Topical Delivery of 5-Fluorouracil from Pheroid™ Formulations and the In Vitro Efficacy Against Human Melanoma

Chinembiri, Tawona N.; Gerber, Minja; Plessis, Lissinda H. Du; Preez, Jan L. du; Plessis, Jeanetta du

doi:10.1208/s12249-015-0328-7

Cited by 27 publications

(23 citation statements)

References 27 publications

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“…For an effective transdermal anticancer activity, chemotherapeutic agents need to exert their action with minimal side effects. This can be achieved if a drug was able to diffuse and accumulate mainly in the epidermis and dermis [54,55]. Therefore, amounts of drugs present in different skin layers were evaluated.…”

Section: Ex Vivo Skin Permeability Studiesmentioning

confidence: 99%

“…Results also showed that there was significant increase in the penetration of 5-FU through the skin when using MSN-NH 2 in comparison to gel alone ( Figure 9A). It is usually less likely for a hydrophilic drug such as 5-FU to remain in the dermis due to the lipophilic nature of skin [54]. However, MSN-NH 2 seems capable of significantly increasing the accumulation of 5-FU in skin layers to a concentration which was around 10 times higher than control, 149.53 ± 17.4 µg/cm 2 and 12.71 ± 3.3 µg/cm 2 for 5-FU MSN-NH 2 and control, respectively.…”

Section: Ex Vivo Skin Permeability Studiesmentioning

confidence: 99%

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The Design of Anionic Surfactant-Based Amino-Functionalized Mesoporous Silica Nanoparticles and their Application in Transdermal Drug Delivery

et al. 2020

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Melanoma remains the most lethal form of skin cancer and most challenging to treat despite advances in the oncology field. Our work describes the utilization of nanotechnology to target melanoma locally in an attempt to provide an advanced and efficient quality of therapy. Amino-functionalized mesoporous silica nanoparticles (MSN-NH2) were developed in situ through the utilization of anionic surfactant and different volumes of 3-aminopropyltriethoxysilane (APTES) as a co-structure directing agent (CSDA). Prepared particles were characterized for their morphology, particles size, 5-flurouracol (5-FU) and dexamethasone (DEX) loading capacity and release, skin penetration, and cytotoxicity in vitro in HT-144 melanoma cells. Results of transmission electron microscopy (TEM) and nitrogen adsorption–desorption isotherm showed that using different volumes of APTES during the functionalization process had an impact on the internal and external morphology of the particles, as well as particle size. However, changing the volume of APTES did not affect the diameter of formed mesochannels, which was about 4 nm. MSN-NH2 showed a relatively high loading capacity of 5-FU (12.6 ± 5.5) and DEX (44.72 ± 4.21) when using drug: MSN-NH2 ratios of 5:1 for both drugs. The release profile showed that around 83% of 5-FU and 21% of DEX were released over 48 h in pH 7.4. The skin permeability study revealed that enhancement ratio of 5-Fu and DEX using MSN-NH2 were 4.67 and 5.68, respectively, relative to their free drugs counterparts. In addition, the accumulation of drugs in skin layers where melanoma cells usually reside were enhanced approximately 10 times with 5-FU and 5 times with DEX when delivering drugs using MSN-NH2 compared to control. MSN-NH2 alone was nontoxic to melanoma cells when incubated for 48 h in the range of 0 to 468 µg/mL. The combination of 5-FU MSN-NH2 and DEX MSN-NH2 showed significant increase in toxicity compared to their free dug counterparts and exhibited a synergetic effect as well as the ability to circumvent DEX induced 5-FU resistance in melanoma cells.

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Section: Ex Vivo Skin Permeability Studiesmentioning

confidence: 99%

Section: Ex Vivo Skin Permeability Studiesmentioning

confidence: 99%

The Design of Anionic Surfactant-Based Amino-Functionalized Mesoporous Silica Nanoparticles and their Application in Transdermal Drug Delivery

et al. 2020

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“…The influence of drug delivery system on the skin permeation and antimelanoma efficacy of 5‐FU was investigated by Chinembiri et al…”

Section: Resultsmentioning

confidence: 99%

“…The influence of drug delivery system on the skin permeation and antimelanoma efficacy of 5-FU was investigated by Chinembiri et al 38 Published studies have proven the role of novel encapsulated systems like Pheroid™ technology and nanosystems in enhancing skin retention, extended and targeted drug release protection of the drugs, and lower skin irritation. 39 New excipients, refined processing techniques, and a better knowledge of the physicochemical properties of vehicles and drugs have led to the development of new delivery systems.…”

Section: Con Clus Ionmentioning

confidence: 99%

Advances in encapsulated dermal formulations in chemoprevention of melanoma: An overview

Ravikumar

Tatke

2019

J of Cosmetic Dermatology

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Background The three forms of skin cancer are cutaneous malignant melanoma, basal cell carcinoma, and squamous cell carcinoma. Melanoma skin cancer is an aggressive type and one of the most chemotherapy‐resistant malignancies. Conventional topical products are beset with limitations, leading to lower efficacy. There is a growing need to develop topical formulations encapsulated in polymeric and lipid nanoparticles, nanoemulsions, dendrimers, and liposomes exhibiting enhanced skin penetration and longer skin retention leading to better efficacy. Objective The objective of this article is the screening of reported novel drug encapsulated delivery systems effective topically in melanoma chemoprevention. Aim The scope of this work is to provide an overview pertaining to the development and evaluation of three exemplary drug delivery systems (DDS), namely vesicular, particulate, and specialized emulsions. Methods Topical drug delivery approaches targeting skin cancer have been reviewed and discussed. The focal point of the article is presentation of insights from published studies. Results This review focuses on the novel delivery systems in chemoprevention of melanoma with discussion highlighting on advances in topical delivery. Conclusion Literature indicates that drug‐loaded encapsulated topical formulations when compared with conventional dosage forms for skin cancer treatment exhibit greater efficacy and provide benefits like extended drug release, protection of the active ingredient against degradation, and lower skin irritation. Incorporation of phytoconstituents in newer delivery systems will be the way forward for improved topical chemoprevention strategy in melanoma. This has raised hope in making dermal therapy more useful and acceptable.

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“…5-FU changes into active metabolite such as fluorodeoxyuridine monophosphate (FdUMP), fluorodeoxyuridine triphosphate (FdUTP) and fluorouridine triphosphate (FUTP) [6]. Furthermore, it causes activation of p53 and dysfunction of mitochondria in releasing cytochrome c and then induces the apoptosis pathway [7]. However, this research was designed to evaluate the effectivity of 5-FU cream from National Cancer Center-Dharmais Cancer Hospital product for squamous cell precancerous lesion through Ki67 expression compared with 5% imiquimod cream commercial product.…”

Section: Introductionmentioning

confidence: 99%

Expression of Ki67 in Precancerous Squamous Cell Skin Lesion of Mice Induced by DMBA

Nurkasanah¹,

Hoemardani

Sinuraya

2019

Indonesian Journal of Cancer

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Background: Squamous cell carcinoma (SCC) is an invasive skin cancer that is found in the human skin. SCC growth from the precancerous lesion is known as a wart or papilloma. Ki67 is a protein expressed by cells during proliferation. Cells with higher Ki67 expression showed abnormal regulation of apoptosis. 5-FU is an antimetabolite compound that works as a DNA/RNA pyrimidine antagonist molecule that can induce cell apoptosis. The main objective of this research is to evaluate the inhibition proliferation of precancerous squamous cell in skin lesion induced by DMBA/croton oil treated by using 5-FU cream topically compared to 5% imiquimod cream. Methods: This research assesses three different concentrations of 5-FU cream namely 1%, 2%, and 5% topically on 24 wild type mice divided into 6 groups of 4 each including positive control (with carcinogenesis but without treatment), negative control (without treatment ; normal), carcinogenesis with treatment 5-FU cream (1%, 2%, and 5%) or 5% imiquimod cream. The expression of Ki67 was analyzed using immunohistochemistry. Statistical analysis was performed by one-way ANOVA using SPSS version 23. Results: Based on this research, 5-FU cream treatment during 4 weeks (week 10-week 14) showed the decrease of cumulative number of papilloma (p<0.05) and immunohistochemistry analysis resulted in the lowest Ki67 expression in 5-FU 2% and 5% groups compared to 5% imiquimod cream (p<0.05). Conclusions: 5-FU cream treatment during 4 weeks showed a decrease of papilloma and Ki67 expression in 5-FU cream 2% and

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Topical Delivery of 5-Fluorouracil from Pheroid™ Formulations and the In Vitro Efficacy Against Human Melanoma

Cited by 27 publications

References 27 publications

The Design of Anionic Surfactant-Based Amino-Functionalized Mesoporous Silica Nanoparticles and their Application in Transdermal Drug Delivery

The Design of Anionic Surfactant-Based Amino-Functionalized Mesoporous Silica Nanoparticles and their Application in Transdermal Drug Delivery

Advances in encapsulated dermal formulations in chemoprevention of melanoma: An overview

Expression of Ki67 in Precancerous Squamous Cell Skin Lesion of Mice Induced by DMBA

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