Full Factorial Design, Optimization, In vitro and Ex vivo Studies of Ocular Timolol-Loaded Microsponges
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ORIGINAL ARTICLE
Full Factorial Design, Optimization, In vitro and Ex vivo Studies of Ocular Timolol-Loaded Microsponges Radwa M. A. Abd-Elal 1 & Ghada H. Elosaily 1,2
&
Shadeed Gad 3 & El-Sayed Khafagy 3,4 & Yasser Mostafa 5
# Springer Science+Business Media, LLC, part of Springer Nature 2019
Abstract Purpose Timolol maleate (TMM) is a hydrophilic model drug. The aim of this study was to formulate TMM-loaded microsponges to sustain TMM release and improve its corneal permeability compared with TMM-aqueous solution. Methods The modified quasi-emulsion solvent diffusion technique (water/oil/oil) was used to prepare TMM-loaded microsponges. The impact of the polymer type (X1) and drug:polymer ratio (X2) were studied and optimized, using full factorial design. The production yield (PY) %, entrapment efficiency (EE) %, particles size (PS), and TMM released % after 6 h were selected as dependent variables. Depended on the desirability value by using the Design-Expert® software version 11, the optimized formulation was selected and subjected to further studies, such as scanning electron microscopy (SEM), porosity determination, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), ex vivo permeation study, and corneal hydration level. Results The optimized formulation composed of TMM: EC within the proportion 1:9 exhibited PY of 96.55 ± 4.01%; EE of 72.00 ± 6.08%; PS (d90) of 6283.33 ± 145.71 nm and released 42.12 ± 3.93% of TMM after 6 h. Particles appeared porous with spherical shape. Thermal analysis proved that the drug has been homogeneously dispersed in its amorphous state. The optimized formulation showed higher corneal permeability about 1.45-fold higher than TMM-aqueous solution in a period of 6 h. Conclusions The modified quasi-emulsion diffusion technique (water/oil/oil) is suitable for improving EE of hydrophilic drug (TMM) and the optimized TMM-loaded microsponge was succeeded to retard the release of TMM and improve its corneal permeability. Keywords Microsponges . Water/oil/oil . Timolol . Optimization . In vitro release . Ex vivo permeation study
Introduction Electronic supplementary material The online version of this article (https://doi.org/10.1007/s12247-019-09418-z) contains supplementary material, which is available to authorized users. * Ghada H. Elosaily [email protected] 1
Department of Pharmaceutics, Faculty of Pharmacy, Modern University for Technology & Information, Maadi, Cairo, Egypt
2
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt
3
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt
4
Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 1142, Saudi Arabia
5
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt
Microsponges are a polymeric conveyance structure which is composed of porous microspheres, having a particle size (PS)
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