Hydroxy propyl Cyclodextrins: Potential Synergism with Carcinogens
References and Notes (17)
- et al.
Anal. Chim. Acta
(1992) - et al.
Toxicology
(1991) - et al.
Lipid Res
(1984) - et al.
Pharm. Sci
(1986) - et al.
Proc. Natl. Acad. Sci. U.S.A
(1990) - et al.
- et al.
Colloid Interface Sci
(1993)
Cited by (13)
Does the Digestibility of Cyclodextrins Influence the In Vivo Absorption of Benzo[a]pyrene in Rats?
2016, Journal of Pharmaceutical SciencesCitation Excerpt :The release mechanism of a compound from a cyclodextrin complex upon oral administration has been suggested to be a combination of dilution, which must be assumed to be constant across groups, and competitive displacement by bile salts present within the intestinal tract,20,21 that is, differences in stability constants between cyclodextrins of both compound and bile salts may in theory influence the release and thereby the absorption. To the best of our knowledge, the stability constant between β-cyclodextrin and benzo[a]pyrene has not been determined, but the apparent stability constants measured by phase solubility studies has been reported for 2-HP-β-cyclodextrin to be 5344 M−1 and 25,900 M−1,22,23 the later value measured in the presence of 15 mM sodium taurocholate, that is, with competitive interaction. For γ-cyclodextrin, we have found an apparent stability constant of 37,050 M−1 at 37°C in a phase solubility study (data not shown); the relative affinity of benzo[a]pyrene toward the 2 different classes of cyclodextrins was in the same range.
A heuristic model to quantify the impact of excess cyclodextrin on oral drug absorption from aqueous solution
2016, European Journal of Pharmaceutics and BiopharmaceuticsFormulations based on alpha cyclodextrin and soybean oil: An approach to modulate the oral release of lipophilic drugs
2012, Journal of Controlled ReleaseCitation Excerpt :Lipid digestion products induce secretion of pancreatic and biliary fluids which alter the luminal environment of the small intestine [38]. Bile salts decrease the partition coefficient of drugs in intestinal media [39–41] while pancreatic lipases participate to lipid digestion [42] and contribute to the release of drugs from oil [43]. Thus, the resulting mixed micelles probably increase the amount of IND available for absorption.
Co-solubilization of poorly soluble drugs by micellization and complexation
2006, International Journal of Pharmaceuticsβ-cyclodextrin reduces bioavailability of orally administered [ <sup>3</sup>H]benzo[a]pyrene in the rat
2005, Journal of Pharmaceutical SciencesCitation Excerpt :Thus, although cyclodextrins are able to increase solubility of lipophilic compounds like BaP, the rate of release from the complex may be decreased in the in vivo situation. In conclusion, rather than causing enhanced absorption of benzo[a]pyrene as proposed by Horsky and Pitha,9 our results indicate that β‐cyclodextrin may act as a scavenger for such compounds following oral administration, thus reducing the systemic exposure by preventing absorption. This finding emphasizes the need to exercise caution in interpreting in vitrosolubility information data when extrapolating to the in vivosituation.
Pharmaceutical applications of cyclodextrins. III. Toxicological issues and safety evaluation
1997, Journal of Pharmaceutical Sciences
Abstract published in Advance ACS Abstracts, November 1, 1995.