Novel Transethosomal Gel Loaded With 5 Fluorouracil: A Promising Approach for Enhanced Skin Cancer Treatment

Introduction:-5-Fluorouracil (5-FU) is an antimetabolite chemotherapeutic agent used primarily to treat various cancers, such as actinic keratosis, breast and skin cancer. It has a biological half-life of 10 – 20 mins. The conventional cream/Ointment dosage may have present challenges such as poor skin penetration, necessitating frequent application for effective treatment. Additionally, they can cause significant skin irritation and discomfort, with some risk of systemic absorption leading to unwanted side effects. To address these issues, a transethosomes gel formulation of 5-FU was developed. This gel enhances skin penetration, provides sustained drug release, improves bioavailability etc, making it a more effective and patient-friendly alternative to conventional creams. Therefore, transethosomes containing 5 - Fluorouracil embedded in appropriate gel delivery systems can effectively deliver this drug for a long time ( slow and sustain drug release) in the treatment of actinic keratosis. Methodology:- 5 - Fluorouracil loaded Transethosomes were formulated by using Cold Method. Total 12 formulations were prepared using Soya phosphotidylcholine, ethanol and with varying concentration of Surfactants/Edge activators such as Span 60, Tween 80, Sodium deoxycholate and Kolliphor RH 40. The formulations were further characterized for various parameters such as, particles size, polydispersity index, zeta potential, entrapment efficiency and in-vitro drug release. The promising transethosomal formulation (TET3) was incorporated into a suitable gel base and evaluated for physical appearance, pH, rheological study, spreadability test, content uniformity, in- vitro drug release and kinetic studies. Results and Discussions:- Among all formulations, the formulation (TET3) prepared with Tween 80 showed Smaller vesicular diameter (167.9 nm) with Excellent PDI ( 0.110 ) and good zeta potential (-21.6 mV), good drug content (98.12 %), better entrapment efficiency (65.15%), optimum drug release for 8 hrs (62.53%). So, Formulation TET3 Was Considered As A Promising Formulation. The Results Revealed That 5 - Fluorouracil Transethosomal Gel Was Successfully Developed As A Transdermal Drug Delivery System. The Gel Formulation TET3 – 1% Showed Optimum Drug Release That Is 58.78% For 8 Hrs. Conclusion:- In Conclusion, The Development Of 5- Fluorouracil - Loaded Transethosomes Using The Cold Method Proved Effective In Enhancing Transdermal Delivery For The Treatment Of Skin Cancer. The Optimized Formulation Exhibited Desirable Characteristics, Superior Skin Permeation And Improved Prolonged Efficacy Compared To The Commercially Formulation, Showcasing Its Potential As A Promising Approach In Treatment.

Publication Details

Journal
Zenodo (CERN European Organization for Nuclear Research)
Published
2024-12-10
DOI
https://doi.org/10.5281/zenodo.14352036
Primary Topic
Advancements in Transdermal Drug Delivery
Type
article
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article

Novel Transethosomal Gel Loaded With 5 Fluorouracil: A Promising Approach for Enhanced Skin Cancer Treatment

Zenodo (CERN European Organization for Nuclear Research)
Advancements in Transdermal Drug Delivery
article

Novel Transethosomal Gel Loaded With 5 Fluorouracil: A Promising Approach for Enhanced Skin Cancer Treatment

article en

Abstract

Introduction:-5-Fluorouracil (5-FU) is an antimetabolite chemotherapeutic agent used primarily to treat various cancers, such as actinic keratosis, breast and skin cancer. It has a biological half-life of 10 – 20 mins. The conventional cream/Ointment dosage may have present challenges such as poor skin penetration, necessitating frequent application for effective treatment. Additionally, they can cause significant skin irritation and discomfort, with some risk of systemic absorption leading to unwanted side effects. To address these issues, a transethosomes gel formulation of 5-FU was developed. This gel enhances skin penetration, provides sustained drug release, improves bioavailability etc, making it a more effective and patient-friendly alternative to conventional creams. Therefore, transethosomes containing 5 - Fluorouracil embedded in appropriate gel delivery systems can effectively deliver this drug for a long time ( slow and sustain drug release) in the treatment of actinic keratosis. Methodology:- 5 - Fluorouracil loaded Transethosomes were formulated by using Cold Method. Total 12 formulations were prepared using Soya phosphotidylcholine, ethanol and with varying concentration of Surfactants/Edge activators such as Span 60, Tween 80, Sodium deoxycholate and Kolliphor RH 40. The formulations were further characterized for various parameters such as, particles size, polydispersity index, zeta potential, entrapment efficiency and in-vitro drug release. The promising transethosomal formulation (TET3) was incorporated into a suitable gel base and evaluated for physical appearance, pH, rheological study, spreadability test, content uniformity, in- vitro drug release and kinetic studies. Results and Discussions:- Among all formulations, the formulation (TET3) prepared with Tween 80 showed Smaller vesicular diameter (167.9 nm) with Excellent PDI ( 0.110 ) and good zeta potential (-21.6 mV), good drug content (98.12 %), better entrapment efficiency (65.15%), optimum drug release for 8 hrs (62.53%). So, Formulation TET3 Was Considered As A Promising Formulation. The Results Revealed That 5 - Fluorouracil Transethosomal Gel Was Successfully Developed As A Transdermal Drug Delivery System. The Gel Formulation TET3 – 1% Showed Optimum Drug Release That Is 58.78% For 8 Hrs. Conclusion:- In Conclusion, The Development Of 5- Fluorouracil - Loaded Transethosomes Using The Cold Method Proved Effective In Enhancing Transdermal Delivery For The Treatment Of Skin Cancer. The Optimized Formulation Exhibited Desirable Characteristics, Superior Skin Permeation And Improved Prolonged Efficacy Compared To The Commercially Formulation, Showcasing Its Potential As A Promising Approach In Treatment.

Zenodo (CERN European Organization for Nuclear Research)
Openalex Percentile: Top 64%
Advancements in Transdermal Drug Delivery
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