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https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3918245/
The most common prodrug approach to deliver pharmacologically potent compounds is through esterase bioconversion. . The esterases involved in drug metabolism are mainly localized in the liver; among these are carboxyl- and butyrylcholinesterase, which can recognize acetate and phenylacetate groups as substrates.Author: Christian Perez, Kevin B. Daniel, Seth M. Cohen
https://www.tandfonline.com/doi/abs/10.1080/10717544.2019.1588424
Esterase-responsive nanoparticle system is widely used due to the overexpressed esterase in tumor cells. For a rational designed esterase-responsive nanoparticle, ester bonds and nanoparticle …Author: Haonan Dong, Long Pang, Hailin Cong, Youqing Shen, Youqing Shen, Bing Yu
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3530194/
Nov 15, 2012 · This report provides a synopsis of the esterase processing of short chain fatty acid (SCFA)-derivatized hexosamine analogs used in metabolic glycoengineering by demonstrating that the extracellular hydrolysis of these compounds is comparatively slow (e.g., with a t 1/2 of ~ 4 hours to several days) in normal cell culture as well as in high serum concentrations intended to mimic in vivo …Author: Mohit P. Mathew, Elaine Tan, Shivam Shah, Rahul Bhattacharya, M. Adam Meledeo, Jun Huang, Freddy A. ...
https://www.researchgate.net/publication/295884388_Esterases_involved_in_hydrolysis_of_prodrug_and_antedrugsoft_drug
The metabolic consideration is most important in the design of prodrug and antedrug/soft drug. Since esterase is abundantly present in several tissues, most of prodrugs and antedrugs/soft drugs are metabolized by esterases and fully converted to their active and inactive metabolite.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3601677/
Sep 07, 2012 · In the following sections, we have attempted to describe barrier properties of the cornea and conjunctiva to anterior segment drug delivery. Conjunctiva as a barrier The conjunctiva is a thin, transparent, elastic, highly vascularized tissue, internally lining the upper eyelid, lower eyelid, and anterior sclera covering almost 80% of the ocular surface.Author: Kishore Cholkar, Sulabh P. Patel, Aswani Dutt Vadlapudi, Ashim K. Mitra
https://www.ncbi.nlm.nih.gov/pubmed/3899454/
Cholinesterases are primarily involved in drug hydrolysis in the plasma, arylesterases in the plasma and red blood cells, and carboxylesterases in the liver, gut and other tissues. The esterases exhibit specificities for certain substrates and inhibitors but a drug is often hydrolysed by more than one esterase at different sites.Author: Faith M. Williams
http://www.pdr.net/drug-summary/Berinert-C1-esterase-inhibitor--human--1237
In a placebo-controlled, randomized study, the median time to the onset of unequivocal relief of angioedema symptoms was 2 hours with C1 inhibitor as compared with more than 4 hours with placebo. In addition, open-label receipt of C1 inhibitor led to a 100% response rate in 35 attacks including 15 laryngeal attacks.
https://www.nature.com/articles/s41467-018-03691-1
Apr 03, 2018 · Local delivery of therapeutics for the treatment of inflammatory arthritis (IA) is limited by short intra-articular half-lives. Since IA severity often fluctuates over time, a local drug delivery method that titrates drug release to arthritis activity would represent an attractive paradigm in IA therapy.Author: Nitin Joshi, Nitin Joshi, Nitin Joshi, Jing Yan, Jing Yan, Seth Levy, Seth Levy, Sachin Bhagchandani...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4407659/
Poor bioavailability of topically instilled drug is the major concern in the field of ocular drug delivery. Efflux transporters, static and dynamic ocular barriers often possess rate limiting factors for ocular drug therapy.Author: Megha Barot, Mahuya Bagui, Mitan R. Gokulgandhi, Ashim K. Mitra
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