Investigating the Effect of Esterification on Retinal Pigment Epithelial Uptake Using Rhodamine B Derivatives.
Transl Vis Sci Technol
; 9(6): 18, 2020 05.
Article
em En
| MEDLINE
| ID: mdl-32821515
ABSTRACT
Purpose:
This study investigated the effects of esterification and increased lipophilicity on cellular penetration, accumulation and retention in ARPE-19-nic cells using ester functionalized rhodamine B dyes.Methods:
Rhodamine B was esterified to generate four dyes with increasing lipophilicity. Cellular uptake, retention and mitochondrial localization were investigated in vitro using ARPE-19-nic cells using direct intracellular and extracellular and mitochondrial fluorescence quantitation, confocal and high-resolution live cell imaging and co-localization with Mito-GFP.Results:
Cellular penetrance, mitochondrial accumulation, and retention of the esterified dyes were increased in ARPE-19-nic cells compared with the nonesterified parent dye by direct fluorescence quantitation. Imaging demonstrated intracellular accumulation was confined to mitochondria as confirmed by colocalization with Mito-GFP.Conclusions:
Esterification is an effective way to increase lipophilicity of a dye to improve cellular penetration of chemical entities. These observations may be key to improving retinal drug delivery for retinal pigment epithelium-based diseases. Translational Relevance Understanding the intracellular distribution of drugs into retinal pigment epithelium cells is a critical component for identifying potential therapies for retinal pigment epithelium-based diseases.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pigmentos da Retina
/
Epitélio Pigmentado da Retina
Idioma:
En
Revista:
Transl Vis Sci Technol
Ano de publicação:
2020
Tipo de documento:
Article
País de afiliação:
Estados Unidos