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Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery
Transdermal drug delivery is important to maintain plasma drug concentrations for therapeutic efficacy. The current study reports the design, formulation, and evaluation of tizanidine transdermal patches formulated using chitosan and thiolated chitosan, ethyl cellulose (EC), polyvinylpyrrolidone (PV...
Autores principales: | , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8659784/ https://www.ncbi.nlm.nih.gov/pubmed/34883720 http://dx.doi.org/10.3390/polym13234217 |
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author | Akhlaq, Muhammad Azad, Abul Kalam Fuloria, Shivkanya Meenakshi, Dhanalekshmi Unnikrishnan Raza, Sajid Safdar, Muhammad Nawaz, Asif Subramaniyan, Vetriselvan Sekar, Mahendran Sathasivam, Kathiresan V. Wu, Yuan Seng Miret, Mireia Mallandrich Fuloria, Neeraj Kumar |
author_facet | Akhlaq, Muhammad Azad, Abul Kalam Fuloria, Shivkanya Meenakshi, Dhanalekshmi Unnikrishnan Raza, Sajid Safdar, Muhammad Nawaz, Asif Subramaniyan, Vetriselvan Sekar, Mahendran Sathasivam, Kathiresan V. Wu, Yuan Seng Miret, Mireia Mallandrich Fuloria, Neeraj Kumar |
author_sort | Akhlaq, Muhammad |
collection | PubMed |
description | Transdermal drug delivery is important to maintain plasma drug concentrations for therapeutic efficacy. The current study reports the design, formulation, and evaluation of tizanidine transdermal patches formulated using chitosan and thiolated chitosan, ethyl cellulose (EC), polyvinylpyrrolidone (PVP), and Eudragit RL100 in different ratios. The tizanidine patches were formulated using flaxseed oil and coriander oil in the concentrations of 1% v/w, 2% v/w, 3% v/w, 4% v/w, 5% v/w, and 10% v/w. The patches were subjected to characterization of physicochemical property (thickness, weight uniformity, drug content, efficiency, percentage moisture uptake/loss), in vitro drug release and drug permeation, skin irritation, in vivo application, pharmacokinetics analysis, and stability studies. The results indicate that the interaction of thiolated chitosan with the negative charges of the skin opens the tight junctions of the skin, whereas flaxseed and coriander oils change the conformational domain of the skin. The novelty of this study is in the use of flaxseed and coriander oils as skin permeation enhancers for the formulation of tizanidine transdermal patches. The formulations follow non-Fickian drug release kinetics. The FTZNE23, FTZNE36 and FTZNE54, with 5% v/w flaxseed oil loaded formulations, exhibited higher flux through rabbit skin compared with FTZNE30, FTZNE35, FTZNE42, and FTZNE47, formulations loaded with 10% v/w coriander oil. The study concludes that flaxseed oil is a better choice for formulating tizanidine patches, offering optimal plasma concentration and therapeutic efficacy, and recommends the use of flaxseed and coriander oil based patches as a novel transdermal delivery system for tizanidine and related classes of drugs. |
format | Online Article Text |
id | pubmed-8659784 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-86597842021-12-10 Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery Akhlaq, Muhammad Azad, Abul Kalam Fuloria, Shivkanya Meenakshi, Dhanalekshmi Unnikrishnan Raza, Sajid Safdar, Muhammad Nawaz, Asif Subramaniyan, Vetriselvan Sekar, Mahendran Sathasivam, Kathiresan V. Wu, Yuan Seng Miret, Mireia Mallandrich Fuloria, Neeraj Kumar Polymers (Basel) Article Transdermal drug delivery is important to maintain plasma drug concentrations for therapeutic efficacy. The current study reports the design, formulation, and evaluation of tizanidine transdermal patches formulated using chitosan and thiolated chitosan, ethyl cellulose (EC), polyvinylpyrrolidone (PVP), and Eudragit RL100 in different ratios. The tizanidine patches were formulated using flaxseed oil and coriander oil in the concentrations of 1% v/w, 2% v/w, 3% v/w, 4% v/w, 5% v/w, and 10% v/w. The patches were subjected to characterization of physicochemical property (thickness, weight uniformity, drug content, efficiency, percentage moisture uptake/loss), in vitro drug release and drug permeation, skin irritation, in vivo application, pharmacokinetics analysis, and stability studies. The results indicate that the interaction of thiolated chitosan with the negative charges of the skin opens the tight junctions of the skin, whereas flaxseed and coriander oils change the conformational domain of the skin. The novelty of this study is in the use of flaxseed and coriander oils as skin permeation enhancers for the formulation of tizanidine transdermal patches. The formulations follow non-Fickian drug release kinetics. The FTZNE23, FTZNE36 and FTZNE54, with 5% v/w flaxseed oil loaded formulations, exhibited higher flux through rabbit skin compared with FTZNE30, FTZNE35, FTZNE42, and FTZNE47, formulations loaded with 10% v/w coriander oil. The study concludes that flaxseed oil is a better choice for formulating tizanidine patches, offering optimal plasma concentration and therapeutic efficacy, and recommends the use of flaxseed and coriander oil based patches as a novel transdermal delivery system for tizanidine and related classes of drugs. MDPI 2021-12-01 /pmc/articles/PMC8659784/ /pubmed/34883720 http://dx.doi.org/10.3390/polym13234217 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Akhlaq, Muhammad Azad, Abul Kalam Fuloria, Shivkanya Meenakshi, Dhanalekshmi Unnikrishnan Raza, Sajid Safdar, Muhammad Nawaz, Asif Subramaniyan, Vetriselvan Sekar, Mahendran Sathasivam, Kathiresan V. Wu, Yuan Seng Miret, Mireia Mallandrich Fuloria, Neeraj Kumar Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery |
title | Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery |
title_full | Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery |
title_fullStr | Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery |
title_full_unstemmed | Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery |
title_short | Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery |
title_sort | fabrication of tizanidine loaded patches using flaxseed oil and coriander oil as a penetration enhancer for transdermal delivery |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8659784/ https://www.ncbi.nlm.nih.gov/pubmed/34883720 http://dx.doi.org/10.3390/polym13234217 |
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