Enteric complex layer-coated controlled release of capsaicin from phytosterol/γ-cyclodextrin microparticles via guest exchange reaction with taurocholic acid

Sasako, Hiroshi; Koyama, Kazuo; Higashi, Kenjirou; Ueda, Keisuke; Ishimoto, Arisa; Moribe, Kunikazu

doi:10.1016/j.ejps.2021.106038

Cited by 4 publications

(2 citation statements)

References 27 publications

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“…19 The release of pungent capsaicin encapsulated in the microparticle is suppressed in the mouth and under gastric conditions, reducing undesirable irritation, whereas the drug is immediately released under intestinal conditions for efficient absorption into the body. 20 In the present study, for further functionalization of the PSE/γ-CD microparticle, we develop a nanoparticle composed of cholesteryl oleate (ChO) and γ-CD. Instead of PSE, ChO is used as a lipid to accurately control the properties of the nanoparticle and gain an in-depth understanding of the formation mechanism of the nanoparticle because PSE is a mixture of various sterol esters.…”

Section: ■ Introductionmentioning

confidence: 99%

“…This microparticle demonstrates significant potential as a controlled drug-release carrier . The release of pungent capsaicin encapsulated in the microparticle is suppressed in the mouth and under gastric conditions, reducing undesirable irritation, whereas the drug is immediately released under intestinal conditions for efficient absorption into the body …”

Section: Introductionmentioning

confidence: 99%

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Drug-Loaded Nanocarriers Composed of Cholesteryl Oleate Crystal Cores and Multiple-Nanosheet Shells of γ-Cyclodextrin Inclusion Complex Crystals

Ishimoto

Sasako²,

Omori

et al. 2022

Langmuir

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In this study, we prepared drug-loaded nanocarriers made of cholesteryl oleate (ChO) and γ-cyclodextrin (γ-CD). A nanosuspension (nanosuspension-I, NS-I) containing nanoparticles with a mean size of approximately 170 nm was obtained through the solvent-diffusion method using ethanol. A second nanosuspension (nanosuspension-II, NS-II), which was prepared by freeze-drying and redispersion of NS-I, exhibited an increased particle size of approximately 210 nm. Cryogenic transmission electron microscopy (cryo-TEM) and atomic force microscopy (AFM) force−distance curves indicated that the nanoparticles in NS-I were oblong and soft. However, those in NS-II were angular and stiff, and, interestingly, multiple nanosheets covered the solid−liquid interface. Synchrotron wide-angle X-ray diffraction (WAXD) analysis of NS-II indicated that the nanoparticles in it had a core−shell structure, where the ChO crystal in the inner core was covered by multiple nanosheets of ChO/γ-CD inclusion complex crystals. The X-ray peak analysis suggested that the γ-CD columns of the nanosheets were vertically stacked onto the ChO crystal interface. It was found that the nanosheets on the nanoparticle interface were formed during the freezing process. A model drug carbamazepine (CBZ) was loaded into the ChO/γ-CD nanoparticles by pre-dissolving CBZ in ethanol during the solvent-diffusion process. Cryo-TEM, 1 H NMR, ζ-potentials, and synchrotron WAXD indicated that CBZ was unexpectedly loaded into the shell as a CBZ/γ-CD inclusion complex crystalline nanosheet. The specific nanosheet structure, where ChO and CBZ coexisted in the same crystal of γ-CD, could achieve CBZ loading in the nanoparticles. ChO/γ-CD nanoparticles with the unique core−shell structure are expected to perform as practical carriers for drug delivery.

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Section: ■ Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%