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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...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
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.
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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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