Simultaneous modulation of transport and metabolism of acyclovir prodrugs across rabbit cornea: An approach involving enzyme inhibitors

Suresh, K.; Talluri, Ravi S.; Mitra, Ashim K.

doi:10.1016/j.ijpharm.2006.04.010

Cited by 10 publications

(13 citation statements)

References 29 publications

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“…Complete inhibition of VACV hydrolysis was observed in the presence of 4-(2-aminoethyl)benzenesulfonyl fluoride and pchloromercuribenzoic acid. Similar trend was also observed with GVACV in the presence of bestatin [69].…”

Section: Enzyme Inhibitors To Modulate Prodrugs Transport and Metabolismsupporting

confidence: 85%

Phase I and Phase II Ocular Metabolic Activities and the Role of Metabolism in Ophthalmic Prodrug and Codrug Design and Delivery

Al-Ghananeem

Crooks

2007

Molecules

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While the mammalian eye is seldom considered an organ of drug metabolism, the capacity for biotransformation is present. Compared to the liver, the metabolic capabilities of the eye are minuscule; however, phase I and phase II metabolic activities have been detected in various ocular structures. The careful consideration of ocular tissue metabolic processes within the eye has important implications for controlling the detoxification of therapeutic agents and for providing the potential for site-specific bio-activation of certain drug molecules, thus enabling significant improvements in drug efficacy and the minimization of side-effect from either local or systemic drug delivery to the eye. Knowledge of these processes is important to prodrug and codrug development and to researchers involved in the design, delivery and metabolism of ophthalmic drugs. This present article reviews the progress in ocular prodrug and codrug design and delivery in light of ocular metabolic activities.

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Section: Enzyme Inhibitors To Modulate Prodrugs Transport and Metabolismsupporting

confidence: 85%

Phase I and Phase II Ocular Metabolic Activities and the Role of Metabolism in Ophthalmic Prodrug and Codrug Design and Delivery

Al-Ghananeem

Crooks

2007

Molecules

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show abstract

“…The hydrolysis mechanism of dipeptide prodrugs of acyclovir was explained before. (Anand et al, 2003a;Anand et al, 2003b;Katragadda et al, 2006) The peptidases hydrolyze the dipeptide bond generating the amino acid ester of acyclovir which will be further hydrolyzed by esterase producing acyclovir. Formation of acyclovir directly from dipeptide is also possible albeit to a small extent (Fig.…”

Section: Discussionmentioning

confidence: 99%

“…amino acid conjugate formed from the dipeptide conjugate. (Katragadda et al, 2006) Hence both the rate of formation (R f ) and degradation (R d ) of the transient amino acid conjugate will affect the cellular permeability of dipeptide conjugate (Fig. 8).…”

Section: Discussionmentioning

confidence: 99%

Synthesis, metabolism and cellular permeability of enzymatically stable dipeptide prodrugs of acyclovir

Talluri

Samanta

Gaudana

et al. 2008

International Journal of Pharmaceutics

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“…32 The results are represented as mean ± SEM. Student's t-test (unpaired) was used to compare the significance between the control and blocker pre-treated groups using SigmaStat statistical software programme ver.2.0 (Jandel, San Jose, CA, USA).…”

Section: Pharmacokinetics and Statistical Analysismentioning

confidence: 99%

Potential pharmacokinetic role of organic cation transporters in modulating the transcorneal penetration of its substrates administered topically

Nirmal

Singh

Biswas

et al. 2013

Eye

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Simultaneous modulation of transport and metabolism of acyclovir prodrugs across rabbit cornea: An approach involving enzyme inhibitors

Cited by 10 publications

References 29 publications

Phase I and Phase II Ocular Metabolic Activities and the Role of Metabolism in Ophthalmic Prodrug and Codrug Design and Delivery

Phase I and Phase II Ocular Metabolic Activities and the Role of Metabolism in Ophthalmic Prodrug and Codrug Design and Delivery

Synthesis, metabolism and cellular permeability of enzymatically stable dipeptide prodrugs of acyclovir

Potential pharmacokinetic role of organic cation transporters in modulating the transcorneal penetration of its substrates administered topically

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