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KMID : 0043320180410080848
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Archives of Pharmacal Research
2018 Volume.41 No. 8 p.848 ~ p.860
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Macropored microparticles with a core?shell architecture for oral delivery of biopharmaceuticals
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Homayun Bahman
Kumar Ankit
Nascimento Priscila T. H.
Choi Hyo-Jick
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Abstract
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Microparticles (MPs) have been extensively researched as a potential drug delivery vehicle. Here, we investigated the fabrication of MPs with pH-responsive macropores and evaluated their potential applicability in developing solid oral drug formulations. Our previous study showed that macropored MPs, made of Eudragit® L100-55, could encapsulate 100 nm, 1 μm, and 4 μm sized fluorescent beads?model drugs that are mimicking vaccines, bacteria, and cells. In the present study, closed-pored MPs after freeze-drying were coated with a gastric soluble Eudragit® EPO layer to protect MPs in the simulated pregastric environment. Subsequently, drug encapsulated MPs maintained their intact closed-pored structure in the simulated gastric environment and exhibited a rapid release in the simulated intestine environment. Our MP system was found to provide a significantly higher level of protection to the encapsulated lactase enzyme compared to the control sample (i.e. without using MPs). Real-time fluorescence microscopy analysis showed that macropored MPs released encapsulated drugs in a burst-release pattern and in a size-independent manner. This work shows that our proposed EPO-coated MPs with pH-responsive macropores can meet the challenges posed by the multiple physiological environments of the digestive tract and be used in developing highly effective solid oral drug/vaccine formulations.
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KEYWORD
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Oral delivery, Microparticles, Macropore, Digestive tract, pH
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