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Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir.

ABSTRACT: Delivering drugs via the ocular route has always been a challenge for poorly soluble drugs. The various anatomical and physiological barriers in the eye cavity hinder the residence of drugs within the corneal and precorneal regions. In this study, the nanosystem that could sufficiently deliver the poorly soluble Acyclovir topically via ocular route. Our nanosystem is composed of the biocompatible PLGA polymer stabilized with TPGS which possess a high emulsifying capacity and is also known as P-gp inhibitor. The optimized nanoparticles were prepared with 0.3% TPGS and had particle-size of 262.3?nm, zeta-potential of +15.14?mV. The physicochemical-characterization, ex vivo transcorneal permeation, ocular-irritation and Acyclovir ocular-availability, following topical ocular application of PLGA-NPs in rabbit eyes, were performed. The tested parameters and irritation by Draize's test suggested the suitability and safety of PLGA-NPs for ocular use. An ultrahigh performance liquid chromatographic method was developed, validated, and applied to quantify Acyclovir in aqueous humor which was shown to be significantly higher (p?0-24h, t_1/2 (h) and MRT_0-24h were found, respectively, with the PLGA-TPGS-NPs as compared to ACY-AqS. These results demonstrate the superiority of delivering Acyclovir using a nanosystem compared to conventional methods.

SUBMITTER: Alkholief M

PROVIDER: S-EPMC6362158 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature

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Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir.

Alkholief Musaed M Albasit Hammam H Alhowyan Adel A Alshehri Sultan S Raish Mohammad M Abul Kalam Mohd M Alshamsan Aws A

Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society 20181123 2

Delivering drugs via the ocular route has always been a challenge for poorly soluble drugs. The various anatomical and physiological barriers in the eye cavity hinder the residence of drugs within the corneal and precorneal regions. In this study, the nanosystem that could sufficiently deliver the poorly soluble Acyclovir topically via ocular route. Our nanosystem is composed of the biocompatible PLGA polymer stabilized with TPGS which possess a high emulsifying capacity and is also known as P-g ...[more]

PMID: 30766442

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Project description:BackgroundIntravenous (IV) hydration is considered a protective factor in reducing the incidence of acyclovir-induced nephrotoxicity. A systems-based review of cases of acyclovir-associated acute kidney injury can be used to examine institution-, care provider-, and task-related factors involved in administering the drug and can serve as a basis for developing a quality improvement intervention to achieve safer administration of acyclovir.ObjectivesTo explore the effectiveness of the study institution's inter-disciplinary quality improvement intervention in increasing the dilution of acyclovir before IV administration.MethodsAfter conducting a systems-based review for intervention development, a retrospective analysis was undertaken to compare IV administration of acyclovir in the 6-month periods before and after implementation of the intervention. The study population was a sequential sample of all patients over 18 years of age who were seen in the emergency department or admitted to a ward and who received at least one IV dose of acyclovir at the study institution. The primary outcome was the volume in which each acyclovir dose was delivered. The secondary outcomes were the hourly rate of fluid administration, the frequency of an increase in hourly hydration rate, and the incidence of acute kidney injury.ResultsEighty-four patients (44 in the pre-intervention period and 40 in the post-intervention period) received IV acyclovir and had evaluable data for the primary outcome. The median volume in which the acyclovir dose was administered was significantly higher in the post-intervention group (250 mL versus 100 mL, p < 0.001).ConclusionsIn this study, an easily implemented intervention significantly increased the volume of IV fluid administered to patients receiving acyclovir. Adequately powered prospective studies are suggested to investigate the effectiveness of this intervention on the clinically relevant incidence of acyclovir-induced nephrotoxicity.

Dataset Information

Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir.

Publications

Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir.

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