercetinusingthephaseinversiontemperaturemethod