An emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders: kojic acid-solid lipid nanoparticles

Kojic acid (KA) as tyrosinase inhibitor shows insufficient skin penetration and several adverse events due topical administration. KA solid lipid nanoparticles (KA-SLNs) were prepared using high speed homogenisation followed by ultra-probe sonication method for improve its effectiveness.KA-SLNs was...

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Main Authors: Khadijeh Khezri, Majid Saeedi, Katayoun Morteza-Semnani, Jafar Akbari, Seyyed Sohrab Rostamkalaei
Format: Article
Language:English
Published: Taylor & Francis Group 2020-01-01
Series:Artificial Cells, Nanomedicine, and Biotechnology
Subjects:
Online Access:https://www.tandfonline.com/doi/10.1080/21691401.2020.1770271
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author Khadijeh Khezri
Majid Saeedi
Katayoun Morteza-Semnani
Jafar Akbari
Seyyed Sohrab Rostamkalaei
author_facet Khadijeh Khezri
Majid Saeedi
Katayoun Morteza-Semnani
Jafar Akbari
Seyyed Sohrab Rostamkalaei
author_sort Khadijeh Khezri
collection DOAJ
description Kojic acid (KA) as tyrosinase inhibitor shows insufficient skin penetration and several adverse events due topical administration. KA solid lipid nanoparticles (KA-SLNs) were prepared using high speed homogenisation followed by ultra-probe sonication method for improve its effectiveness.KA-SLNs was optimised by Glyceryl mono-stearate (GMS) and Cholesterol (Chol) as lipid excipients and span 60 (SP 60) and Tween 20 (Tw 20) as co-emulsifiers (particle size 156.97 ± 7.15 nm, encapsulation efficiency 59.02 ± 0.74%, drug loading 14.755 ± 1.63%, polydispersity index (PDI) of 0.388 ± 0.004 and zeta potential (ZP) of -27.67 ± 1.89 mV). Optimum formulation (KA-SLN3 dispersion) was stable at 4 and 25 °C for 3 months. Also, TEM image confirmed these results. The results of XRD, DSC and ATR-FTIR analysis indicated that KA was well encapsulated within the SLNs either in molecularly dispersed state and stabilised in amorphous form and there was no chemical interaction between drug and other ingredients. Controlled release was achieved with this formulation. KA-SLN3 dispersion have more tyrosinase inhibition potency in comparison with pure KA. Also, the results of the ex vivo and in vitro percutaneous absorption show that KA-SLN3 dispersion improved percutaneous delivery of KA as a promising and potential novel topical preparation and might open new avenues for treatment of hyperpigmentation disorders.
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spelling doaj.art-2d1a06b6955b45d898c517f0460889262024-07-23T18:44:31ZengTaylor & Francis GroupArtificial Cells, Nanomedicine, and Biotechnology2169-14012169-141X2020-01-0148184185310.1080/21691401.2020.1770271An emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders: kojic acid-solid lipid nanoparticlesKhadijeh Khezri0Majid Saeedi1Katayoun Morteza-Semnani2Jafar Akbari3Seyyed Sohrab Rostamkalaei4Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, IranDepartment of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, IranDepartment of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, IranDepartment of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, IranDepartment of Pharmaceutics, Faculty of Pharmacy, Islamic Azad University, Ayatollah Amoli Branch, Amol, IranKojic acid (KA) as tyrosinase inhibitor shows insufficient skin penetration and several adverse events due topical administration. KA solid lipid nanoparticles (KA-SLNs) were prepared using high speed homogenisation followed by ultra-probe sonication method for improve its effectiveness.KA-SLNs was optimised by Glyceryl mono-stearate (GMS) and Cholesterol (Chol) as lipid excipients and span 60 (SP 60) and Tween 20 (Tw 20) as co-emulsifiers (particle size 156.97 ± 7.15 nm, encapsulation efficiency 59.02 ± 0.74%, drug loading 14.755 ± 1.63%, polydispersity index (PDI) of 0.388 ± 0.004 and zeta potential (ZP) of -27.67 ± 1.89 mV). Optimum formulation (KA-SLN3 dispersion) was stable at 4 and 25 °C for 3 months. Also, TEM image confirmed these results. The results of XRD, DSC and ATR-FTIR analysis indicated that KA was well encapsulated within the SLNs either in molecularly dispersed state and stabilised in amorphous form and there was no chemical interaction between drug and other ingredients. Controlled release was achieved with this formulation. KA-SLN3 dispersion have more tyrosinase inhibition potency in comparison with pure KA. Also, the results of the ex vivo and in vitro percutaneous absorption show that KA-SLN3 dispersion improved percutaneous delivery of KA as a promising and potential novel topical preparation and might open new avenues for treatment of hyperpigmentation disorders.https://www.tandfonline.com/doi/10.1080/21691401.2020.1770271Kojic acidHyperpigmentation disordersTyrosinaseSolid lipid Nanoparticles
spellingShingle Khadijeh Khezri
Majid Saeedi
Katayoun Morteza-Semnani
Jafar Akbari
Seyyed Sohrab Rostamkalaei
An emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders: kojic acid-solid lipid nanoparticles
Artificial Cells, Nanomedicine, and Biotechnology
Kojic acid
Hyperpigmentation disorders
Tyrosinase
Solid lipid Nanoparticles
title An emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders: kojic acid-solid lipid nanoparticles
title_full An emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders: kojic acid-solid lipid nanoparticles
title_fullStr An emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders: kojic acid-solid lipid nanoparticles
title_full_unstemmed An emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders: kojic acid-solid lipid nanoparticles
title_short An emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders: kojic acid-solid lipid nanoparticles
title_sort emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders kojic acid solid lipid nanoparticles
topic Kojic acid
Hyperpigmentation disorders
Tyrosinase
Solid lipid Nanoparticles
url https://www.tandfonline.com/doi/10.1080/21691401.2020.1770271
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