Gellan Gum BasedSol-to-GelTransforming System of Natamycin Transfersomes Improves Topical Ocular Delivery

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 cytocompatibility 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.

Ciprofloxacin Loaded Nanostructured Lipid Carriers Incorporated into In-Situ Gels to Improve Management of Bacterial Endophthalmitis

“…The viscosity of the CIP-NLC-IG (0.2% w/v) was found to be 7.9 ± 0.2 cP and 55 ± 2.7 cP without and with STF, respectively. After the addition of STF, there was an increase in the viscosity due to the cross-linking of the polymer chain by the mono or divalent cations present in the STF [25,29,37]. GT and GRT are the critical properties, which determine the efficiency of the ocular IG systems [25].…”

“…However, static and dynamic barriers, reflex blinking, tear turnover and nasolachrymal drainage are anatomical and physiological barriers that constrain ocular delivery [22]. Novel drug delivery and nanotechnology-based drug delivery systems to improve penetration into the anterior and posterior segments of the eye have been extensively investigated [19,[23][24][25][26][27][28][29].…”

“…This leads to prolonged ocular surface residence which may enhance the ocular bioavailability of drugs and therefore lead to better therapeutic outcomes [29,[35][36][37]. Moreover, reduction of the pre-corneal elimination of the gel minimizes absorption into systemic circulation during ocular administration and thus may reduce side effects [25].…”

Neuroprotective Effect of Ropinirole Lipid Nanoparticles Enriched Hydrogel for Parkinson’s Disease: In Vitro, Ex Vivo, Pharmacokinetic and Pharmacodynamic Evaluation

“…Various approaches have been used to alter skin to enhance the transport of therapeutic agents, such as using penetration enhancers [12], iontophoresis [13], microneedles [14] and lipid vesicle carriers [15]. The vesicular carrier systems used for topical application of bioactive include lipid nanoparticles such as solid lipid nanoparticles (SLNs) [16], and nanostructured lipid carriers (NLCs) [17], transfersomes [18], liposomes, niosomes and ethosomes [15,19] have been investigated.…”

Enhanced Corneal Penetration of a Poorly Permeable Drug Using Bioadhesive Multiple Microemulsion Technology

“…The potential cell toxicity of our ME was evaluated in vitro using methyl thiazolyl tetrazolium (MTT) assay according to our previously published protocols [22,36,37]. Because our formulations are intended to be used topically in the eye, a human corneal limbal epithelial cell line (HCLE) was used to evaluate the effect that our ME has on epithelial cell viability [26].…”