2015
DOI: 10.3390/molecules21010042
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The Prodrug Approach: A Successful Tool for Improving Drug Solubility

Abstract: Prodrug design is a widely known molecular modification strategy that aims to optimize the physicochemical and pharmacological properties of drugs to improve their solubility and pharmacokinetic features and decrease their toxicity. A lack of solubility is one of the main obstacles to drug development. This review aims to describe recent advances in the improvement of solubility via the prodrug approach. The main chemical carriers and examples of successful strategies will be discussed, highlighting the advanc… Show more

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Cited by 214 publications
(144 citation statements)
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References 122 publications
(127 reference statements)
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“…A successful approach to address this challenge has been the development of prodrugs that target the intestinal peptide transporter, PepT1 (SLC15A1) (4) ( SI Figure 1 ). Prodrugs are bioreversible derivatives of drug molecules that undergo an enzymatic or chemical transformation in vivo to release the active parent drug (5). Over the past 10 years significant effort has been made in the design of novel prodrug molecules with improved pharmacokinetic profiles (6).…”
Section: Introductionmentioning
confidence: 99%
“…A successful approach to address this challenge has been the development of prodrugs that target the intestinal peptide transporter, PepT1 (SLC15A1) (4) ( SI Figure 1 ). Prodrugs are bioreversible derivatives of drug molecules that undergo an enzymatic or chemical transformation in vivo to release the active parent drug (5). Over the past 10 years significant effort has been made in the design of novel prodrug molecules with improved pharmacokinetic profiles (6).…”
Section: Introductionmentioning
confidence: 99%
“…The most important criteria of mutual prodrugs is their stability in aqueous solution and gastrointestinal fluids (at different pHs), but they must be readily hydrolyzed by esterase enzyme in human blood plasma [46].…”
Section: Chemical Hydrolysismentioning
confidence: 99%
“…Geralmente, a estratégia inicial baseia-se no desenvolvimento de formulações, como, por exemplo, formação de sais e co-cristais, uso de 19 INTRODUÇÃO solubilizantes e tensoativos, redução do tamanho de partícula, dispersões sólidas, entre outros. A latenciação também é uma estratégia consolidada entre os pesquisadores que têm como objetivo aumentar a solubilidade em água de compostos farmacologicamente ativos, através de modificação molecular (STELLA, NTI-ADDAE, 2007;STEGEMANN et al, 2007;JORNADA et al, 2016;RAUTIO et al, 2018). Nesse caso, pode-se obter inovação, ainda que incremental, o que nem sempre é possível com o desenvolvimento de formulações.…”
Section: Takagi E Colaboradores (2006) Estimaram Que Aproximadamente 40%unclassified
“…Os principais grupos funcionais reversíveis utilizados na latenciação incluem carboxilas, hidroxilas, aminas, carbonilas e fosfatos. As modificações desses grupos no desenvolvimento de pró-fármacos dão origem a ésteres, carbonatos, carbamatos, amidas, fosfatos, entre outros (RAUTIO et al, 2008;JORNADA et al, 2016). Entre eles, a esterificação tem se mostrado muito promissora devido à suscetibilidade à hidrólise tanto in vivo quanto in vitro (TESTA, 2009;ZAWILSKA, WOJCIESZAK, OLEJNICZAK, 2013;JORNADA et al, 2016).…”
Section: Latenciaçãounclassified
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