Physicochemical, in silico and in vivo evaluation of a danazol–β-cyclodextrin complex

Ganesh Jadhav, Pradeep R. Vavia
In: International Journal of Pharmaceutics · 2007 · vol. 352(1-2) , pp. 5–16 · doi:10.1016/j.ijpharm.2007.10.005 · PMID:18023545 · W1968084938
article OA: closed CC0 ⤵ 2 in-corpus citations
View on OpenAlex View on PubMed View at publisher
⚙ AI-generated summary by gemini-2.5-flash-lite, 2026-06-09 ⓘ

This study investigated the physicochemical properties, computational interactions, and in vivo behavior of a danazol-beta-cyclodextrin complex to assess its potential as a drug formulation.

One-sentence paraphrase of the abstract; not a substitute for reading it. No clinical advice. How this works

Abstract

Inclusion complexation of danazol with beta-cyclodextrin (BCD) in aqueous solution, in solid state and in silico state was investigated to examine the interactions of danazol with BCD. The study also explored the potential application of danazol-beta-cyclodextrin complex as an oral antiovulatory agent. Phase solubility analysis suggested formation of first-order soluble complex with stability constant 972.03 M(-1) while Job's plot affirmed 1:1 stoichiometry. Solution state complexation in water was studied by ultra violet absorption, circular dichroism and nuclear magnetic resonance ((1)H NMR) spectroscopy. The solid state complexes were evaluated by differential scanning calorimetry, powder X-ray diffractometry, fourier transform infrared spectroscopy and scanning electron microscopy. Thermodynamic studies in water indicated exothermic nature of inclusion complexation. Molecular modeling was used to help establish the mode of interaction of BCD with danazol. (1)H NMR analysis suggested that the protons of steroidal skeleton of danazol are preferably involved in the complexation with BCD, which was confirmed by molecular dynamic simulations. An inclusion complex model has been established for explaining the observed enhancement of solubility of danazol in water by BCD. Moreover, in mouse model, danazol-beta-cyclodextrin complex at 51.2mg/kg (equivalent to 400mg human dose) showed 100% anovulation when given orally.

My notes (saved in your browser only)

Citation neighborhood

Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

References (42)

Cited by (1)

Source provenance

openalex
last seen: 2026-05-11T05:49:40.447239+00:00
unpaywall
last seen: 2026-08-18T06:27:49.008893+00:00
License: CC0 · commercial use OK