Preparation and Characterization of Tenofovir Disoproxil-Loaded Enteric Microparticle
- Authors
- Kim, Young Hoon; Kim, Yu-Chul; Kim, Jae Yeol; Byeon, Jimi; Maeng, Han-Joo; Kim, Sung Tae; Min, Kyoung Ah; Jang, Dong-Jin; Cho, Kwan Hyung
- Issue Date
- Sep-2020
- Publisher
- AMER SCIENTIFIC PUBLISHERS
- Keywords
- Tenofovir Disorpoxil; Eudragit L-100; Ethyl Cellulose; Enteric Microparticle
- Citation
- JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY, v.20, no.9, pp.5796 - 5799
- Journal Title
- JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
- Volume
- 20
- Number
- 9
- Start Page
- 5796
- End Page
- 5799
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/60105
- DOI
- 10.1166/jnn.2020.17641
- ISSN
- 1533-4880
- Abstract
- Tenofovir disoproxil (TD) has narrow absorption site mostly in upper intestinal tract where tenofovir rapidly decomposes. The aim of this work was to prepare and evaluate tenofovir disoproxil-loaded enteric microparticles (TDEMs) for the enhanced duodenal delivery. TDEMs were composed of TD, eudragit L-100 (EL) and ethyl cellulose (EC) as release-controlling polymers. For the physicochemical characterization, TDEMs were evaluated in terms of encapsulation efficiency (EE%), scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR). The dissolution test was also performed while continuously changing the medium pH. The EE% of TO in TDEMs was good and more than 90%. The EC and EL formed a physically mixed structure and maintained their respective properties in TDEMs as confirmed by SEM image and FT-IR analysis. Combination of EL and EC gave higher enteric properties to TDEMs than the single use of EL or EC. The optimized TDEM (TD/EUEC = 0.2/1/1, w/w/w ratio) yielded mean dissolution rate less than 10% in 1 h at pH 1.2, but completed dissolution with a dissolution more than 85% within 1 h at pH 6.5. Thus, the suggested TDEM would be promising enteric microparticles for the intensive delivery of TD to the duodenum.
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