Abstract
Age-related macular degeneration is a multifactorial disease affecting the posterior segment of the eye and is characterized by aberrant nascent blood vessels that leak blood and fluid. It ends with vision loss. In the present study, artemisinin which is poorly water-soluble and has potent anti-angiogenic and anti-inflammatory properties was formulated into nanomicelles and characterized for its ocular application and anti-angiogenic activity using a CAM assay. Artemisinin-loaded nanomicelles were prepared by varying the concentrations of PVP k90 and poloxamer 407 at different ratios and showed spherical shape particles in the size range of 41–51 nm. The transparency and cloud point of the developed artemisinin-loaded nanomicelles was found to be 99–94% and 68–70 °C, respectively. The in vitro release of artemisinin from the nanomicelles was found to be 96.0–99.0% within 8 h. The trans-corneal permeation studies exhibited a 1.717–2.169 µg permeation of the artemisinin from nanomicelles through the excised rabbit eye cornea for 2 h. Drug-free nanomicelles did not exhibit noticeable DNA damage and showed an acceptable level of hemolytic potential. Artemisinin-loaded nanomicelles exhibited remarkable anti-angiogenic activity compared to artemisinin suspension. Hence, the formulated artemisinin-loaded nanomicelles might have the potential for the treatment of AMD.
Highlights
Current treatment options adopted for posterior segment eye diseases such as agerelated macular degeneration (AMD) are far from satisfactory due to the limited exposure of therapeutic drugs to the posterior segment of the eye with poor bioavailability [1,2]
The interactions between the drug and the excipients were analyzed by comparing the FTIR spectra of the pure drug, the individual excipients, the physical mixture, the processed mixture of the polymer and the polymeric surfactant and the artemisinin-loaded nanomicelles
The cloudiness that appeared in the tested artemisinin-loaded nanomicelle disappeared upon the decrease in temperature just below the cloud point and this happened within a few minutes. These results indicate that the developed artemisinin-loaded nanomicelles might be stable at body temperature
Summary
Attempts to increase the dose of drugs may lead to posterior segment toxicity [3,4]. Site specific intravitreal injections/implants may improve the localized drug concentration which results in cataract development, endophthalmitis, haemorrhage and retinal detachment [5]. Administered drugs are penetrated and distributed into the posterior segment of the eye through diffusion across ocular tissues, trans-corneal permeation, direct entry through uvea and lateral diffusion across sclera and conjunctiva [8,9]. The topical application of particulate drug delivery systems such as nanosuspension, nanodispersion, nanocrystals, nanogels and nanomicelles has shown enhanced ocular bioavailability by minimizing the precorneal loss, increasing the corneal residence time, improving the corneal penetration and providing controlled or prolonged drug delivery to the disease site [10]
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