Publication: Formulation development and in vitro evaluation of transferrin-conjugated liposomes as a carrier of ganciclovir targeting the retina
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Issued Date
2020
Resource Type
File Type
application/pdf
ISSN
3785173
Other identifier(s)
2-s2.0-85078451640
Rights Holder(s)
Scopus
Bibliographic Citation
International Journal of Pharmaceutics. Vol 577, (2020)
Suggested Citation
Asasutjarit R., Managit C., Phanaksri T., Treesuppharat W., Fuongfuchat A. Formulation development and in vitro evaluation of transferrin-conjugated liposomes as a carrier of ganciclovir targeting the retina. International Journal of Pharmaceutics. Vol 577, (2020). doi:10.1016/j.ijpharm.2020.119084 Retrieved from: https://hdl.handle.net/20.500.14740/4626
Abstract
Ganciclovir (GCV) is an antiviral drug approved for treatment of cytomegalovirus (CMV) retinitis. It can be delivered to the eye via systemic administrations. However, local delivery of GCV that targets the retina is considered as an alternative to increase efficacy of the treatment and lessen side effects. Thus, this study aimed to develop formulations of transferrin (Tf)-conjugated liposomes containing GCV (Tf-GCV-LPs) for intravitreal injection and topical instillation. Tf-GCV-LPs were prepared by the reverse-phase evaporation technique and then conjugated to Tf. Their physicochemical properties were evaluated. The optimized formulation was selected and subjected to the cytotoxicity test, cellular uptake study in the human retinal pigment epithelial cells (the ARPE-19 cells) and antiviral activity evaluation. The results showed that physicochemical properties of Tf-GCV-LPs were affected by formulation compositions. The optimized Tf-GCV-LPs had a particle size lower than 100 nm with a negative value of zeta potential. They were safe for the ARPE-19 cells. These Tf-GCV-LPs were taken up by these cells via Tf receptors-mediated endocytosis and showed inhibitory activity on CMV in the infected cells. Therefore, the optimized Tf-GCV-LPs could be accepted as a promising drug delivery system for targeted GCV delivery to the retina in the treatment of CMV retinitis. © 2020 Elsevier B.V.
Subject(s)
Drug carrier
Ganciclovir
Glycoprotein B
Liposome
Transferrin
Antivirus agent
Drug carrier
Ganciclovir
Liposome
Transferrin
Antiviral activity
ARPE-19 cell line
Article
Cell surface
Controlled study
Cytotoxicity test
Dispersity
Drug conjugation
Drug delivery system
Drug formulation
Drug release
Endocytosis
Endosome
Fourier transform infrared spectroscopy
Human
Human cell
In vitro study
Internalization
Particle size
Physical chemistry
Priority journal
Retina cell
Retinal pigment epithelium
Zeta potential
Cell line
Chemistry
Comparative study
Cytology
Cytomegalovirus retinitis
Intravitreal drug administration
Metabolism
Topical drug administration
Administration, Topical
Antiviral Agents
Cell Line
Cytomegalovirus Retinitis
Drug Carriers
Drug Delivery Systems
Ganciclovir
Humans
Intravitreal Injections
Liposomes
Particle Size
Retinal Pigment Epithelium
Transferrin
Ganciclovir
Glycoprotein B
Liposome
Transferrin
Antivirus agent
Drug carrier
Ganciclovir
Liposome
Transferrin
Antiviral activity
ARPE-19 cell line
Article
Cell surface
Controlled study
Cytotoxicity test
Dispersity
Drug conjugation
Drug delivery system
Drug formulation
Drug release
Endocytosis
Endosome
Fourier transform infrared spectroscopy
Human
Human cell
In vitro study
Internalization
Particle size
Physical chemistry
Priority journal
Retina cell
Retinal pigment epithelium
Zeta potential
Cell line
Chemistry
Comparative study
Cytology
Cytomegalovirus retinitis
Intravitreal drug administration
Metabolism
Topical drug administration
Administration, Topical
Antiviral Agents
Cell Line
Cytomegalovirus Retinitis
Drug Carriers
Drug Delivery Systems
Ganciclovir
Humans
Intravitreal Injections
Liposomes
Particle Size
Retinal Pigment Epithelium
Transferrin