Pharmacokinetics and Toxicity of a <i>p</i>-Boronophenylalanine—Cyclodextrin Formulation Delivered by Intravenous Infusion to Dogs

LaHann, T. R.; Bauer, William F.; Gavin, Paul; Lu, Dongrui R.

doi:10.1021/bk-1994-0545.ch006

Cited by 4 publications

(2 citation statements)

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“…LaHann et al 62,63 have studied the pharmacokinetics in dogs of p-boronophenylalanine following iv administration of 4.43 mg‚kg -1 drug in an aqueous HP--CD solution (to effect greater solubility) versus a more dilute 0.96 mg‚kg -1 aqueous solution. The pharmacokinetics of p-boronophenylalanine were found to be significantly different from the two dosage forms.…”

Section: Parenteral Applications Of Cyclodextrinsmentioning

confidence: 99%

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Rajewski¹,

Stella²

1996

Journal of Pharmaceutical Sciences

759

374

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The objective of this Review is to summarize and critique recent findings and applications of both unmodified and modified cyclodextrins for in vivo drug delivery. This review focuses on the use of cyclodextrins for parenteral, oral, ophthalmic, and nasal drug delivery. Other routes including dermal, rectal, and pulmonary delivery are also briefly addressed. This Review primarily focuses on newer findings concerning cyclodextrin derivatives which are likely to receive regulatory acceptance due to improved aqueous solubility and safety profiles as compared to the unmodified cyclodextrins. Many of the applications reviewed involve the use of hydroxypropyl-beta-cyclodextrins (HP-beta-CDs) and sulfobutylether-beta-cyclodextrins (SBE-beta-CDs) which show promise of greater safety while maintaining the ability to form inclusion complexes. The advantages and limitations of HP-beta-CD, SBE-beta-CD, and other cyclodextrins are addressed.

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Section: Parenteral Applications Of Cyclodextrinsmentioning

confidence: 99%

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Rajewski¹,

Stella²

1996

Journal of Pharmaceutical Sciences

759

374

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“…11,12 BPA was recently approved in Japan as a 10 B delivery drug for BNCT of head and neck cancer. 13 However, BPA does have drawbacks, such as low solubility requiring formulation with fructose 14 or sorbitol; 15 high-volume continuous infusion during BNCT; and in many cancers, low tumor delivery and low tumor-to-blood and normal tissue ratios. Thus, there is a need to identify new boron delivery drugs that improve these drawbacks of BPA.…”

Section: ■ Introductionmentioning

confidence: 99%

Boronotyrosine, a Borylated Amino Acid Mimetic with Enhanced Solubility, Tumor Boron Delivery, and Retention for the Re-emerging Boron Neutron Capture Therapy Field

Raitano,

Martin,

Zhang

et al. 2023

J. Med. Chem.

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Boron neutron capture therapy (BNCT) is a reemerging binary cellular level cancer intervention that occurs through the interaction of a cancer-specific 10 boron ( 10 B) drug and neutrons. We created a new 10 B drug, 3-borono-L-tyrosine (BTS), that improves on the characteristics of the main historical BNCT drug 4-borono-L-phenylalanine (BPA). BTS has up to 4 times greater uptake in vitro than BPA and increased cellular retention. Like BPA, BTS uptake is mediated by the L-type amino acid transporter-1 (LAT1) but is less sensitive to natural amino acid competition. BTS can be formulated and bolus dosed at much higher levels than BPA, resulting in 2−3 times greater boron delivery in vivo. Fast blood clearance and greater tumor boron delivery result in superior tumor-to-blood ratios. BTS boron delivery appears to correlate with LAT1 expression. BTS is a promising boron delivery drug that has the potential to improve modern BNCT interventions.

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