Ocular pharmacokinetics and toxicity of nanoparticular acetazolamide: In vivo distribution and safety of PHBV-ACZ nanoparticle

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dc.authoridUGURLU, NAGIHAN/0000-0002-1072-6126
dc.authoridAKYOL, Mesut/0000-0003-1449-7874
dc.authoridBAKICI, CANER/0000-0003-2413-3142
dc.authoridYAMAN, MEHMET EMRAH/0000-0002-8406-7653
dc.authoridARSLAN, ASLIHAN/0000-0002-3520-608X
dc.authoridBatur, Baris/0000-0001-9669-9917
dc.contributor.authorErdal, Ebru
dc.contributor.authorBakici, Caner
dc.contributor.authorArslan, Aslihan
dc.contributor.authorBatur, Baris
dc.contributor.authorYaman, Mehmet Emrah
dc.contributor.authorAlcigir, Mehmet Eray
dc.contributor.authorAkyol, Mesut
dc.date.accessioned2025-01-21T16:43:01Z
dc.date.available2025-01-21T16:43:01Z
dc.date.issued2023
dc.departmentKırıkkale Üniversitesi
dc.description.abstractDiabetic macular edema (DME) is defined as fluid accumulation in the macular region, between the retinal layers, due to many diseases, especially diabetes. DME is one of the major complications of diabetic retinopathy (DRP). Carbonic anhydrase inhibitors (CAI) are a pharmaceutical agent used in different fields, especially glaucoma treatment. Acetazolamide (ACZ), which is a CAI, is an active substance that has been used off-label for many years in the treatment of macular edema due to diabetes and many other diseases. The low solubility and bioavailability of ACZ limit its use in the treatment of DME. In this study, a nanoparticulate formulation was developed that would increase the solubility and bioavailability of ACZ and allow it to be administered intravitreally. ACZ was loaded on poly(3-hydroxybutyrate-co-3-Hydroxyvalerate) (PHBV) nanoparticles and the loading efficiency was 71.58 +/- 1.22%. Toxicity of nanoparticles after intravitreal application was evaluated with anterior segment and posterior segment examination findings, intraocular pressure (IOP) measurements and electrophysiological tests. At the end of the 3-month follow-up, electroretinography (ERG) measurements demonstrated that ACZ loaded PHBV (PHBV-ACZ) nanoparticles did not cause loss of function in retinal cells. On histological examination, rare degenerative changes were observed in several cell groups. In addition, pharmacokinetic studies were performed to determine the tissue distribution of ACZ at various periods. ACZ was identified in vitreous humor and retina at the highest concentration. Based on our results, the prepared nanoparticle formulation can release long-term CAI for DRP therapy and accordingly can reduce the need for monthly intravitreal injections.
dc.description.sponsorshipTUBITAK [216S700]
dc.description.sponsorshipThis study was financially supported by TUBITAK with the project number 216S700.
dc.identifier.doi10.1016/j.ijpharm.2023.123336
dc.identifier.issn0378-5173
dc.identifier.issn1873-3476
dc.identifier.pmid37598873
dc.identifier.scopus2-s2.0-85170432700
dc.identifier.scopusqualityQ1
dc.identifier.urihttps://doi.org/10.1016/j.ijpharm.2023.123336
dc.identifier.urihttps://hdl.handle.net/20.500.12587/25187
dc.identifier.volume645
dc.identifier.wosWOS:001075206800001
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherElsevier
dc.relation.ispartofInternational Journal of Pharmaceutics
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_20241229
dc.subjectPharmacokinetic; In vivo toxicity; Nanoparticles; Poly(3-hydroxybutyrate-co-3-Hydroxyvalerate); Acetazolamide; Rabbit eye
dc.titleOcular pharmacokinetics and toxicity of nanoparticular acetazolamide: In vivo distribution and safety of PHBV-ACZ nanoparticle
dc.typeArticle

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