Atorvastatin-loaded solid lipid nanoparticles as eye drops: proposed treatment option for age-related macular degeneration (AMD)



Downloads per month over past year

Yadav, Monika and Schiavone, Nicola and Guzmán Aránguez, Ana Isabel and Giansanti, Fabrizio and Papucci, Laura and Pérez de Lara, María Jesús and Singh, Mandeep and Kaur, Indu Pal (2020) Atorvastatin-loaded solid lipid nanoparticles as eye drops: proposed treatment option for age-related macular degeneration (AMD). Drug Delivery and Translational Research . ISSN 2190-393X

[thumbnail of Aranguez_Yadav2020_Article_Atorvastatin-loadedSolidLipidN.pdf] PDF
Restringido a Repository staff only


Official URL:


Statins, widely prescribed for cardiovascular diseases, are also being eyed for management of age-related macular degeneration (AMD). Poor bioavailability and blood-aqueous barrier may however limit significant ocular concentration of statins following oral administration. We for the first time propose and investigate local application of atorvastatin (ATS; representative statin) loaded into solid lipid nanoparticles (SLNs), as self-administrable eye drops. Insolubility, instability, and high molecular weight > 500 of ATS, and ensuring that SLNs reach posterior eye were the challenges to be met. ATS-SLNs, developed (2339/DEL/2014) using suitable components, quality-by-design (QBD) approach, and scalable hot high-pressure homogenization, were characterized and evaluated comprehensively for ocular suitability. ATS-SLNs were 8 and 12 times more bioavailable (AUC) in aqueous and vitreous humor, respectively, than free ATS. Three-tier (in vitro, ex vivo, and in vivo) ocular safety, higher corneal flux (2.5-fold), and improved stability (13.62 times) including photostability of ATS on incorporation in ATS-SLNs were established. Autoclavability and aqueous nature are the other highlights of ATS-SLNs. Presence of intact fluorescein-labeled SLNs (F-SLNs) in internal eye tissues post–in vivo application as eye drops provides direct evidence of successful delivery. Perinuclear fluorescence in ARPE-19 cells confirms the effective uptake of F-SLNs. Prolonged residence, up to 7 h, was attributed to the mucus-penetrating nature of ATS-SLNs.

Item Type:Article
Uncontrolled Keywords:Ocular delivery, In vivo safety, Uptake studies, Ocular pharmacokinetics, Posterior eye delivery, Statins, Nanostructured carriers
Subjects:Sciences > Chemistry > Biochemistry
Medical sciences > Medicine > Ophtalmology
Medical sciences > Optics > Eyes anatomy
ID Code:60467
Deposited On:13 May 2020 08:12
Last Modified:13 May 2020 10:09

Origin of downloads

Repository Staff Only: item control page