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Drug Discov Ther. 2019;13(6):343-353. doi: 10.5582/ddt.2019.01090.

Janus microspheres for enhanced enteral drug delivery: Preparation and orientated attachment to a Caco-2 monolayer.

Author information

1
Laboratory of Pharmaceutics, Faculty of Pharmacy, Osaka Ohtani University, Tondabayashi, Osaka, Japan.
2
Laboratory of Clinical Pathology, Faculty of Pharmacy, Josai University, Sakadoshi, Saitama, Japan.

Abstract

Conventional oral preparations generally release incorporated drugs omnidirectionally, including into the lumen, leading to a low bioavailability of drugs that are unstable in the gastrointestinal tract. Here, we designed Janus microspheres for efficient mucosal drug delivery as single-sided-release microspheres with the oriented attachment to mucus and evaluated their attachment to and orientation on a Caco-2 (human Caucasian colon adenocarcinoma cell line) monolayer. The microspheres comprised a mucus-oriented hemisphere of an ammonioalkyl methacrylate copolymer and a protective hemisphere of a hard fat. Fluorescein isothiocyanate-dextran with an average molecular weight of 3,000-5,000 Da (FD4) was used as a model hydrophilic drug. A water-in-oil emulsion-type solvent evaporation method was employed for fabrication of the Janus microspheres. The yield of Janus microspheres was found to be dependent on the polymer-to-hard fat ratio, with a maximum yield of over 90% being obtained at a ratio of 1:2, whereas lower and higher ratios resulted in monolithic or star-shaped microspheres. FD4 was specifically localized in the polymeric hemisphere. A cell culture study revealed that the Janus microspheres attached to a Caco-2 monolayer via their polymeric hemispheres with the hard fat hemisphere providing a protective sealing. This may lead to the development of an effective enteral drug delivery system for biomedicines, such as polypeptides and nucleic acids.

KEYWORDS:

Single-sided-release microspheres; ammonioalkyl methacrylate copolymer; hard-fat; solvent evaporation method

PMID:
31956233
DOI:
10.5582/ddt.2019.01090
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