In situ gel of triamcinolone acetonide-loaded solid lipid nanoparticles for improved topical ocular delivery

Tear kinetics and ocular disposition studies

Akshaya Tatke, Narendar Dudhipala, Karthik Yadav Janga, Sai Prachetan Balguri, Bharathi Avula, Monica Jablonski, Soumyajit Majumdar

Research output: Contribution to journalArticle

1 Citation (Scopus)

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.

Original languageEnglish (US)
Article number33
JournalNanomaterials
Volume9
Issue number1
DOIs
StatePublished - Jan 1 2019

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Triamcinolone Acetonide
Lipids
Gels
Tissue
Nanoparticles
Kinetics
Zeta potential
Drug delivery
Assays
Surface active agents
Particle size
Poloxamer

All Science Journal Classification (ASJC) codes

  • Chemical Engineering(all)
  • Materials Science(all)

Cite this

In situ gel of triamcinolone acetonide-loaded solid lipid nanoparticles for improved topical ocular delivery : Tear kinetics and ocular disposition studies. / Tatke, Akshaya; Dudhipala, Narendar; Janga, Karthik Yadav; Balguri, Sai Prachetan; Avula, Bharathi; Jablonski, Monica; Majumdar, Soumyajit.

In: Nanomaterials, Vol. 9, No. 1, 33, 01.01.2019.

Research output: Contribution to journalArticle

Tatke, Akshaya ; Dudhipala, Narendar ; Janga, Karthik Yadav ; Balguri, Sai Prachetan ; Avula, Bharathi ; Jablonski, Monica ; Majumdar, Soumyajit. / In situ gel of triamcinolone acetonide-loaded solid lipid nanoparticles for improved topical ocular delivery : Tear kinetics and ocular disposition studies. In: Nanomaterials. 2019 ; Vol. 9, No. 1.
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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{\circledR} 888ATO as solid lipids and Tween{\circledR}80 and Pluronic{\circledR} 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.",
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AU - Tatke, Akshaya

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AU - Janga, Karthik Yadav

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AU - Avula, Bharathi

AU - Jablonski, Monica

AU - Majumdar, Soumyajit

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