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. 2021 Feb 5;13(2):221.
doi: 10.3390/pharmaceutics13020221.

Formulation and Characterization of Acetazolamide/Carvedilol Niosomal Gel for Glaucoma Treatment: In Vitro, and In Vivo Study

Rehab Abdelmonem  1 , Sammar F Elhabal  2 , Nevine S Abdelmalak  3   4 , Mohamed A El-Nabarawi  3 , Mahmoud H Teaima  3
Affiliations

Formulation and Characterization of Acetazolamide/Carvedilol Niosomal Gel for Glaucoma Treatment: In Vitro, and In Vivo Study

Rehab Abdelmonem et al. Pharmaceutics. .

Abstract

Acetazolamide (ACZ) is a diuretic used in glaucoma treatment; it has many side effects. Carvedilol (CAR) is a non-cardioselective beta-blocker used in the treatment of elevated intraocular pressure; it is subjected to the first-pass metabolism and causes fluids accumulation leading to edema. This study focuses on overcoming previous side effects by using a topical formula of a combination of the two previous drugs. Sixty formulations of niosomes containing Span 20, Span 60, Tween 20, and Tween 60 with two different ratios were prepared and characterized. Formulation with the lowest particle size (416.30 ± 0.23), the highest zeta potential (72.04 ± 0.43 mv), and the highest apparent coefficient of corneal permeability (0.02 ± 0.29 cm/h) were selected. The selected formula was incorporated into the gel using factorial design 23. Niosomes (acetazolamide/carvedilol) consisting of Span 60 and cholesterol in the molar ratio (7:6), HMPC, and carbopol with two different ratios were used. The selected formula was subjected to an in vivo study of intraocular pressure in ocular hypertensive rabbits for 60 h. The sustained gel formula of the combination decreased (IOP) to normal after 1 h and sustained efficacy for 4 days. Histological analysis of rabbit eyeballs treated with the selected formula showed improvement in glaucomatous eye retinal atrophy.

Keywords: acetazolamide; carvedilol; gel; glaucoma; intraocular pressure; niosomes.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
FTIR images of combination acetazolamide and carvedilol optimized transfersomal formula.
Figure 2
Figure 2
Differential scanning calorimetry (DSC) thermograms of pure ACZ, Span 60, cholesterol, CAR, and drug-loaded combination niosomal formulation.
Figure 3
Figure 3
Transmission electron microscope (TEM) pictures of combination niosomes and niosomal gel (A) A+C-S60-C6 & (B) H-LV A+C-S60-C6.
Figure 4
Figure 4
Mean IOP of hypertensive rabbits for first 48 h with a different administration in comparison with physiological minimum IOP for rabbit (IOP lower limit) and physiological maximum (IOP upper limit).
Figure 5
Figure 5
Photomicrographs of the cornea (H&E). Where (a) normal group showed histologically normal cornea, (b) glaucoma group showed marked corneal stromal edema, (c) Group 1 and (d) Group 2 showed mild edema, (e) Group 3 showed normal cornea, (f) Group 4 showed moderate edema, and (g) Group 5 showed normal cornea.
See this image and copyright information in PMC

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