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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...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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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. |
format | Online Article Text |
id | pubmed-10606039 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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