Abstract
Triamcinolone acetonide (TA), an intermediate acting corticosteroid, is used in the treatment of posterior ocular diseases, such as inflammation, posterior uveitis, and diabetic macular edema. The objective of this investigation was to prepare TA-loaded solid lipid nanoparticles (TA-SLNs) and in situ gel (TA-SLN-IG) formulations for delivery into the deeper ocular tissues through the topical route. TA-SLNs were prepared by hot homogenization and ultrasonication method using glyceryl monostearate and Compritol® 888ATO as solid lipids and Tween®80 and Pluronic® F-68 as surfactants. TA-SLNs were optimized and converted to TA-SLN-IG by the inclusion of gellan gum and evaluated for their rheological properties. In vitro transcorneal permeability and in vivo ocular distribution of the TA-SLNs and TA-SLN-IG were studied using isolated rabbit corneas and New Zealand albino rabbits, respectively, and compared with TA suspension, used as control (TA-C). Particle size, PDI, zeta potential, assay, and entrapment efficiency of TA-SLNs were in the range of 200–350 nm, 0.3–0.45, −52.31 to −64.35 mV, 70–98%, and 97–99%, respectively. TA-SLN-IG with 0.3% gellan gum exhibited better rheological properties. The transcorneal permeability of TA-SLN and TA-SLN-IG was 10.2 and 9.3-folds higher compared to TA-C. TA-SLN-IG showed maximum tear concentration at 2 h, indicating an improved pre-corneal residence time, as well as higher concentrations in aqueous humor, vitreous humor and cornea at 6 h, suggesting sustained delivery of the drug into the anterior and posterior segment ocular tissues, when compared to TA-SLN and TA-C. The results, therefore, demonstrate that the lipid based nanoparticulate system combined with the in situ gelling agents can be a promising drug delivery platform for the deeper ocular tissues.
Highlights
triamcinolone acetonide (TA) intravitreal injections namely, Kenalog®, Kenacort®, Tricinolon®, and Flutex®, have gained substantial attention for the treatment of various ocular disorders, like temporal arteritis, uveitis, and inflammation, which are not responsive to other topical corticosteroids[3,4,5].Though this delivery gives a more targeted approach, it is associated with various complications, such as retinal hemorrhage or detachment, ocular hypertension, postoperative infectious, and non-infectious endophthalmitis, which might in turn lead to cataract formation or vision loss [6,7,8,9]
The percent content for all the excipient were below the limit in the inactive ingredients (IIG) database [29]
TA-loaded solid lipid nanoparticles (TA-solid lipid nanoparticles (SLNs)) were prepared using homogenization followed by probe sonication method
Summary
Ocular delivery of steroids has been extensively explored to treat various ophthalmic disorders including inflammation, uveitis, sympathetic ophthalmia, age-related macular. TA intravitreal injections namely, Kenalog® , Kenacort® , Tricinolon® , and Flutex® , have gained substantial attention for the treatment of various ocular disorders, like temporal arteritis, uveitis, and inflammation, which are not responsive to other topical corticosteroids[3,4,5].Though this delivery gives a more targeted approach, it is associated with various complications, such as retinal hemorrhage or detachment, ocular hypertension, postoperative infectious, and non-infectious endophthalmitis, which might in turn lead to cataract formation or vision loss [6,7,8,9]. Amongst different lipid nano carriers, solid lipid nanoparticles (SLNs) have been used for effective drug delivery. SLNs are nano-sized lipid carriers, ranging from 50–1000 nm, having the capability to encapsulate lipophilic molecules inside the lipid matrix [15]
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