Prodrug design for improving the biopharmaceutical properties of therapeutic drugs

Choudhary, Devendra; Goykar, Hanmant; Kalyane, Dnyaneshwar; Sreeharsha, Nagaraja; Tekade, Rakesh K.

doi:10.1016/b978-0-12-814455-8.00006-2

Cited by 11 publications

(5 citation statements)

References 38 publications

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“…The improvement of the properties of a drug by a prodrug design process should consider some criteria, such as the existence of functional groups capable of undergoing reversible derivatization; the existence of mechanisms in the organism able to bioactivate the prodrug; facility and simplicity of the synthesis and purification of the prodrug; chemical stability of the prodrug; regeneration, in vivo , of the parent molecule in ideal amounts. In addition, the drug carrier must have low toxicity. − …”

Section: Carbon Nanotubesmentioning

confidence: 99%

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A Review on Carbon Nanotubes Family of Nanomaterials and Their Health Field

Brito,

Silva,

Gonzaga

et al. 2024

ACS Omega

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The use of carbon nanotubes (CNTs), which are nanometric materials, in pathogen detection, protection of environments, food safety, and in the diagnosis and treatment of diseases, as efficient drug delivery systems, is relevant for the improvement and advancement of pharmacological profiles of many molecules employed in therapeutics and in tissue bioengineering. It has contributed to the advancement of science due to the development of new tools and devices in the field of medicine. CNTs have versatile mechanical, physical, and chemical properties, in addition to their great potential for association with other materials to contribute to applications in different fields of medicine. As, for example, photothermal therapy, due to the ability to convert infrared light into heat, in tissue engineering, due to the mechanical resistance, flexibility, elasticity, and low density, in addition to many other possible applications, and as biomarkers, where the electronic and optics properties enable the transduction of their signals. This review aims to describe the state of the art and the perspectives and challenges of applying CNTs in the medical field. A systematic search was carried out in the indexes Medline, Lilacs, SciELO, and Web of Science using the descriptors "carbon nanotubes", "tissue regeneration", "electrical interface (biosensors and chemical sensors)", "photosensitizers", "photothermal", "drug delivery", "biocompatibility" and "nanotechnology", and "Prodrug design" and appropriately grouped. The literature reviewed showed great applicability, but more studies are needed regarding the biocompatibility of CNTs. The data obtained point to the need for standardized studies on the applications and interactions of these nanostructures with biological systems.

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Section: Carbon Nanotubesmentioning

confidence: 99%

“…The bond between drug/bioactive compound must be reversible, and it depends on the chemical groups available in the parent drug/bioactive compound. This and the purpose of the designing allow one to choose the proper carrier, which must be nontoxic, in principle. − …”

Section: Carbon Nanotubesmentioning

confidence: 99%

A Review on Carbon Nanotubes Family of Nanomaterials and Their Health Field

Brito,

Silva,

Gonzaga

et al. 2024

ACS Omega

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“…Different anti-viral stratagems have been employed for the provision of the drug at the location of action. Prodrug plays an important role in the optimization of effect (Choudhary et al, 2020). For example, HIV infection has become a chronic disease due to the disproportionate use of anti-viral medicines so the drugs are given in combination e.g.…”

Section: Prodrug Approaches For Viral Diseasesmentioning

confidence: 99%

Approaches of Prodrug Designing to Treat Cancer, Neurodegenerative Disorders and Viral Diseases

Ashraf

Rehman

Fatima

et al. 2020

GDDDR

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Classical prodrug design is a sweeping approach to throw away futile side effects related to drug therapy. The main purpose of prodrug designing is to ameliorate physicochemical, pharmaceutical, and pharmacokinetic characteristics of particular compounds to resolve issues like formulation, delivery to the target site, and toxicity limitations. To fabricate the pharmacological action in CNS, drugs must cross the blood-brain barrier (BBB). Therefore, prodrug strategies are designed which include lipidization and the use of carriers and transporters. In this article, we have reviewed different anticancer, neuroprotective, and antiviral prodrugs. Flurbiprofen prodrugs, glycosylated prodrugs, resveratrol prodrugs, levodopa, etc., are mapped out for neurodegenerative disorders in CNS. Due to the poor oral pharmacokinetic properties of antiviral agents, drug design methods are performed by combining the parent drug molecule with a number of active components such as dipeptide esters, amino acids, nucleosides, and macromolecular-based prodrugs.

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“…The synthesized mutual prodrugs have less GI-irritancy with improved therapeutic effects (25)(26) . The main objectives of the development of prodrugs are to ameliorate the stability, improve solubility profile, decrease side effects, enhance the bioavailability, enhanced penetration and permeability which lead to increase therapeutic potential (27)(28) .…”

Section: Introductionmentioning

confidence: 99%

Chemical Characterization and Pharmacological Evaluation of Phytophenols-Etodolac Mutual Prodrugs

Shah,

Krishna

2023

IJPS

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Etodolac is choice of drug for pain and inflammation but has major side effects of gastric ulcers that are due to free carboxylic group. Etodolac belongs to the chemical class of non-selective COX-inhibitor but preferentially COX-2 inhibitor. Here the ester linked mutual prodrugs of etodolac with phytophenols like vanillin, carvacrol, umbelliferone, guaiacol, sesamol and syringaldehyde were synthesized. All the prodrugs were characterized by IR-spectroscopy, 1H-NMR, 13C-NMR and mass spectrometry. Among the synthesized prodrugs, the Eto-van, Eto-umbe, Eto-sesa and Eto-syr showed improved analgesic and anti-inflammatory activity compared to etodolac. All the synthesized prodrugs showed less ulcerogenic side effects compared to etodolac.

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Prodrug design for improving the biopharmaceutical properties of therapeutic drugs

Cited by 11 publications

References 38 publications

A Review on Carbon Nanotubes Family of Nanomaterials and Their Health Field

A Review on Carbon Nanotubes Family of Nanomaterials and Their Health Field

Approaches of Prodrug Designing to Treat Cancer, Neurodegenerative Disorders and Viral Diseases

Chemical Characterization and Pharmacological Evaluation of Phytophenols-Etodolac Mutual Prodrugs

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