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Effect of Formulation Variables and Gamma Sterilization on Transcorneal Permeation and Stability of Proniosomal Gels as Ocular Platforms for Antiglaucomal Drug

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Abstract

This study aims to evaluate the effect of different formulation variables (surfactant type and HLB value) adopting full factorial design (51. 21) using coacervation phase technique on in vitro characterization of dorzolamide hydrochloride (DZ)-loaded proniosomal gels, namely, entrapment efficiency percentage (EE%), vesicle size distribution, polydispersion index (PDI), and in vitro DZ release. The optimum formula F2 with a desirability value of 0.937 composed of 40 mg DZ, 500 mg span 60, 500 mg of L-α-Lethicin, and 55.5 mg cholesterol showing EE% of 84.5 ± 1.5%, PS of 189.5 ± 35.76 nm with PDI 0.8 ± 0.28 and 58.51% ± 1.00 of DZ released after 8 h was further evaluated using differential scanning calorimetry (DSC) and transmission electron microscopy (TEM). The effect of gamma sterilization on transcorneal permeation and stability of DZ from the selected formulation (F2) revealed that F2 was significantly tolerable, stable, and competent to corneal permeation confirmed by histological examination, confocal laser microscopy, and intraocular pressure (IOP) measurement. Significant corneal bioavailability was attained from formula F2 (370.6 mg. h/m) compared to the market product Trusopt® eye drops (92.59 mg. h/ml) following IOP measurement, thereby proniosomal gels could be considered as tolerable and competent ocular platforms for improving the transcorneal permeation of DZ.

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Authors and Affiliations

  1. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini, Cairo, 11562, Egypt

    Sinar Sayed, Maha M. Amin & Omnia M. Khowessah

  2. Quality Assurance Department, Sigma Tec. Pharmaceutical Company, Giza Governorate, Egypt

    Mostafa Abdelmoteleb

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  1. Sinar Sayed
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  2. Mostafa Abdelmoteleb
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Correspondence to Sinar Sayed.

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The experimental protocol was confirmed by Research Ethics Committee, Faculty of Pharmacy, Cairo University (REC-FOPCU) with a number of PI 2134. This study was approved by “Animal Care and Use Committee, Faculty of Pharmacy, Cairo University” (PI 2134).

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Sayed, S., Abdelmoteleb, M., Amin, M.M. et al. Effect of Formulation Variables and Gamma Sterilization on Transcorneal Permeation and Stability of Proniosomal Gels as Ocular Platforms for Antiglaucomal Drug. AAPS PharmSciTech 21, 87 (2020). https://doi.org/10.1208/s12249-020-1626-2

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