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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Liposomes as carriers of hydrophilic small molecule drugs: Strategies to enhance encapsulation and delivery

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Eloy, Josimar Oliveira [1, 2] ; de Souza, Marina Claro [1] ; Petrilli, Raquel [1, 2] ; Abriata Barcellos, Juliana Palma [1] ; Lee, Robert J. [2] ; Marchetti, Juliana Maldonado [1]
Número total de Autores: 6
Afiliação do(s) autor(es):
[1] Univ Sao Paulo, Coll Pharmaceut Sci Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil
[2] Ohio State Univ, Coll Pharm, Columbus, OH 43210 - USA
Número total de Afiliações: 2
Tipo de documento: Artigo de Revisão
Fonte: COLLOIDS AND SURFACES B-BIOINTERFACES; v. 123, p. 345-363, NOV 1 2014.
Citações Web of Science: 148

Although hydrophilic small molecule drugs are widely used in the clinic, their rapid clearance, suboptimal biodistribution, low intracellular absorption and toxicity can limit their therapeutic efficacy. These drawbacks can potentially be overcome by loading the drug into delivery systems, particularly liposomes; however, low encapsulation efficiency usually results. Many strategies are available to improve both the drug encapsulation efficiency and delivery to the target site to reduce side effects. For encapsulation, passive and active strategies are available. Passive strategies encompass the proper selection of the composition of the formulation, zeta potential, particle size and preparation method. Moreover, many weak acids and bases, such as doxorubicin, can be actively loaded with high efficiency. It is highly desirable that once the drug is encapsulated, it should be released preferentially at the target site, resulting in an optimal therapeutic effect devoid of side effects. For this purpose, targeted and triggered delivery approaches are available. The rapidly increasing knowledge of the many overexpressed biochemical makers in pathological sites, reviewed herein, has enabled the development of liposomes decorated with ligands for cell-surface receptors and active delivery. Furthermore, many liposomal formulations have been designed to actively release their content in response to specific stimuli, such as a pH decrease, heat, external alternating magnetic field, ultrasound or light. More than half a century after the discovery of liposomes, some hydrophilic small molecule drugs loaded in liposomes with high encapsulation efficiency are available on the market. However, targeted liposomes or formulations able to deliver the drug after a stimulus are not yet a reality in the clinic and are still awaited. (C) 2014 Elsevier B.V. All rights reserved. (AU)

Processo FAPESP: 12/10388-3 - Lipossomas e imunolipossomas contendo fármacos antitumorais: desenvolvimento, caracterização e avaliação da eficácia contra o câncer de mama
Beneficiário:Josimar de Oliveira Eloy
Linha de fomento: Bolsas no Brasil - Doutorado
Processo FAPESP: 13/05362-8 - Funcionalização de lipossomas contendo paclitaxel e metformina com Trastuzumab: desenvolvimento, caracterização e avaliação da eficácia contra o câncer de mama
Beneficiário:Josimar de Oliveira Eloy
Linha de fomento: Bolsas no Exterior - Estágio de Pesquisa - Doutorado
Processo FAPESP: 12/21513-3 - Estratégias para veiculação de paclitaxel e metformina para otimização da terapia do câncer de mama: lipossomas e dendrímeros
Beneficiário:Juliana Maldonado Marchetti
Linha de fomento: Auxílio à Pesquisa - Regular