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PubMed · 8254492

Improved bioavailability of para-boronophenylalanine by cyclodextrin complexation.

H Hatanaka·F Komada·Y Mishima·K Okumura
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Abstract

This study was undertaken to develop an oral dosage form for para-boronophenylalanine (BPA) plus cyclodextrin (CD) for use in the thermal neutron capture therapy for malignant melanoma. Powders of the BPA and CD complexes were obtained in a molar ratio of 1:2. X-ray diffraction of the BPA-CD complexes showed halo patterns that indicated that each complex was in a new solid state as an amorphous compound. The enhancement of BPA solubility by glucosyl (G1)- and maltosyl (G2)-alpha-CD was greater than that with the other CDs. The isolation rate of BPA from its complex was different for each BPA-CD complex. The bioavailability of BPA in rats was improved with oral administration of the BPA-alpha-CD, G1-alpha-CD, and G2-alpha-CD complexes. In contrast, a complex of BPA and dimaltosyl (G2G2) or G2-beta-CD, which had low release rate and low solubility, did not improve the bioavailability of BPA. These results indicate that the solubility and release rate of BPA from a complex in solution are important for the bioavailability of BPA after oral administration of BPA-CD complexes.

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AnimalsBiological AvailabilityBoron CompoundsChromatography, High Pressure LiquidCyclodextrinsDrug DesignMalePhenylalaninePowdersRatsRats, WistarSolubilitySpectrophotometry, InfraredX-Ray DiffractionJournal ArticleResearch Support, Non-U.S. Gov't

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H Hatanaka, F Komada, Y Mishima, K Okumura. 1993. Improved bioavailability of para-boronophenylalanine by cyclodextrin complexation.. https://pubmed.ncbi.nlm.nih.gov/8254492/

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