Cargando…

Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration

BACKGROUND: The aim of this study was to assess the pharmacokinetics after transdermal administration by a novel skin microdialysis technology in rats. The guinea pig model was established by investigating the pharmacodynamics. MATERIAL/METHODS: Three different agents were given after hair removal,...

Descripción completa

Detalles Bibliográficos
Autores principales: Zhu, Na, Wu, Xiao-xiang, Tian, Yong, Zhu, Jin-xiu, Li, Jian-chun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: International Scientific Literature, Inc. 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5926275/
https://www.ncbi.nlm.nih.gov/pubmed/29666359
http://dx.doi.org/10.12659/MSM.906140
_version_ 1783318868223066112
author Zhu, Na
Wu, Xiao-xiang
Tian, Yong
Zhu, Jin-xiu
Li, Jian-chun
author_facet Zhu, Na
Wu, Xiao-xiang
Tian, Yong
Zhu, Jin-xiu
Li, Jian-chun
author_sort Zhu, Na
collection PubMed
description BACKGROUND: The aim of this study was to assess the pharmacokinetics after transdermal administration by a novel skin microdialysis technology in rats. The guinea pig model was established by investigating the pharmacodynamics. MATERIAL/METHODS: Three different agents were given after hair removal, and the samples were extracted by microdialysis and detected by HPLC. Subcutaneous/plasma concentration-time curves of the 3 different agents were analyzed and the pharmacokinetic parameters were calculated. The SS-04B UV light therapy instrument was used in the modeling. Changes in melanin index and histopathology were observed with HE staining. RESULTS: The increment and decrement results showed that the concentration had no significant effect on drug recovery both in vivo and in vitro. After the paeonol cubic liquid crystalline nanoparticles gel (PAE-LCNPs) was administered, the maximum peak time (t(max)) of paeonol skin concentration appeared at 2.42±0.20 h, the maximum skin concentration C(max) was (926±105) ng/ml, and the area under the curve AUC(0–8) was (8056±954) ng/h/ml. The t(max) was shortened much more than in the other groups, and the performance of PAE-LCNPs targeting was good. Pharmacodynamic results showed that PAE-LCNPs can reduce melanocytes and reduce the melanin index, proving its utility in the treatment of melanin deposition. CONCLUSIONS: The skin microdialysis study indicated PAE-LCNPs have good transdermal permeability and efficacy. Pharmacological experiments based on the study found that the topical pigmentation model of guinea pigs showed a better therapeutic effect.
format Online
Article
Text
id pubmed-5926275
institution National Center for Biotechnology Information
language English
publishDate 2018
publisher International Scientific Literature, Inc.
record_format MEDLINE/PubMed
spelling pubmed-59262752018-05-01 Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration Zhu, Na Wu, Xiao-xiang Tian, Yong Zhu, Jin-xiu Li, Jian-chun Med Sci Monit Lab/In Vitro Research BACKGROUND: The aim of this study was to assess the pharmacokinetics after transdermal administration by a novel skin microdialysis technology in rats. The guinea pig model was established by investigating the pharmacodynamics. MATERIAL/METHODS: Three different agents were given after hair removal, and the samples were extracted by microdialysis and detected by HPLC. Subcutaneous/plasma concentration-time curves of the 3 different agents were analyzed and the pharmacokinetic parameters were calculated. The SS-04B UV light therapy instrument was used in the modeling. Changes in melanin index and histopathology were observed with HE staining. RESULTS: The increment and decrement results showed that the concentration had no significant effect on drug recovery both in vivo and in vitro. After the paeonol cubic liquid crystalline nanoparticles gel (PAE-LCNPs) was administered, the maximum peak time (t(max)) of paeonol skin concentration appeared at 2.42±0.20 h, the maximum skin concentration C(max) was (926±105) ng/ml, and the area under the curve AUC(0–8) was (8056±954) ng/h/ml. The t(max) was shortened much more than in the other groups, and the performance of PAE-LCNPs targeting was good. Pharmacodynamic results showed that PAE-LCNPs can reduce melanocytes and reduce the melanin index, proving its utility in the treatment of melanin deposition. CONCLUSIONS: The skin microdialysis study indicated PAE-LCNPs have good transdermal permeability and efficacy. Pharmacological experiments based on the study found that the topical pigmentation model of guinea pigs showed a better therapeutic effect. International Scientific Literature, Inc. 2018-04-18 /pmc/articles/PMC5926275/ /pubmed/29666359 http://dx.doi.org/10.12659/MSM.906140 Text en © Med Sci Monit, 2018 This work is licensed under Creative Common Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0 (https://creativecommons.org/licenses/by-nc-nd/4.0/) )
spellingShingle Lab/In Vitro Research
Zhu, Na
Wu, Xiao-xiang
Tian, Yong
Zhu, Jin-xiu
Li, Jian-chun
Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration
title Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration
title_full Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration
title_fullStr Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration
title_full_unstemmed Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration
title_short Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration
title_sort pharmacokinetic and pharmacodynamics of self-assembled cubic liquid crystalline nanoparticle gel after transdermal administration
topic Lab/In Vitro Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5926275/
https://www.ncbi.nlm.nih.gov/pubmed/29666359
http://dx.doi.org/10.12659/MSM.906140
work_keys_str_mv AT zhuna pharmacokineticandpharmacodynamicsofselfassembledcubicliquidcrystallinenanoparticlegelaftertransdermaladministration
AT wuxiaoxiang pharmacokineticandpharmacodynamicsofselfassembledcubicliquidcrystallinenanoparticlegelaftertransdermaladministration
AT tianyong pharmacokineticandpharmacodynamicsofselfassembledcubicliquidcrystallinenanoparticlegelaftertransdermaladministration
AT zhujinxiu pharmacokineticandpharmacodynamicsofselfassembledcubicliquidcrystallinenanoparticlegelaftertransdermaladministration
AT lijianchun pharmacokineticandpharmacodynamicsofselfassembledcubicliquidcrystallinenanoparticlegelaftertransdermaladministration