Volume 24, Number 1 (April 2017)                   J Birjand Univ Med Sci. 2017, 24(1): 19-27 | Back to browse issues page


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Hajiahmadi F, Derkhshan A, Nikandish M, Malaekeh-Nikouei B. Preparation of tacrolimus ophthalmic solution using cyclodextrins. J Birjand Univ Med Sci.. 2017; 24 (1) :19-27
URL: http://journal.bums.ac.ir/article-1-2230-en.html

1- Faculty of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
2- Eye Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
3- Department of Ophthalmology, Faculty of Medicine, Birjand University of Medical Sciences, Birjand, Iran.
4- Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran. , malaekehb@mums.ac.ir
Abstract:   (1256 Views)

Background and Aim: Application of topical tacrolimus in Vernal Keratoconjunctivitis is considered as an alternative to steroids. Due to the low aqueous solubility of the drug, preparing a solution of the drug has got particular importance. In the present study, tacrolimus eye drop was prepared using cyclodextrin, as a drug solubility enhancer.

Materials and Methods: To improve the aqueous solubility of tacrolimus, 5 types of cyclodextrins called α, γ, hydroxypropyl (HP)-β, HP-γ, and sulfobutyl ether (SBE)-β-cyclodextrin (CD), were used. After phase solubility studies, the most appropriate cyclodextrin was selected to prepare tacrolimus eye drop. For eye drop preparation, phosphate buffer (pH=7.4), hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA) polymers (viscosity increasing agent), methyl paraben and benzalkonium chloride (preservative agent) were used together with cyclodextrin-tacrolimus complex.

Results: α, HP-β, and γ-CD had the most effect on aqueous solubility, respectively. These 3 types of CDs, respectively increased the intrinsic solubility of tacrolimus174, 160, and 102 times. Taking this into account, α and HP-β-CD were chosen to prepare a soluble form of tacrolimus. In the eye drop formulation containing CD-tacrolimus complex, methyl paraben and HPMC, remarkably reduced the drug solubility while there was not a critical change in the solubility of tacrolimus in the case of CD-tacrolimus complex, buffer, HPMC or PVA and benzalkonium chloride.

Conclusion: It is possible to prepare tacrolimus eye drop (0.05%) using cyclodextrins.

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Type of Study: Original Article | Subject: Pharmacology
Received: 2017/01/23 | Accepted: 2017/05/14 | Published: 2017/05/29

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