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Research Article

HPLC–MS/MS-Based Analysis of Everolimus in Rabbit Aqueous Humor: Pharmacokinetics of in Situ Gel Eye Drops of Suspension

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Pages 267-278 | Received 27 Aug 2018, Accepted 04 Dec 2018, Published online: 21 Jan 2019
 

Abstract

Aim: Everolimus is an inhibitor of mTOR which is derived from rapamycin. Its high corneal permeability and bioavailability makes it an effective treatment for ocular disorders. To study the pharmacokinetics of in situ gel eye drops of everolimus suspension after ocular administration in rabbit aqueous humor, we developed a rapid and reliable HPLC–MS/MS method. Methodology/results: Ascomycin was selected as the internal standard. HPLC–MS/MS method was used to investigate the concentration–time relationship of everolimus in rabbit aqueous humor through protein precipitation technique. The validated results showed good linearity, accuracy and precision. Conclusion: The method developed in this study is rapid, sensitive and reliable for the determination of the concentration of everolimus in rabbit aqueous humor.

Financial & competing interests disclosure

The project was supported by grants from Zhejiang Provincial Science and Technology Foundation (2017F30005), Public Welfare Foundation (2016C37074) and Zhejiang Pharmaceutical Association Foundation (2018ZYY16). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

We thank Freescience for their professional English language editing services funded by Zhejiang Provincial Science and Technology Foundation (2017F30005).

Ethical conduct of research

The authors’ state that they have obtained appropriate institutional review board approval or have followed the principles outlined in the Declaration of Helsinki for all human or animal experimental investigations. In addition, for investigations involving human subjects, informed consent has been obtained from the participants involved.

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