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Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer

The plain 5-fluorouracil (5FU) formulations available in the market are associated with adverse effects such as skin irritation, pruritus, redness, blisters, allergy, and dryness on the site of application. The objective of the present study was to develop a liposomal emulgel of 5FU with increased s...

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Autores principales: Pachauri, Ankur, Chitme, Havagiray, Visht, Sharad, Chidrawar, Vijay, Mohammed, Nawaj, Abdel-Wahab, Basel A., Khateeb, Masood Medleri, Habeeb, Mohammed Shafiuddin, Orabi, Mohamed A. A., Bakir, Marwa B.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10048565/
https://www.ncbi.nlm.nih.gov/pubmed/36975657
http://dx.doi.org/10.3390/gels9030209
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author Pachauri, Ankur
Chitme, Havagiray
Visht, Sharad
Chidrawar, Vijay
Mohammed, Nawaj
Abdel-Wahab, Basel A.
Khateeb, Masood Medleri
Habeeb, Mohammed Shafiuddin
Orabi, Mohamed A. A.
Bakir, Marwa B.
author_facet Pachauri, Ankur
Chitme, Havagiray
Visht, Sharad
Chidrawar, Vijay
Mohammed, Nawaj
Abdel-Wahab, Basel A.
Khateeb, Masood Medleri
Habeeb, Mohammed Shafiuddin
Orabi, Mohamed A. A.
Bakir, Marwa B.
author_sort Pachauri, Ankur
collection PubMed
description The plain 5-fluorouracil (5FU) formulations available in the market are associated with adverse effects such as skin irritation, pruritus, redness, blisters, allergy, and dryness on the site of application. The objective of the present study was to develop a liposomal emulgel of 5FU with increased skin permeability and efficacy using clove oil and eucalyptus oil along with pharmaceutically acceptable carriers, excipients, stabilizers, binders, and additives. A series of seven formulations were developed and evaluated for their entrapment efficiency, in vitro release profile, and cumulative drug release profile. The compatibility of drugs and excipients, as confirmed by FTIR (fourier-transform infrared spectroscopy) and DSC (differential scanning calorimetry) as well as SEM (scanning electron microscopy) and TEM (transmission electron microscopy) studies, revealed that the size and shape of liposomes are smooth and spherical, and the liposomes are non-aggregated. To understand their efficacy, the optimized formulations were evaluated for cytotoxicity using B16-F10 mouse skin melanoma cells. The eucalyptus oil and clove oil-containing preparation significantly produced a cytotoxic effect against a melanoma cell line. The addition of clove oil and eucalyptus oil increased the efficacy of the formulation by improving skin permeability and reducing the dose required for the anti-skin cancer activity.
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spelling pubmed-100485652023-03-29 Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer Pachauri, Ankur Chitme, Havagiray Visht, Sharad Chidrawar, Vijay Mohammed, Nawaj Abdel-Wahab, Basel A. Khateeb, Masood Medleri Habeeb, Mohammed Shafiuddin Orabi, Mohamed A. A. Bakir, Marwa B. Gels Article The plain 5-fluorouracil (5FU) formulations available in the market are associated with adverse effects such as skin irritation, pruritus, redness, blisters, allergy, and dryness on the site of application. The objective of the present study was to develop a liposomal emulgel of 5FU with increased skin permeability and efficacy using clove oil and eucalyptus oil along with pharmaceutically acceptable carriers, excipients, stabilizers, binders, and additives. A series of seven formulations were developed and evaluated for their entrapment efficiency, in vitro release profile, and cumulative drug release profile. The compatibility of drugs and excipients, as confirmed by FTIR (fourier-transform infrared spectroscopy) and DSC (differential scanning calorimetry) as well as SEM (scanning electron microscopy) and TEM (transmission electron microscopy) studies, revealed that the size and shape of liposomes are smooth and spherical, and the liposomes are non-aggregated. To understand their efficacy, the optimized formulations were evaluated for cytotoxicity using B16-F10 mouse skin melanoma cells. The eucalyptus oil and clove oil-containing preparation significantly produced a cytotoxic effect against a melanoma cell line. The addition of clove oil and eucalyptus oil increased the efficacy of the formulation by improving skin permeability and reducing the dose required for the anti-skin cancer activity. MDPI 2023-03-09 /pmc/articles/PMC10048565/ /pubmed/36975657 http://dx.doi.org/10.3390/gels9030209 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
Pachauri, Ankur
Chitme, Havagiray
Visht, Sharad
Chidrawar, Vijay
Mohammed, Nawaj
Abdel-Wahab, Basel A.
Khateeb, Masood Medleri
Habeeb, Mohammed Shafiuddin
Orabi, Mohamed A. A.
Bakir, Marwa B.
Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer
title Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer
title_full Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer
title_fullStr Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer
title_full_unstemmed Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer
title_short Permeability-Enhanced Liposomal Emulgel Formulation of 5-Fluorouracil for the Treatment of Skin Cancer
title_sort permeability-enhanced liposomal emulgel formulation of 5-fluorouracil for the treatment of skin cancer
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10048565/
https://www.ncbi.nlm.nih.gov/pubmed/36975657
http://dx.doi.org/10.3390/gels9030209
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