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Abstract

Introduction: Poor bioavailability of drugs from ocular dosage forms is mainly due to the tear production, nonproductive absorption, transient residence time, and impermeability of corneal epithelium. The aim of the present study was to design, characterize of a novel nanoemulsion (NE) system as an ocular delivery system for celecoxib (CXB) and to evaluate its physicochemical characteristics and rabbit corneal permeability to enhance the penetration of the drug. Methods: CXB NEs were prepared by testing its solubility in oils, surfactants, and cosurfactants. Utilizing pseudoternary phase diagram, the optimum ratios were chosen and full factorial design was used with 3 variables at 2 levels for preparing eight formulations. The prepared NEs were evaluated regarding their viscosity, pH, particle size, differential scanning calorimetry thermograms, stability, in vitro drug release, and corneal rabbit permeability. Results and Discussion: The results showed that the mean droplet size range of NE formulations was in the range of 6.96-26.65 nm and pH was 6.5-6.9, respectively. Viscosity range was 118-245 cps. Drug release profile showed that 82.6% of the drug released in the 24 h of the experiment. The maximum and minimum drug permeated percentage through rabbit cornea was observed in NE component (NEC)-5 (15.73%) and NEC-1 (6.1%), respectively. All NE formulations with different compositions and properties significantly increased partitioning, flux, and permeability coefficient from rabbit cornea. Dapp and Papp parameters in NEC-3 and NEC-5 formulation were 0.0233 cm 2 h

Nanoemulsion and Solid Nanoemulsion for Improving Oral Delivery of a Breast Cancer Drug: Formulation, Evaluation, and a Comparison Study

“…For this purpose, the surfactant molecules were added, which may make adsorption at the oil–water interface and screening the thermodynamically unfavorable molecular interactions between the oil and water phases. Moreover, tween 80 may suggest decreasing the interfacial tension and the decrease in oil droplet disruption ( Wadhwa et al, 2012 , Gupta et al, 2013 , Sullivan et al, 2014 , Yuan et al, 2014 , Moghimipour et al, 2017 , Charoo et al, 2019 , Zhu et al, 2019 ). This study data was illustrated in Fig.…”

Ocular Delivery of Quercetin Using Microemulsion System: Design, Characterization, and Ex-vivo Transcorneal Permeation

“…They range from 10-100 nm in size and exhibit minimal surface tension. The properties of MEs are ideal for helping drugs pass through the cornea, thus making them advantageous carriers during ocular drug delivery (17)(18)(19). Moreover, ME carriers contain surfactants and co-surfactants, which also assist in corneal drug penetration.…”