Approaches for Prodrugs

Redasani, Vivekkumar K.; Bari, Sanjay B.

doi:10.1016/b978-0-12-803519-1.00004-0

Cited by 12 publications

(13 citation statements)

References 5 publications

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“…The ensuing mode-of-action would resemble that of small-molecule prodrugs, which have been in the pharmacopoeia for decades. 15 …”

mentioning

confidence: 99%

“…In other words, GFP– 1 appears to enter cells by passing directly through the plasma membrane, like a small-molecule prodrug. 15 …”

mentioning

confidence: 99%

“…Thus, the esters formed upon reaction with 1 are substrates for endogenous esterases, like prodrugs. 15 Moreover, the alcohol product of the esterase-mediated hydrolysis is benign to mammalian cells (Figure S8). …”

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confidence: 99%

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Cytosolic Delivery of Proteins by Bioreversible Esterification

Lomax²,

2017

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Cloaking its carboxyl groups with a hydrophobic moiety is shown to enable a protein to enter the cytosol of a mammalian cell. Diazo compounds derived from (p-methylphenyl)glycine were screened for the ability to esterify the green fluorescent protein (GFP) in an aqueous environment. Esterification of GFP with 2-diazo-2-(p-methylphenyl)-N,N-dimethylacetamide was efficient. The esterified protein entered the cytosol by traversing the plasma membrane directly, like a small-molecule prodrug. As with prodrugs, the nascent esters are substrates for endogenous esterases, which regenerate native protein. Thus, esterification could provide a general means to deliver native proteins to the cytosol.

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“…The ensuing mode-of-action would resemble that of small-molecule prodrugs, which have been in the pharmacopoeia for decades. 15 …”

mentioning

confidence: 99%

“…In other words, GFP– 1 appears to enter cells by passing directly through the plasma membrane, like a small-molecule prodrug. 15 …”

mentioning

confidence: 99%

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Cytosolic Delivery of Proteins by Bioreversible Esterification

Lomax²,

2017

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“…Pacelli et al [ 51 ] used dextran-polyethene glycol cryogels to produce scaffolds exhibiting cytocompatibility with controlled vitamin B12 release profiles. Additionally, dextran-drug conjugates such as dextran-flurbiprofen and dextran-suprofen resulted in better therapeutic effects by enhancing their analgesic and antipyretic properties whilst reducing their constituent drug’s ulcerogenic effect [ 52 ]. Valproic acid-dextran conjugates have been shown to possess anticonvulsant properties as well as reducing the hepatocyte-toxicity and ulcerogenic effect of the epilepsy drug [ 53 ].…”

Section: The History Contemporary Status and Future Applicationsmentioning

confidence: 99%

Biomedical Applications of Bacteria-Derived Polymers

et al. 2021

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Plastics have found widespread use in the fields of cosmetic, engineering, and medical sciences due to their wide-ranging mechanical and physical properties, as well as suitability in biomedical applications. However, in the light of the environmental cost of further upscaling current methods of synthesizing many plastics, work has recently focused on the manufacture of these polymers using biological methods (often bacterial fermentation), which brings with them the advantages of both low temperature synthesis and a reduced reliance on potentially toxic and non-eco-friendly compounds. This can be seen as a boon in the biomaterials industry, where there is a need for highly bespoke, biocompatible, processable polymers with unique biological properties, for the regeneration and replacement of a large number of tissue types, following disease. However, barriers still remain to the mass-production of some of these polymers, necessitating new research. This review attempts a critical analysis of the contemporary literature concerning the use of a number of bacteria-derived polymers in the context of biomedical applications, including the biosynthetic pathways and organisms involved, as well as the challenges surrounding their mass production. This review will also consider the unique properties of these bacteria-derived polymers, contributing to bioactivity, including antibacterial properties, oxygen permittivity, and properties pertaining to cell adhesion, proliferation, and differentiation. Finally, the review will select notable examples in literature to indicate future directions, should the aforementioned barriers be addressed, as well as improvements to current bacterial fermentation methods that could help to address these barriers.

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“…This approach offers improved drug solubility, stability, drug release and pharmacokinetics. Additionally, it can facilitate the accumulation of a drug at the site of action and improve safety [9,10]. Bioprecursors are inactive compounds that do not have a carrier and are rapidly converted to an active drug after metabolic reactions (normally redox reactions) [5,8].…”

Section: Introductionmentioning

confidence: 99%

The Prodrug Approach: A Successful Tool for Improving Drug Solubility

et al. 2015

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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 advances of this field in the last ten years.

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Approaches for Prodrugs

Cited by 12 publications

References 5 publications

Cytosolic Delivery of Proteins by Bioreversible Esterification

Cytosolic Delivery of Proteins by Bioreversible Esterification

Biomedical Applications of Bacteria-Derived Polymers

The Prodrug Approach: A Successful Tool for Improving Drug Solubility

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