Abstract
Objective: The objective of the present work was to improve the retention and penetration of ciprofloxacin (CF) ion pair entrapped within submicron emulsion (SE) in goat eyes and characterize the SE for improvement of ocular activity. The developed delivery system resulted with prolonged drug release as compared to the conventional dosage form.
 Methods: SE prepared by high-energy emulsification and sonication to obtain uniform globule size. Ion-pair complex is prepared by precipitation method.
 Results: Average internal droplets size of the optimized formulation was 0.300 μm, pH of the optimized formulation was 6.4±0.7 (average of three determinations) and viscosity 3.2±0.3 cP suitable for ocular use. Entrapment was 92.12%. In vitro drug release pattern in dialysis membrane showed sustain release of CF, a cumulative percent release of CF was found 77% in 10 h. Scanning electron microscopy showed spherical shape and size within 1 μm. In vitro release in goat eyes was found 35.86 % for optimized formulation compared to market, 26.83% in 60 min.
 Conclusion: Developed optimized formulation can be a good candidate for ocular drug delivery in severe ocular infections where frequent dosing required such as endophthalmitis, corneal ulcer, and penetrating trauma.
Highlights
When a traditional eye drop instilled in the ocular area, there are many factors such as dilution of the drug by overflow, tear renewal, nasolacrimal drainage, conjunctival absorption, and enzyme metabolism affect the drug penetration to the eyes, leading to poor ocular bioavailability [1]
Advantages of using the controlled ocular delivery system are as follows: (a) Overcoming the side effects of pulsed and frequent dosing of the traditional delivery systems, (b) providing sustained and controlled drug delivery, and (c) increases the ocular bioavailability of drug by increasing precorneal cornel contact time; this can be achieved by effective adherence to the corneal surface [5]
In the current work, drug identification is done by UV and high-performance liquid chromatography (HPLC) method
Summary
When a traditional eye drop instilled in the ocular area, there are many factors such as dilution of the drug by overflow, tear renewal, nasolacrimal drainage, conjunctival absorption, and enzyme metabolism affect the drug penetration to the eyes, leading to poor ocular bioavailability [1]. Frequent instillation of drug is required to achieve desired therapeutic effect which results with systemic absorption of drug and may result in undesirable effects [3]. The non-corneal route involves absorption across the sclera and conjunctiva, which restrains the entry of drugs into the aqueous humor. Advantages of using the controlled ocular delivery system are as follows: (a) Overcoming the side effects of pulsed and frequent dosing of the traditional delivery systems, (b) providing sustained and controlled drug delivery, and (c) increases the ocular bioavailability of drug by increasing precorneal cornel contact time; this can be achieved by effective adherence to the corneal surface [5]
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