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

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

This study aims to evaluate the effect of different formulation variables (surfactant type and HLB value) adopting full factorial design (5 1 . 2 1 ) using coacervation phase technique on in vitro characterization of dorzolamide hydrochloride (DZ)-loaded proniosomal gels, namely, entrapment efficien...

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Bibliographic Details
Published in:AAPS PharmSciTech Vol. 21; no. 3; p. 87
Main Authors: Sayed, Sinar, Abdelmoteleb, Mostafa, Amin, Maha M., Khowessah, Omnia M.
Format: Journal Article
Language:English
Published: Cham Springer International Publishing 03-02-2020
Subjects:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Pharmacology/Toxicology
Pharmacy
Research Article
transcorneal permeation
intraocular pressure
gamma sterilization
corneal bioavailability
proniosomal gel
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Summary:This study aims to evaluate the effect of different formulation variables (surfactant type and HLB value) adopting full factorial design (5 1 . 2 1 ) 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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ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-020-1626-2