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Miscellaneous (34)

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Abstract #78445 Published in IGR 20-1

Metal-organic frameworks, NH-MIL-88(Fe), as carriers for ophthalmic delivery of brimonidine

Kim SN; Park CG; Huh BK; Lee SH; Min CH; Lee YY; Kim YK; Park KH; Choy YB
Acta biomaterialia 2018; 79: 344-353

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: We have proposed a metal-organic framework (MOF), NH-MIL-88(Fe), as a novel carrier for topical drug delivery to the eye. The NH-MIL-88(Fe) particles were prepared via a solvothermal synthesis method and their structure was confirmed by powder X-ray diffraction, Fourier transform infrared analysis, thermogravimetric analysis, electron microscopy, and N adsorption-desorption measurements. When brimonidine, an anti-glaucoma medicine, was encapsulated into NH-MIL(Fe)-88 (i.e., NH-MIL-88(Fe)/Br), the drug was loaded at 121.3 µg/mg and released in a sustained manner for up to 12 h. The NH-MIL-88(Fe)/Br exhibited mucoadhesive properties and remained on rabbit eyes for a period of up to 4 h. Consequently, a high concentration of brimonidine was found in tears for a prolonged period after the administration of NH-MIL-88(Fe)/Br, which resulted in a greater than two-fold increase in drug bioavailability and activity period compared with those of Alphagan P, which are brimonidine eye drops already approved for clinical use. Hence, NH-MIL-88(Fe) is suggested to be a promising carrier for topical delivery to the eye that provides enhanced bioavailability of ocular drugs. STATEMENT OF SIGNIFICANCE: We suggest NH-MIL(Fe)-88, a type of metal-organic frameworks (MOFs), as delivery carriers of an ophthalmic drug, brimonidine. The NH-MIL(Fe)-88 particles possess a mucoadhesive property, hence prolonged retention in the preocular space when topically administered to the eye. The particles can also encapsulate the drug in their micro-pores, through which the drug can be released in a sustained manner. Therefore, when tested to rabbit eyes in vivo, the drug-loaded NH-MIL(Fe)-88 particles were shown to enhance the ocular drug bioavailability, as compared with Alphagan P, the marketed eye drops of brimonidine.

Interdisciplinary Program in Bioengineering, College of Engineering, Seoul National University, Seoul 08826, Republic of Korea.

Full article

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Classification:

11.16 Vehicles, delivery systems, pharmacokinetics, formulation (Part of: 11 Medical treatment)
11.3.3 Apraclonidine, brimonidine (Part of: 11 Medical treatment > 11.3 Adrenergic drugs)

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