In vitro investigations of α-amylase mediated hydrolysis of cyclodextrins in the presence of ibuprofen, flurbiprofen, or benzo[a]pyrene

Zwitterionic near infrared fluorescent agents for noninvasive real-time transcutaneous assessment of kidney function

“…Firstly, introduction of HPβCD is used to increase hydrophilicity, decrease PPB and accelerate excretion, due to HPβCD having better water solubility than β-cyclodextrin (βCD) and higher stability against hydrolysis by α-amylases from either porcine or human origin, 14 and it allows the encapsulation of the lipophilic fluorophore into the cavity of HPβCD. The merit of its non-toxicity resulted in FDA approval ten years ago.…”

“…The merit of its non-toxicity resulted in FDA approval ten years ago. 14 Additionally, its well-defined structure, low cost and excellent availability make it an ideal component for GFR agents in comparison with inulin and sinistrin. Secondly, NIR fluorophores were employed for labeling HPβCD, thus, providing a deeper penetration depth and minimizing the disturbance of auto-fluorescence from skin tissue during transcutaneous measurements.…”

Light‐Emitting Agents for Noninvasive Assessment of Kidney Function

“…CDs are well tolerated in humans and have no adverse effects on the kidneys or other organs following either oral or intravenous administration . The merits of their nontoxicity resulted in FDA approval more than ten years ago . The reason for the utilization of HPCDs rather than CDs is that HPCDs not only have better water solubility than their native CDs, but they are also more stable to hydrolysis by α‐amylases of either porcine or human origin .…”

Pharmacokinetics of cyclodextrins and drugs after oral and parenteral administration of drug/cyclodextrin complexes

“…[2] It is known that the degradation rate of CDs in the GI tract can be hampered by inclusion complex formation. [12] After parenteral administration, CDs, such as HPβCD, SBEβCD and sugammadex are rapidly excreted intact from the body in urine via glomerular filtration. [13,14] For example, HPβCD has a small volume of distribution (VD ≈ 0.2 l/kg) and a short half-life (t 1 ⁄2 ≈ 1.7 h in humans with normal kidney function), and is mainly (approximately 97%) excreted unchanged in urine after parenteral administration.…”

“…They have very low to negligible oral bioavailability (well below 4%) and are metabolized in the GI tract, mainly by bacterial digestion, to form oligosaccharides, monosaccharides and gases such as hydrogen, carbon dioxide and methane [2]. It is known that the degradation rate of CDs in the GI tract can be hampered by inclusion complex formation [12]. After parenteral administration, CDs, such as HPβCD, SBEβCD and sugammadex are rapidly excreted intact from the body in urine via glomerular filtration [13,14].…”