article · Pharmaceutics
Acetazolamide is an effective drug used to treat glaucoma, but taking it orally triggers unwanted side effects. To address this issue, researchers developed a gel-based nanocarrier system known as transgelosomes to deliver the medicine directly to the eye. The formulation combined lipid transfersomes with poloxamer gelling agents, optimised using statistical software to evaluate different surfactants and lipid ratios. The selected formulation produced spherical, elastic nanovesicles displaying high drug entrapment efficiency and sustained release. When tested, the transgelosomes demonstrated enhanced corneal permeation compared to the untreated drug and successfully maintained lower intraocular pressure over a full twenty-four hours in vivo. This approach provides a viable route to improve ocular delivery while potentially avoiding the adverse effects linked to conventional oral administration.
Glaucoma requires reliable pressure reduction in the eye, yet standard oral treatments can trigger systemic side effects throughout the body. Developing targeted, topical drug delivery systems that remain active over 24 hours allows patients to receive sustained relief directly at the ocular surface, potentially reducing side effects and improving treatment compliance.
This formulation could enable pharmaceutical manufacturers to develop topical therapies for glaucoma management, targeting clinical ophthalmology providers and patients seeking alternatives to oral medication. Given that testing has reached ex vivo permeation and in vivo animal evaluations, the technology is applied and tested, representing mid-stage pharmaceutical development requiring formal clinical validation before commercial use.
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Acetazolamide (ACZ) is a potent carbonic anhydrase inhibitor that is used for the treatment of glaucoma. Its oral administration causes various undesirable side effects. This study aimed to formulate transgelosomes (TGS) for enhancing the ocular delivery of ACZ. ACZ-loaded transfersomes were formulated by the ethanol injection method, using phosphatidylcholine (PC) and different edge activators, including Tween 80, Span 60, and Cremophor RH 40. The effects of the ratio of lipid to surfactant and type of surfactant on % drug released after 8 h (Q<sub>8h</sub>) and entrapment efficiency (EE%) were investigated by using Design-Expert software. The optimized formula was formulated as TGS, using poloxamers as gelling agents. In vitro and in vivo characterization of ACZ-loaded TGS was performed. According to optimization study, F8 had the highest desirability value and was chosen as the optimized formula for preparing TGS. F8 appeared as spherical elastic nanovesicles with Q<sub>8h</sub> of 93.01 ± 3.76% and EE% of 84.44 ± 2.82. Compared to a free drug, TGS exhibited more prolonged drug release of 71.28 ± 0.46% after 8 h, higher ex vivo permeation of 66.82 ± 1.11% after 8 h and a significant lowering of intraocular pressure (IOP) for 24 h. Therefore, TGS provided a promising technique for improving the corneal delivery of ACZ.
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DOI: 10.3390/pharmaceutics12050465
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