Development of Triamcinolone Acetonide-Loaded Microemulsion as a Prospective Ophthalmic Delivery System for Treatment of Uveitis: In Vitro and In Vivo Evaluation

Treatment of uveitis (i.e., inflammation of the uvea) is challenging due to lack of convenient ophthalmic dosage forms. This work is aimed to determine the efficiency of triamcinolone acetonide (TA)-loaded microemulsion as an ophthalmic delivery system for the treatment of uveitis. Water titration method was used to construct different pseudo-ternary phase diagrams. Twelve microemulsion formulations were prepared using oleic acid, Cremophor EL, and propylene glycol. Among all tested formulations, Formulation F3, composed of oil: surfactant-co-surfactant (1:1): water (15:35:50% w/w, respectively), was found to be stable and showed acceptable pH, viscosity, conductivity, droplet size (211 ± 1.4 nm), and zeta potential (−25 ± 1.7 mV) and almost complete in vitro drug release within 24 h. The in vivo performance of the optimized formulation was evaluated in experimentally uveitis-induced rabbit model and compared with a commercial TA suspension (i.e., Kenacort®-A) either topically or by subconjunctival injection. Ocular inflammation was evaluated by clinical examination, white blood cell count, protein content measurement, and histopathological examination. The developed TA-loaded microemulsion showed superior therapeutic efficiency in the treatment of uveitis with high patient compliance compared to commercial suspension. Hence, it could be considered as a potential ocular treatment option in controlling of uveitis.

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Development of a naringenin microemulsion as a prospective ophthalmic delivery system for the treatment of corneal neovascularization: in vitro and in vivo evaluation

Drug Delivery ◽

10.1080/10717544.2021.2021323 ◽

2021 ◽

Vol 29 (1) ◽

pp. 111-127

Author(s):

Yu Ma ◽

Jingjing Yang ◽

Yali Zhang ◽

Chunyan Zheng ◽

Zhen Liang ◽

...

Keyword(s):

Delivery System ◽

Corneal Neovascularization ◽

In Vivo Evaluation ◽

Ophthalmic Delivery

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Liquid Crystalline Nanoparticles as an Ophthalmic Delivery System for Tetrandrine: Development, Characterization, and In Vitro and In Vivo Evaluation

Nanoscale Research Letters ◽

10.1186/s11671-016-1471-0 ◽

2016 ◽

Vol 11 (1) ◽

Cited By ~ 21

Author(s):

Rui Liu ◽

Shuangshuang Wang ◽

Shiming Fang ◽

Jialu Wang ◽

Jingjing Chen ◽

...

Keyword(s):

Delivery System ◽

Liquid Crystalline ◽

In Vivo Evaluation ◽

Ophthalmic Delivery ◽

Liquid Crystalline Nanoparticles

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Composite carbohydrate interpenetrating polyelectrolyte nano-complexes (IPNC) as a controlled oral delivery system of citalopram HCl for pediatric use: in-vitro/in-vivo evaluation and histopathological examination

Drug Delivery and Translational Research ◽

10.1007/s13346-018-0506-8 ◽

2018 ◽

Vol 8 (3) ◽

pp. 657-669 ◽

Cited By ~ 3

Author(s):

Rabab Kamel ◽

Haidy Abbas ◽

Mona El-Naa

Keyword(s):

Delivery System ◽

Oral Delivery ◽

Histopathological Examination ◽

In Vivo Evaluation ◽

Oral Delivery System ◽

Pediatric Use

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A Novel Intravaginal Delivery System for Itraconazole: In Vitro and In Vivo Evaluation

Current Drug Delivery ◽

10.2174/156720109787846289 ◽

2009 ◽

Vol 6 (2) ◽

pp. 151-158 ◽

Cited By ~ 2

Author(s):

N. Dobaria ◽

R. Mashru ◽

A. Badhan ◽

A. Thakkar

Keyword(s):

Delivery System ◽

In Vivo Evaluation ◽

Intravaginal Delivery

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Melt-Cast Films Significantly Enhance Triamcinolone Acetonide Delivery to the Deeper Ocular Tissues

Pharmaceutics ◽

10.3390/pharmaceutics11040158 ◽

2019 ◽

Vol 11 (4) ◽

pp. 158

Author(s):

Akshaya Tatke ◽

Narendar Dudhipala ◽

Karthik Janga ◽

Bhavik Soneta ◽

Bharathi Avula ◽

...

Keyword(s):

Triamcinolone Acetonide ◽

Polymer Matrix ◽

Rabbit Model ◽

In Vivo Studies ◽

Invasive Technique ◽

Content Uniformity ◽

Scanning Calorimetry ◽

Ocular Tissues

Delivering an effective drug load to the posterior section of the ocular tissues, while using a non-invasive technique, has always been a challenge. In this regard, the goal of the present study was to develop sustained release triamcinolone acetonide (TA) loaded polymeric matrix films for ocular delivery. The TA-films were prepared in two different polymer matrices, with drug loadings of 10% and 20% w/w, and they were evaluated for ocular distribution in vivo in a conscious rabbit model. A 4% w/v TA suspension (TA-C) was used as a control for in vitro and in vivo studies. The TA-films, prepared with melt-cast technology, used polyethylene oxide (PEO) and Soluplus® as the polymer matrix. The films were evaluated with respect to assay, content uniformity, excipient interaction, and permeability across isolated rabbit sclera. The distribution of TA in the ocular tissues, post topical administration, was determined in New Zealand male albino rabbits as a function of dose, and was compared against TA-C. The assay of the 10% and 20% w/w film was in the range from 70–79% and 92–94% for the Soluplus® and PEO films, respectively, and content uniformity was in the range of 95–103% for both the films. The assay of the TA from Soluplus® films was less compared with the PEO films and showed an interaction with TA, as revealed by Differential Scanning Calorimetry (DSC). Hence, Soluplus® films were not selected for further studies. No interaction was observed between the drug and PEO polymer matrix. The enhancement of trans-scleral flux and permeability of TA was about 1.16 and 1.33-folds, respectively, from the 10% w/w PEO and 3.5 and 2.12-folds, respectively, from the 20% w/w PEO films, as compared with TA-C formulations. The in vivo studies demonstrate that significantly higher TA levels were observed in the anterior and posterior segments of the eye at the end of 6h with the PEO films. Therefore, the PEO based polymeric films were able to deliver TA into the back of the eye efficiently and for prolonged periods.

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