Optimization of Brinzolamide Loaded Microemulsion using Formulation by Design Approach: Characterization and In-vitro Evaluation

Author(s): Riyaz Gohil, Asha Patel*, Tosha Pandya, Abhay Dharamsi

Journal Name: Current Drug Therapy

Volume 15 , Issue 1 , 2020

Become EABM
Become Reviewer
Call for Editor

Graphical Abstract:


Background: The clinical application of Brinzolamide, a drug used in the treatment of glaucoma is limited due its poor aqueous solubility. Microemulsion based ocular delivery can be an effective means to improve its solubility and in turn the bioavailability.

Objective: The main objective of the present work was optimization and characterization of Brinzolamide loaded microemulsion for the treatment of glaucoma.

Method: The solubility of Brinzolamide in various oils and surfactants was checked in order to identify components of microemulsion. Pseudo-ternary phase diagram using Prosim software was plotted to identify microemulsion existence area. D-optimal mixture design was used for optimization of microemulsion. The optimized formulation consisted of Isopropyl myristate, Tween-80 and Transcutol-P as surfactant and co-surfactant respectively, and water. The chosen critical responses were droplet size, zeta potential, nepheloturbidimetric unit, and viscosity.

Results: The selected optimal composition shows favorable features, such as droplet size (41.69 nm), Zeta potential (-9.496 mV), Viscosity (170.8 cps), Transparency (1.483 NTU) and pH (7.646) that are suitable for ocular delivery. Moreover, a prolonged drug release (78.08 % within 7 hour) was found in in-vitro experiments. By and large the formulation was found to be safe and nonirritant as proven by the ocular irritation study.

Conclusion: Our study illustrated potential of Brinzolamide loaded microemulsion for ocular delivery for the treatment of glaucoma.

Keywords: Brinzolamide, microemulsion, glaucoma, D-optimal mixture design, viscosity, transparency.

Quigley HA, Broman AT. The number of people with glaucoma worldwide in 2010 and 2020. Br J Ophthalmol 2006; 90(3): 262-7.
Weinreb RN, Aung T, Medeiros FA. The pathophysiology and treatment of glaucoma, a review. JAMA 2014; 311(18): 1901-11.
Brinzolamide drug profile’ [Internet]. Drugs.com; 2017 [Cited 2017 April 25]. Available from: http://www.drugs.com
Profile of Brinzolamide’ [Internet]. Pubchem; 2017 [Cited 2017 April 25]. Available from: http//www.pubchem.com
AZOPT brinzolamide ophthalmic suspension’ [Internet]. Rxlist; 2017 [cited 2017 April 25]. Available from: http://www.rxlist.com
Patel A, Cholkar K, Agrahari V, Mitra AK. Ocular drug delivery systems: An overview. World J Pharmacol 2013; 2(2): 47-64.
Singh PK, Iqubal MK, Shukla VK, Shuaib M. Microemulsions: Current trends in novel drug delivery systems. J Pharmaceutical Chem Biol Sciences 2014; 1(1): 39-51.
Bhattacharya R, Mukhopadhyay S, Kothiyal P. Review on microemulsion- as a potential novel drug delivery system. World J Pharm Pharm Sci 2016; 5(6): 700-29.
Moghimipour E, Salimi A, Karami M, Isazadeh S. Preparation and characterization of dexamethasone microemulsion based on pseudoternary phase diagram. J Nat Pharmaceutical Products 2013; 8(3): 105-12.
Madhav S, Gupta D. A review on microemulsion based system. Int J Pharm Sci Res 2011; 2(8): 1888-99.
Kumar N. Shishu. D-optimal experimental approach for designing topical microemulsion of itraconazole: Characterization and evaluation of antifungal efficacy against a standardized Tinea pedisinfection model in Wistar rats. Eur J Pharm Sci 2014; 67: 97-112.
Wu W, Li J, Wu L, et al. Ophthalmic delivery of brinzolamide by liquid crystalline nanoparticles: In vitro and in vivo evaluation. AAPS PharmSciTech 2013; 14(3): 1063-71.
Ince I, Karasulu E, Ates H, Yavasoglu A, Kirilmaz L. A novel pilocarpine microemulsion as an ocular delivery system: In vitro and in vivo studies. J Clin Exp Ophthalmol 2015; 6: 408.
Habib F, Mahdy M, Maher S. Microemulsions for ocular delivery: Evaluation and characterization. J Drug Deliv Sci Technol 2011; 21(6): 485-9.
Moghimipour E, Salimi A, Rad AS. A microemulsion system for controlled corneal delivery of timolol. Int Res J Pharmaceut Appl Sci 2013; 3(4): 32-9.
Sutar R, Masareddy R, Nagesh C, et al. Formulation and evaluation of Clarithromycin poorly soluble as microemulsion. Int Res J Pharmacy 2011; 2(11): 153-8.
Rakesh K, Sinha V. Preparation and optimization of voriconazole microemulsion forocular delivery. Colloids Surf B Biointerfaces 2014; 117: 82-8.
Gallarate M, Chirio D, Bussano R, et al. Development of O/W nanoemulsions for ophthalmic administration of timolol. Int J Pharm 2013; 440: 126-34.
Mahboobian MM, Foroutan SM, Aboofazeli R. Brinzolamide-loaded nanoemulsions: In vitro release evaluation. Indian J Pharm Sci 2016; 12(3): 75-93.
Hegde R, Bhattacharya SS, Verma A, Ghosh A. Physicochemical and pharmacological investigation of water/oil microemulsion of non-selective beta blocker for treatment of glaucoma. Curr Eye Res 2014; 39(2): 155-63.
Morsi N, Mohamed M, Refati H, Sorogy H. Nanoemulsion as a novel ophthalmic delivery system for acetazolamide. Int J Pharm Pharm Sci 2014; 6(11): 227-36.
Chaemin L, Da-won K, Taehoon S, et al. Preparation and characterization of a lutein loading nanoemulsion system for ophthalmic eye drops. J Drug Deliv Sci Technol 2016; 36: 168-74.
Patel A, Gohel M, Soni T, Patel N. Development of plant extract loaded Nanoemulsion for the treatment of inflammatory disorder. Curr Res Drug Discovery 2014; 2: 29-39.
Shafiq-un-Nabi S, Shakeel F, Talegaonkar S, et al. Formulation development and optimization using nanoemulsion technique: A technical note. AAPS PharmSciTech 2007; 8(2): E12-7.
Hegde RR, Verma A, Ghosh A. Microemulsion: New insights into the ocular drug delivery. ISRN Pharm 2013; Article ID 826798.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2020
Published on: 14 January, 2020
Page: [37 - 52]
Pages: 16
DOI: 10.2174/1574885514666190104115802
Price: $65

Article Metrics

PDF: 24