2012
DOI: 10.1016/j.ejpb.2011.10.001
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Nonpolymeric nanoassemblies for ocular administration of acyclovir: Pharmacokinetic evaluation in rabbits

Abstract: The aim of this study was to increase bioavailability of the antiviral drug acyclovir (ACV) when administered by the ocular route. For this purpose, a new lipophilic derivative of acyclovir was synthesized, both possessing greater lipophilicity and providing the formation of a homogeneous water dispersion with higher amount of ACV than the aqueous solution of the parent drug. This was done by chemically linking acyclovir to the isoprenoid chain of squalene, obtaining 4′-trisnorsqualenoylacyclovir (SQACV), in w… Show more

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Cited by 24 publications
(17 citation statements)
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“…The apparent first order elimination rate constants (K e ) of CyA from the tear fluid and the corresponding half-lives (t 1 2 = 0.963/K e ) were calculated from linear phase of [log tear fluid concentration] vs. time plots [41]. The Areas Under Curve values (AUC) were calculated from 1 min to 30 min after instillation from appropriate graph applying the linear trapezoidal method.…”
Section: In Vivo Evaluation Of Precorneal Residence Time Of Cyamentioning
confidence: 99%
“…The apparent first order elimination rate constants (K e ) of CyA from the tear fluid and the corresponding half-lives (t 1 2 = 0.963/K e ) were calculated from linear phase of [log tear fluid concentration] vs. time plots [41]. The Areas Under Curve values (AUC) were calculated from 1 min to 30 min after instillation from appropriate graph applying the linear trapezoidal method.…”
Section: In Vivo Evaluation Of Precorneal Residence Time Of Cyamentioning
confidence: 99%
“…Nanotechnology is an advanced approach to produce nanoscale drug carriers with feasible potential for uniform delivery to mucosal tissue [ 12 , 13 , 14 ]. Previously published by our group data demonstrated that silver nanoparticles modified with tannic acid (TA-AgNPs) effectively reduced HSV-2 infectivity at the vaginal mucosal surface, suggesting a potential for nanoparticles as microbicide in HSV prevention [ 15 ].…”
Section: Introductionmentioning
confidence: 99%
“…The pharmacokinetic profile of the nanoassemblies in tear fluid and aqueous humor showed increased absorption of the drug as compared to free drug solution. [87] Recently, five new molecules were synthesized and characterized for their capacity to form NP in water and to encapsulate ACV with high loading and sustained release. [88] The features of NP used in clinical therapeutics like US FDA-approved nanomedicines were characterized through various analytical methods for physicochemical characterization, sterility, pyrogenicity assessment, biodistribution (absorption, distribution, metabolism and excretion) and toxicity studies.…”
Section: Nanoparticulate Delivery Systemsmentioning
confidence: 99%