Gellan gum based sol-to-gel transforming system of natamycin transfersomes improves topical ocular delivery

Karthik Yadav Janga, Akshaya Tatke, Narendar Dudhipala, Sai Prachetan Balguri, Mohamed Moustafa Ibrahim, Doaa Nabih Maria, Monica Jablonski, Soumyajit Majumdar

Research output: Contribution to journalArticle

Abstract

Short precorneal residence time and poor transocular membrane permeability are the major challenges associated with topical ocular drug delivery. In the present research, the efficiency of the electrolyte-triggered sol-to-gel-forming system of natamycin (NT) transfersomes was investigated for enhanced and prolonged ophthalmic delivery. Transfersomes were optimized by varying the molar ratios of phospholipid, sorbitan monostearate (Span) and tocopheryl polyethylene glycol succinate (TPGS). NT transfersome formulations (FNs) prepared with a 1:1 molar ratio of phospholipid-to-Span and low levels of TPGS showed optimal morphometric properties, and were thus selected to fabricate the in situ gelling system. Gellan gum-based (0.3% w/v) FN-loaded formulations (FNGs) immediately formed an in situ gel in the simulated tear fluid, with considerable viscoelastic characteristics. In vitro cytotoxicity in corneal epithelial cells and corneal histology studies demonstrated the ocular safety and cytocom-patibility of these optimized formulations. Transcorneal permeability of NT from these formulations was significantly higher than in the control suspension. Moreover, the ocular disposition studies of NT, from the FNs and FNGs, in New Zealand male albino rabbits demonstrated the superiority of the electrolyte-sensitive FNGs in terms of NT delivery to the ocular tissues.

Original languageEnglish (US)
Pages (from-to)814-822
Number of pages9
JournalJournal of Pharmacology and Experimental Therapeutics
Volume370
Issue number3
DOIs
StatePublished - Jan 1 2019

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Natamycin
Polymethyl Methacrylate
Gels
Electrolytes
Permeability
Phospholipids
Tears
New Zealand
Suspensions
Histology
Epithelial Cells
gellan gum
Rabbits
Safety
Membranes
Research
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Pharmacology

Cite this

Gellan gum based sol-to-gel transforming system of natamycin transfersomes improves topical ocular delivery. / Janga, Karthik Yadav; Tatke, Akshaya; Dudhipala, Narendar; Balguri, Sai Prachetan; Ibrahim, Mohamed Moustafa; Maria, Doaa Nabih; Jablonski, Monica; Majumdar, Soumyajit.

In: Journal of Pharmacology and Experimental Therapeutics, Vol. 370, No. 3, 01.01.2019, p. 814-822.

Research output: Contribution to journalArticle

Janga, Karthik Yadav ; Tatke, Akshaya ; Dudhipala, Narendar ; Balguri, Sai Prachetan ; Ibrahim, Mohamed Moustafa ; Maria, Doaa Nabih ; Jablonski, Monica ; Majumdar, Soumyajit. / Gellan gum based sol-to-gel transforming system of natamycin transfersomes improves topical ocular delivery. In: Journal of Pharmacology and Experimental Therapeutics. 2019 ; Vol. 370, No. 3. pp. 814-822.
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