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The role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic

Transdermal drug delivery systems have made significant contributions to the medical community, but have yet to completely substitute oral or parenteral delivery. Recently, various strategies have been used to augment the transdermal delivery of therapeutics. Primarily, they include iontophoresis, e...

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Autores principales: Singh, Sima, Vardhan, Harsh, Kotla, Niranjan G, Maddiboyina, Balaji, Sharma, Dinesh, Webster, Thomas J
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4833371/
https://www.ncbi.nlm.nih.gov/pubmed/27114707
http://dx.doi.org/10.2147/IJN.S100253
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author Singh, Sima
Vardhan, Harsh
Kotla, Niranjan G
Maddiboyina, Balaji
Sharma, Dinesh
Webster, Thomas J
author_facet Singh, Sima
Vardhan, Harsh
Kotla, Niranjan G
Maddiboyina, Balaji
Sharma, Dinesh
Webster, Thomas J
author_sort Singh, Sima
collection PubMed
description Transdermal drug delivery systems have made significant contributions to the medical community, but have yet to completely substitute oral or parenteral delivery. Recently, various strategies have been used to augment the transdermal delivery of therapeutics. Primarily, they include iontophoresis, electrophoresis, sonophoresis, chemical permeation enhancers, microneedles, and vesicular systems. Among these strategies, elastic liposomes appear promising. Elastic vesicle scaffolds have been developed and evaluated as novel topical and transdermal delivery systems, with an infrastructure consisting of hydrophobic and hydrophilic moieties together, and as a result, such scaffolds can accommodate drug molecules with a wide range of solubility. High deformability of these vesicles provides for better penetration of intact vesicles. This system is much more efficient at delivering low- and high-molecular-weight drugs to the skin in terms of quantity and depth. In this work, elastic liposomes of Tramadol HCl were prepared using a solvent evaporation method with different surfactants and were characterized using microscopy, and particle size, shape, drug content, ex vivo release, and zeta potential were also calculated. The prepared elastic liposomes were found to be in the range of 152.4 nm with a zeta potential of −22.4 mV; the entrapment efficiencies of the selected formulation was found to be 79.71%±0.27%. All formulations in the form of a gel were evaluated for physicochemical properties and were found to be homogeneous with no grittiness, and the pH of all formulations was found to be neutral. The optimized selected elastic liposomal formulation followed the Higuchi equation and Fickian diffusion and released the drug for a period of 24 hours. The overall results provide much promise for the continued investigation of deformable vesicles as transdermal drug carriers.
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spelling pubmed-48333712016-04-25 The role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic Singh, Sima Vardhan, Harsh Kotla, Niranjan G Maddiboyina, Balaji Sharma, Dinesh Webster, Thomas J Int J Nanomedicine Original Research Transdermal drug delivery systems have made significant contributions to the medical community, but have yet to completely substitute oral or parenteral delivery. Recently, various strategies have been used to augment the transdermal delivery of therapeutics. Primarily, they include iontophoresis, electrophoresis, sonophoresis, chemical permeation enhancers, microneedles, and vesicular systems. Among these strategies, elastic liposomes appear promising. Elastic vesicle scaffolds have been developed and evaluated as novel topical and transdermal delivery systems, with an infrastructure consisting of hydrophobic and hydrophilic moieties together, and as a result, such scaffolds can accommodate drug molecules with a wide range of solubility. High deformability of these vesicles provides for better penetration of intact vesicles. This system is much more efficient at delivering low- and high-molecular-weight drugs to the skin in terms of quantity and depth. In this work, elastic liposomes of Tramadol HCl were prepared using a solvent evaporation method with different surfactants and were characterized using microscopy, and particle size, shape, drug content, ex vivo release, and zeta potential were also calculated. The prepared elastic liposomes were found to be in the range of 152.4 nm with a zeta potential of −22.4 mV; the entrapment efficiencies of the selected formulation was found to be 79.71%±0.27%. All formulations in the form of a gel were evaluated for physicochemical properties and were found to be homogeneous with no grittiness, and the pH of all formulations was found to be neutral. The optimized selected elastic liposomal formulation followed the Higuchi equation and Fickian diffusion and released the drug for a period of 24 hours. The overall results provide much promise for the continued investigation of deformable vesicles as transdermal drug carriers. Dove Medical Press 2016-04-08 /pmc/articles/PMC4833371/ /pubmed/27114707 http://dx.doi.org/10.2147/IJN.S100253 Text en © 2016 Singh et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Original Research
Singh, Sima
Vardhan, Harsh
Kotla, Niranjan G
Maddiboyina, Balaji
Sharma, Dinesh
Webster, Thomas J
The role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic
title The role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic
title_full The role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic
title_fullStr The role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic
title_full_unstemmed The role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic
title_short The role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic
title_sort role of surfactants in the formulation of elastic liposomal gels containing a synthetic opioid analgesic
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4833371/
https://www.ncbi.nlm.nih.gov/pubmed/27114707
http://dx.doi.org/10.2147/IJN.S100253
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