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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Main Authors: Perwez Alam, Mohd Imran, Dipak Kumar Gupta, Ali Akhtar
Format: Article
Language:English
Published: MDPI AG 2023-10-01
Series:Gels
Subjects:
Online Access:https://www.mdpi.com/2310-2861/9/10/831
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author Perwez Alam
Mohd Imran
Dipak Kumar Gupta
Ali Akhtar
author_facet Perwez Alam
Mohd Imran
Dipak Kumar Gupta
Ali Akhtar
author_sort Perwez Alam
collection DOAJ
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<sub>skin max</sub> and AUC<sub>0-8</sub> 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 doaj.art-2c32da64a3394048a8f9eb276348bbdf2023-11-19T16:36:01ZengMDPI AGGels2310-28612023-10-0191083110.3390/gels9100831Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin CancerPerwez Alam0Mohd Imran1Dipak Kumar Gupta2Ali Akhtar3Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaSchool of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, IndiaSchool of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, IndiaDepartment of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaStrychnine (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<sub>skin max</sub> and AUC<sub>0-8</sub> 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.https://www.mdpi.com/2310-2861/9/10/831strychninetransliposomesskin cancerpermeabilitydermatokinetics
spellingShingle Perwez Alam
Mohd Imran
Dipak Kumar Gupta
Ali Akhtar
Formulation of Transliposomal Nanocarrier Gel Containing Strychnine for the Effective Management of Skin Cancer
Gels
strychnine
transliposomes
skin cancer
permeability
dermatokinetics
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 strychnine
transliposomes
skin cancer
permeability
dermatokinetics
url https://www.mdpi.com/2310-2861/9/10/831
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