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Aspectos fundamentais no desenvolvimento de sistemas microemulsionados contendo anfotericina B para uso oftálmico

Authors: Lima Silveira, Walteçá Louis; de Lima Damasceno, Bolivar Ponciano Goulart; Silva, Kattya Gyselle Holanda; Oliveira, Anselmo Gomes de; Egito, Eryvaldo Sócrates Tabosa;

Aspectos fundamentais no desenvolvimento de sistemas microemulsionados contendo anfotericina B para uso oftálmico

Abstract

A exemplo do que ocorre com outros fármacos, a biodisponibilidade da anfotericina B (AmB) através da via ocular repreesenta um grande desafio para a pesquisa científica. Na verdade, a baixa biodisponibilidade apresentada por tal molécula é devido, principalmente, a presença das barreiras oculares que impedem a absorção deste fármaco para os tecidos internos. A toxicidade associada a este fármaco, assim como a sua baixa capacidade em permear a córnea íntegra também consiste em um problema associado ao seu uso clínico. Novos veículos seguros e eficazes para a liberação ocular da AmB são, portanto, necessários. As microemulsões (MEs) aparecem como um interessante sistema devido à sua transparência, estabilidade termodinâmica e favorável viscosidade. O conhecimento do processo de formação das MEs contendo AmB, assim como a compreensão de toda a sua caracterização físico- química correspondem a aspectos importantes para se determinar as condições favoráveis para que estes sistemas venham a ser empregados como colírios. Esta revisão tem como objetivo, portanto, abordar este tema enfatizando os principais aspectos relacionados com a utilização de MEs como sistemas de liberação para a AmB através da via tópica oftálmica.

As occurs with a number of drugs, the bioavailability of amphotericin B (AmB) used to treat fungal infections by the ocular route remains a great challenge to research scientists. In fact, the poor bioavailability of AmB is due mainly to the corneal barrier, which leads to a precorneal loss and consequent decrease in the absorption of this drug into the intraocular tissues. The toxicity associated with this molecule, together with its poor ability to penetrate the intact corneal epithelium, also represents a major drawback to its clinical use. New effective and safe drug vehicles for ocular delivery of AmB are therefore urgently needed. Microemulsions (MEs) seem to be an interesting system, owing to their transparent appearance, thermodynamic stability and favorable viscosity. Knowledge of the process of formation of AmB-containing MEs, as well as a good understanding of the physical chemistry of such systems, would provide reliable information on the best conditions for the use of these systems as eye drops. The goal of this research was thus to make an approach to this subject by reviewing the main studies on the use of MEs as delivery systems for AmB in topical eye treatment.

Country
Brazil
Keywords

drug vehicle, Anfotericina B, Eye, Microemulsões, cornea epithelium, thermodynamics, Pharmacy and materia medica, Amphotericin B, physical chemistry, human, Pharmaceutical industry, drug absorption, drug bioavailability, Anfotericina B. Microemulsões. Olho. Soluções Oftálmicas., Ophthalmic solutions, microemulsion, amphotericin B, fungal eye infection, RS1-441, ophthalmology, Soluções Oftálmicas, Microemulsions, Olho, HD9665-9675

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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
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