Sorbitan Monolaurate–Containing Liposomes Enhance Skin Cancer Cell Cytotoxicity and in Association with Microneedling Increase the Skin Penetration of 5-Fluorouracil

Crisóstomo, Luiziana Cavalcante Costa Fernandes; Carvalho, Genuína Stephanie Guimarães; Leal, Luzia Kalyne Almeida Moreira; Araújo, Tamara Gonçalves de; Nogueira, Karina Alexandre Barros; Silva, Durcilene Alves da; Ribeiro, Fábio de Oliveira Silva; Petrilli, Raquel; Eloy, Josimar O.

doi:10.1208/s12249-022-02356-z

Cited by 6 publications

(5 citation statements)

References 53 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The chemotherapeutic treatment with 5FU is difficult because of the very hydrophilic nature of the compound, which results in limited penetration and compromised efficacy. A recent study [ 47 ] recommends the use of 5FU liposomes with penetration enhancers such as sorbtitan monolaurate and span 20 in order to improve the drug’s efficacy and its ability to reach its target. Based on the findings of the present investigation, we assume it would be worthwhile to prepare a liposomal emulgel of 5FU with eucalyptus and/or clove oil and test its efficacy against squamous cell carcinoma cell lines.…”

Section: Resultsmentioning

confidence: 99%

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

Pachauri

Chitme

Visht

et al. 2023

Gels

View full text Add to dashboard Cite

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.

show abstract

Section: Resultsmentioning

confidence: 99%

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

Pachauri

Chitme

Visht

et al. 2023

Gels

View full text Add to dashboard Cite

show abstract

“…Specifically, the stratum corneum (SC), the outermost layer of the skin, which acts as a barrier to the external environment. In this context, the resistivity measurement is an important parameter to infer the penetration of substances into the skin, since low values mean some structural alteration, facilitating this process [ 25 , 48 ]. Herein, the resistivity values obtained without the application of sonophoresis are close to 85.94 kΩ cm 2 , which indicates preservation of the skin structure.…”

Section: Resultsmentioning

confidence: 99%

“…For the calculation of encapsulation efficiency, the indirect method described by Crisóstomo et al was used with adaptations [ 25 ]. Herein, the amount of free drug is calculated and correlated with its theoretical amount.…”

Section: Methodsmentioning

confidence: 99%

Nanoencapsulation of Methylene-Blue for Enhanced Skin Cancer Cell Phototoxicity and Cutaneous Penetration in Association with Sonophoresis

et al. 2023

Self Cite

View full text Add to dashboard Cite

Photodynamic therapy (PDT) using methylene blue (MB) as a photosensitizer has emerged as an alternative treatment for skin cancers, such as squamous cell carcinoma (SCC). To increase the cutaneous penetration of the drug, some strategies are used, such as the association of nanocarriers and physical methods. Thus, herein we address the development of nanoparticles based on poly-Ɛ-caprolactone (PCL), optimized with the Box–Behnken factorial design, for topical application of MB associated with sonophoresis. The MB-nanoparticles were developed using the double emulsification-solvent evaporation technique and the optimized formulation resulted in an average size of 156.93 ± 8.27 nm, a polydispersion index of 0.11 ± 0.05, encapsulation efficiency of 94.22 ± 2.19% and zeta potential of −10.08 mV ± 1.12. Morphological evaluation by scanning electron microscopy showed spherical nanoparticles. In vitro release studies show an initial burst compatible with the first-order mathematical model. The nanoparticle showed satisfactory generation of reactive oxygen species. The MTT assay was used to assess cytotoxicity and IC50; values of 79.84; 40.46; 22.37; 9.90 µM were obtained, respectively, for the MB-solution and the MB-nanoparticle without and with light irradiation after 2 h of incubation. Analysis using confocal microscopy showed high cellular uptake for the MB-nanoparticle. With regard to skin penetration, a higher concentration of MB was observed in the epidermis + dermis, corresponding to 9.81, 5.27 μg/cm2 in passive penetration and 24.31 and 23.81 μg/cm2 after sonophoresis, for solution-MB and nanoparticle-MB, respectively. To the best of our knowledge, this is the first report of MB encapsulation in PCL nanoparticles for application in skin cancer using PDT.

show abstract

“…The amounts of 5-FU deposited in different skin layers were determined as previously described with slight modifications [ 9 ]. Firstly, the dosed area on the pig skin was gently washed with MilliQ ® water (10 mL) to remove excess formulations on the surface and dried at room temperature for 2 h. The SC layer of the skin was then removed by a tape-stripping method.…”

Section: Methodsmentioning

confidence: 99%

“…Whilst 5-FU’s high melting point (291.82 °C) and low Log P (–0.85) may be indicative of unfavourable diffusion into the skin, an adequate aqueous solubility of 16.76 mg/mL and a low molecular weight of 130.01 g/mol may favour its skin permeation [ 8 ]. Although the accurate prediction of drug permeation using only a few physicochemical properties may not always be feasible, several studies demonstrated that 5-FU alone would generally have limited skin permeation [ 9 , 10 ].…”

Section: Introductionmentioning

confidence: 99%

Enhanced Skin Permeation of 5-Fluorouracil through Drug-in-Adhesive Topical Patches

Kim,

Youssef,

Lee

et al. 2024

Pharmaceutics

View full text Add to dashboard Cite

5-fluorouracil (5-FU), commercially available as a topical product, is approved for non-melanoma skin cancer (NMSC) treatment with several clinical limitations. This work aimed to develop 5-FU-loaded topical patches as a potential alternative to overcome such drawbacks. The patches offer accurate dosing, controlled drug release and improved patient compliance. Our study highlights the development of Eudragit® E (EuE)-based drug-in-adhesive (DIA) patches containing a clinically significant high level of 5-FU (approximately 450 µg/cm2) formulated with various chemical permeation enhancers. The patches containing Transcutol® (Patch-TRAN) or oleic acid (Patch-OA) demonstrated significantly higher skin penetration ex vivo than their control counterpart, reaching 5-FU concentrations of 76.39 ± 27.7 µg/cm2 and 82.56 ± 8.2 µg/cm2, respectively. Furthermore, the findings from in vitro permeation studies also validated the superior skin permeation of 5-FU achieved by Patch-OA and Patch-TRAN over 72 h. Moreover, the EuE-based DIA patch platform demonstrated suitable adhesive and mechanical properties with an excellent safety profile evaluated through an inaugural in vivo human study involving 11 healthy volunteers. In conclusion, the DIA patches could be a novel alternative option for NMSC as the patches effectively deliver 5-FU into the dermis layer and receptor compartment ex vivo for an extended period with excellent mechanical and safety profiles.

show abstract

Sorbitan Monolaurate–Containing Liposomes Enhance Skin Cancer Cell Cytotoxicity and in Association with Microneedling Increase the Skin Penetration of 5-Fluorouracil

Cited by 6 publications

References 53 publications

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

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

Nanoencapsulation of Methylene-Blue for Enhanced Skin Cancer Cell Phototoxicity and Cutaneous Penetration in Association with Sonophoresis

Enhanced Skin Permeation of 5-Fluorouracil through Drug-in-Adhesive Topical Patches

Contact Info

Product

Resources

About