Adv Pharm Bull. 2020;10(3): 389-398.
doi: 10.34172/apb.2020.047
  Abstract View: 60
  PDF Download: 73

Research Article

Self-nanoemulsifying System Optimization for Higher Terconazole Solubilization and Non-Irritant Ocular Administration

Carol Yousry 1 * ORCID logo, Pakinam Mohsen Zikry 2, Emad Basalious Basalious 1, Omaima Naem El-Gazayerly 1

1 Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini, Cairo 11562, Egypt.
2 Department of Pharmaceutics, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Egypt.


Purpose: Eye drops’ formulations of poorly water-soluble drugs, offer the advantage of crossingthe lipophilic cornea, but their limited aqueous solubility may lead to low ocular bioavailabilitylimiting their therapeutic uses. Terconazole (TZ) is an antifungal drug with low aqueous solubility,restricting its application in ocular fungal infection. Thus, the aim of the work in this study is toenhance TZ solubilization, permitting better ocular permeation and higher bioavailability. Toachieve this goal, different self-nanoemulsifying systems (SNESs) were prepared using differentoils, surfactants and co-surfactants.Methods: Ternary phase diagrams were constructed to identify self nano-emulsification regionsfor each oil system examined; either Labrafil® M2125CS or Capryol™ 90. TZ saturated solubilityin the different formulated systems were measured and systems showing highest potential forTZ solubilization were selected. The optimized systems were chosen based on their globulesize, polydispersity index, self-emulsification characteristics. Finally, TZ release as well as theirritation effect via Hen’s Egg test-chorioallantoic membrane (HET-CAM test) of the optimizedsystem was observed in vitro.Results: The optimized system was formulated using 20% w/w Labrafil® M2125 CS, 50% w/wTween® 80 and 30% w/w Transcutol® HP. Oil globules showed size range of 15.13 nm andself-emulsification time of 12.80 seconds. The system released 100% of the drug within half anhour compared to 2 hours in case of TZ-suspension. Finally, HET-CAM test showed non-irritatingresponse and normal vascularization of the chorioallantoic membrane.Conclusion: The formulated SNES could be a promising approach to enhance ocular efficacyof TZ.
Keywords: Chorioallantoic membrane, High pressure liquid chromatography, Oils, Surface-active agent, Terconazole, Transmission electron microscopy
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Submitted: 28 Jul 2019
Revision: 30 Nov 2019
Accepted: 02 Dec 2019
ePublished: 11 May 2020
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