Topical chemotherapy with 5-fluorouracil

Goette, Detlef K.

doi:10.1016/s0190-9622(81)80196-x

Cited by 220 publications

(85 citation statements)

References 113 publications

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“…In this regard, and to test whether our peptide dendrimers possessed permeation enhancing properties, we selected the relevant model drug, 5-fluorouracil (5-FU) for use in skin-based studies. 5-FU is an anticancer agent used in the treatment of skin, breast and gastrointestinal cancers, while also showing efficacy in the topical treatment of psoriasis, premalignant and malignant skin conditions (Tsuji & Sugai, 1975;Goette, 1981;Diasio & Harris, 1989). Separately, there are also a few reports on the use of chemicals to enhance the skin permeation of 5-FU.…”

Section: Introductionmentioning

confidence: 99%

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

et al. 2013

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Enhancing the deposition and permeation of 5-fluorouracil across human epidermis assisted by appropriately charged and well-defined peptide dendrimers was investigated. Peptide dendrimers with arginine as the terminal amino acid and having a range of terminal positive charges (4þ and 16 þ ) were synthesized by solid phase peptide synthesis. Various parameters including effect of peptide dendrimers on the solubility and partition coefficient of 5-FU, degradation of drug in skin as well as deposition and permeation of 5-FU in/through skin were studied. All the tested dendrimers increased the aqueous solubility and partition coefficient of 5-FU with each also significantly (p50.05) enhancing the deposition and permeation of 5-FU in/across human epidermis in a concentration-dependent manner. Of the three peptide dendrimers examined, R8 dendrimer (bearing 8 þ charge derived from four terminal arginines and MW of &1000 Da) showed greatest values for flux, Q 48 (cumulative amount of drug permeated at the end of 48 h) and amount of drug retained in human skin. Furthermore, this study also scrutinized and reports on the likely mechanisms by which peptide dendrimers act as transdermal permeation enhancers.

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Section: Introductionmentioning

confidence: 99%

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

et al. 2013

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“…Los pacientes que desarrollan otro cáncer de piel no melanoma durante cinco años de seguimiento tienen un riesgo elevado para desarrollar melanoma (al menos en pacientes con fototipos I y II). En efecto, se ha calculado que el riesgo de presentar otro CBC es del 17 % durante el primer año, 35 % en los tres primeros años y 50 % en los cinco primeros años (31,32,33).…”

Section: Seguimientounclassified

Cáncer de piel: Una realidad cotidianamente ignorada.

Piñeros

Osorio

2017

carta comunitaria

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INTRODUCCIÓNLa piel es el mayor órgano del cuerpo humano. Ocupa aproximadamente 2 m 2 y su espesor varía entre los 0,5 mm (en los párpados) y los 4 mm (en el talón). Su peso aproximado es de 5 kg. Actúa como barrera protectora que aísla al organismo del medio que lo rodea, protegiéndolo y contribuyendo a mantener íntegras sus estructuras, al tiempo que actúa como sistema de comunicación con el entorno.Dado el tamaño y características de este órgano, podemos afirmar que el cáncer de piel es la patología tumoral maligna más común, especialmente en sujetos de raza blanca como lo veremos más adelante (1, 2).

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“…For 5-fluorouracil (5FU) (log P = −0.89) which is one hydrophilic model drug used to treat skin diseases, has been reporte to have very poor penetration in skin [196][197][198]. Many strategies to increase skin permeation of this drug have been tested: prodrugs, terpenes, fatty acids, iontophoresis, sonophoresis, laser ablation and dendrimers which increased 5FU permeation across the skin by altering the skin structure [198][199][200][201][202][203].…”

Section: Applications Of Nanocarrier Systems In Topical/transdermal Dmentioning

confidence: 99%

“…Many strategies to increase skin permeation of this drug have been tested: prodrugs, terpenes, fatty acids, iontophoresis, sonophoresis, laser ablation and dendrimers which increased 5FU permeation across the skin by altering the skin structure [198][199][200][201][202][203].…”

Section: Applications Of Nanocarrier Systems In Topical/transdermal Dmentioning

confidence: 99%

Nanocarrier Systems for Transdermal Drug Delivery

Escobar-Chávez¹,

Rodríguez-Cruz²,

Domínguez-Delgado³

et al. 2012

Recent Advances in Novel Drug Carrier Systems

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is an open discussion, in one hand, the nanotechnologist continue making new and more sophisticated nanocarriers and in the other hand, toxicologist continue evaluating possible damaging effects.Whatever it happens, nanotechnology is the new era and nanomedicine cannot be taking off. New nanocarriers will be created and the entire scientist working in nanomedicine bet for it to be the cure of diseases that in this moment are difficult to deal with [3] The application of preparations to the skin for medical purposes is as old as the history of medicine itself, with references to the use of ointments and salves found in the records of Babylonian and Egyptian medicine. The historical development of permeation research is well described by Hadgraft & Lane [4]. Over time, the skin has become an important route for drug delivery in which topical, regional or systemic effects are desired. Nevertheless, skin constitutes an excellent barrier and presents difficulties for the transdermal delivery of therapeutic agents, since few drugs possess the characteristics required to permeate across the stratum corneum in sufficient quantities to reach a therapeutic concentration in the blood. In order to enhance drug transdermal absorption different methodologies have been investigated developed and patented [5,6]. Improvement in physical permeationenhancement technologies has led to renewed interest in transdermal drug delivery. Some of these novel advanced transdermal permeation enhancement technologies include: iontophoresis, electroporation, ultrasound, microneedles to open up the skin and more recently the use of transdermal nanocarriers [3,[7][8][9][10].A number of excellent reviews that have been published contain detailed discussions concerning many aspects of transdermal nanocarriers [11][12][13][14][15][16][17]. The present chapter shows an updated overview of the use of submicron particles and other nanostructures in the pharmaceutical field, specifically in the area of topical and transdermal drugs. This focus is justified due to the magnitude of the experimental data available with the use of these nanocarriers. The development of submicron particles and other nanostructures in the pharmaceutical and cosmetic fields has been emerged in the last decades for designing best formulations for application through the skin [18][19][20][21]. The skinThe skin is the largest organ of the body [22][23][24], accounting for more than 10% of body mass, and the one that enables the body to interact more intimately with its environment. Essentially, the skin consists of four layers: The SC, that is the outer layer of the skin (nonviable epidermis), and forms the rate-controlling barrier for diffusion for almost all compounds. It is composed of dead flattened, keratin-rich cells, the corneocytes. These dense cells are surrounded by a complex mixture of intercellular lipids, namely, ceramides, free fatty acids, cholesterol, and cholesterol sulphate. Their most important feature is that they are structured as ordered bilayer arrays [25]...

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Topical chemotherapy with 5-fluorouracil

Cited by 220 publications

References 113 publications

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

Cáncer de piel: Una realidad cotidianamente ignorada.

Nanocarrier Systems for Transdermal Drug Delivery

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