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Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin Cancer

Strychnine (STCN) has demonstrated an exceptional anticancer effect against various cancers. However, the STCN clinical utility has been hampered by its low water solubility, restricted therapeutic window, short half-life, and significant toxicity. The objective of this investigation was to design a...

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Autores principales: Alam, Perwez, Imran, Mohd, Gupta, Dipak Kumar, Akhtar, Ali
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10606039/
https://www.ncbi.nlm.nih.gov/pubmed/37888405
http://dx.doi.org/10.3390/gels9100831
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author Alam, Perwez
Imran, Mohd
Gupta, Dipak Kumar
Akhtar, Ali
author_facet Alam, Perwez
Imran, Mohd
Gupta, Dipak Kumar
Akhtar, Ali
author_sort Alam, Perwez
collection PubMed
description Strychnine (STCN) has demonstrated an exceptional anticancer effect against various cancers. However, the STCN clinical utility has been hampered by its low water solubility, restricted therapeutic window, short half-life, and significant toxicity. The objective of this investigation was to design and optimize a formulation of strychnine-loaded transliposomes (STCN–TLs) for dermal administration of STCN to treat skin cancer. The formulations of STCN–TL were examined in terms of vesicle size (VS), polydispersity index (PDI), entrapment efficiency (EE), and in vitro delivery. The improved STCN–TL formulation exhibited VS, PDI, EE, and in vitro delivery of 101.5 ± 2.14 nm, 0.218 ± 0.12, 81.74 ± 1.43%, and 85.39 ± 2.33%, respectively. In an ex vivo penetration, the created STCN–TL formulation demonstrated a 2.5-fold increase in permeability compared to the STCN solution. CLSM pictures of skin (rat) revealed that the rhodamine B-loaded transliposome preparation penetrated deeper than the rhodamine B hydroalcoholic mixture. Additionally, rat skin managed with STCN–TL nanogel exhibited a significant increase in C(skin max) and AUC(0-8) compared to rat skin treated with traditional STCN gel. The findings demonstrated that the transliposome preparation might be a suitable nanocarrier for the cutaneous distribution of STCN in the amelioration of skin cancer.
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spelling pubmed-106060392023-10-28 Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin Cancer Alam, Perwez Imran, Mohd Gupta, Dipak Kumar Akhtar, Ali Gels Article Strychnine (STCN) has demonstrated an exceptional anticancer effect against various cancers. However, the STCN clinical utility has been hampered by its low water solubility, restricted therapeutic window, short half-life, and significant toxicity. The objective of this investigation was to design and optimize a formulation of strychnine-loaded transliposomes (STCN–TLs) for dermal administration of STCN to treat skin cancer. The formulations of STCN–TL were examined in terms of vesicle size (VS), polydispersity index (PDI), entrapment efficiency (EE), and in vitro delivery. The improved STCN–TL formulation exhibited VS, PDI, EE, and in vitro delivery of 101.5 ± 2.14 nm, 0.218 ± 0.12, 81.74 ± 1.43%, and 85.39 ± 2.33%, respectively. In an ex vivo penetration, the created STCN–TL formulation demonstrated a 2.5-fold increase in permeability compared to the STCN solution. CLSM pictures of skin (rat) revealed that the rhodamine B-loaded transliposome preparation penetrated deeper than the rhodamine B hydroalcoholic mixture. Additionally, rat skin managed with STCN–TL nanogel exhibited a significant increase in C(skin max) and AUC(0-8) compared to rat skin treated with traditional STCN gel. The findings demonstrated that the transliposome preparation might be a suitable nanocarrier for the cutaneous distribution of STCN in the amelioration of skin cancer. MDPI 2023-10-20 /pmc/articles/PMC10606039/ /pubmed/37888405 http://dx.doi.org/10.3390/gels9100831 Text en © 2023 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
Alam, Perwez
Imran, Mohd
Gupta, Dipak Kumar
Akhtar, Ali
Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin Cancer
title Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin Cancer
title_full Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin Cancer
title_fullStr Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin Cancer
title_full_unstemmed Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin Cancer
title_short Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin Cancer
title_sort formulation of transliposomal nanocarrier gel containing strychnine for the effective management of skin cancer
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10606039/
https://www.ncbi.nlm.nih.gov/pubmed/37888405
http://dx.doi.org/10.3390/gels9100831
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