Incomplete Desorption of Liquid Excipients Reduces the in Vitro and in Vivo Performance of Self-Emulsifying Drug Delivery Systems Solidified by Adsorption onto an Inorganic Mesoporous Carrier

Michiel Van Speybroeck, Hywel D. Williams, Tri‐Hung Nguyen, Mette U. Anby, Christopher J. H. Porter, Patrick Augustijns
In: Molecular Pharmaceutics · 2012 · vol. 9(9) , pp. 2750–2760 · doi:10.1021/mp300298z · PMID:22870936 · W2333527722
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 ⓘ

Solidifying self-emulsifying drug delivery systems onto a mesoporous carrier reduced danazol's in vitro and in vivo performance due to incomplete desorption from the carrier.

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

Abstract

The purpose of the current study was to provide a mechanistic basis for in vitro and in vivo performance differences between lipid-based formulations solidified by adsorption onto a high surface area material and their respective liquid (i.e., nonadsorbed) counterparts. Two self-emulsifying formulations (based on either medium-chain or long-chain lipids) of the poorly water-soluble drug danazol were solidified by adsorption onto Neusilin US2. Liquid and adsorbed lipid-based formulations were subjected to in vitro dispersion-digestion tests, and additional in vitro experiments were performed to elucidate the cause of performance differences. The bioavailability of danazol after oral administration to rats was also assessed. The percentage of the dose solubilized in the aqueous phase during in vitro dispersion-digesting was ∼35% lower for the adsorbed formulations when compared to their liquid counterparts. This trend was also reflected in vivo, where the bioavailability of danazol after administration of the adsorbed formulations was ∼50% lower than that obtained after administration of the equivalent liquid formulation. Incomplete desorption of the microemulsion preconcentrate from the carrier on dispersion-digestion was identified as the main contributor to the reduced pharmaceutical performance of the adsorbed formulations. The results of the current study indicate that solidification of lipid-based formulations through adsorption onto a high surface area carrier may limit formulation (and drug) release in vivo and thereby reduce oral bioavailability.

My notes (saved in your browser only)

Citation neighborhood (sparse)

Too few in-corpus citations on either side for a chart; here are the lists.

Cites (1)

Cited by (1)

References (40)

Cited by (1)

Source provenance

openalex
last seen: 2026-05-10T10:37:44.503657+00:00
License: CC0 · commercial use OK