Designing of a pH-Triggered Carbopol®/HPMC In Situ Gel for Ocular Delivery of Dorzolamide HCl: In Vitro, In Vivo, and Ex Vivo Evaluation

2019 ◽  
Vol 20 (5) ◽  
Author(s):  
Maryam Kouchak ◽  
Mina Mahmoodzadeh ◽  
Fereydoun Farrahi
Keyword(s):  
Ex Vivo ◽  
2019 ◽  
Vol 46 (1) ◽  
pp. 50-56 ◽  
Author(s):  
Pooja Jain ◽  
Chandra Prakash Jaiswal ◽  
Mohd. Aamir Mirza ◽  
Md. Khalid Anwer ◽  
Zeenat Iqbal
Keyword(s):  
Ex Vivo ◽  

2020 ◽  
Vol 55 ◽  
pp. 101373 ◽  
Author(s):  
Mori Dhaval ◽  
Jatin Devani ◽  
Ramesh Parmar ◽  
M.M. Soniwala ◽  
Jayant Chavda
Keyword(s):  
Ex Vivo ◽  

2019 ◽  
Vol 554 ◽  
pp. 264-275 ◽  
Author(s):  
Ketan M. Ranch ◽  
Furqan A. Maulvi ◽  
Mausam J. Naik ◽  
Akshay R. Koli ◽  
Rajesh K. Parikh ◽  
...  

2018 ◽  
Vol 68 (16) ◽  
pp. 965-977 ◽  
Author(s):  
Hossein Kamali ◽  
Elham Khodaverdi ◽  
Farzin Hadizadeh ◽  
Seyed Ahmad Mohajeri ◽  
Younes Kamali ◽  
...  

Drug Delivery ◽  
2021 ◽  
Vol 28 (1) ◽  
pp. 1836-1848
Author(s):  
Khaled M. Hosny ◽  
Waleed Y. Rizg ◽  
Hala M. Alkhalidi ◽  
Walaa A. Abualsunun ◽  
Rana B. Bakhaidar ◽  
...  

2020 ◽  
Vol 9 (4) ◽  
pp. 578-587
Author(s):  
Sima Talaei ◽  
Mohammad Mehdi Mahboobian ◽  
Mojdeh Mohammadi

Abstract Glaucoma is an ocular disease i.e. more common in older adults with elevated intraocular pressure and a serious threat to vision if it is not controlled. Due to the limitations regarding the conventional form of brinzolamide (Azopt®), two optimum formulations of in situ gel nanoemulsion were developed. To ensure the safety and efficacy of developed formulations for ocular drug delivery, the current study was designed. MTT assay was carried out on the human retinal pigmentation epithelial cells. To investigate the irritation potential of the chosen formulations, hen’s egg test-chorioallantoic membrane as a borderline test between in vivo and in vitro methods has been done. The modified Draize method was utilized to evaluate eye tolerance against the selected formulations. Intraocular pressure was measured by applying the prepared formulations to the eyes of normotensive albino rabbits in order to assess the therapeutic efficacy. Based on MTT test, cell viability for NE-2 at 0.1% and NE-1 at 0.1 and 0.5% concentrations was acceptable. The results of the hen’s egg test-chorioallantoic membrane test indicated no sign of vessel injury on the chorioallantoic membrane surface for both formulations. Also, during 24 h, both formulations were well-tolerated by rabbit eyes. The pharmacodynamics effects of formulations had no difference or were even higher than that of suspension in case of adding lower concentration (0.5%) of brinzolamide to the formulations. With regard to the results of the mentioned methods, our advanced formulations were effective, safe, and well-tolerated, thus can be introduced as an appropriate vehicle for ocular delivery of brinzolamide.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 465 ◽  
Author(s):  
Eman A. Mazyed ◽  
Abdelaziz E. Abdelaziz

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 (Q8h) 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 Q8h 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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