| Title |
In Vitro Lipolysis Data Does Not Adequately Predict the In Vivo Performance of Lipid-Based Drug Delivery Systems Containing Fenofibrate
|
|---|---|
| Published in |
The AAPS Journal, April 2014
|
| DOI | 10.1208/s12248-014-9589-4 |
| Pubmed ID | |
| Authors |
Nicky Thomas, Katharina Richter, Thomas B. Pedersen, René Holm, Anette Müllertz, Thomas Rades |
| Abstract |
The present study investigated the utility of in vitro lipolysis performance indicators drug solubilization and maximum supersaturation ratio (SR(M)) for their predictive use for the in vivo performance in a minipig model. The commercial Lipanthyl formulation and a series of LbDDS based on identical self-nanoemulsifying drug delivery systems (SNEDDS) containing 200 mg of fenofibrate, either dissolved or suspended, were subjected to combined gastric (pH 2) and intestinal (pH 6.5) in vitro lipolysis. Based on the solubilization profiles and SRM the rank-order SNEDDS (75% drug load) > super-SNEDDS (150% drug load, dissolved) = SNEDDS suspension (150% drug load, partially suspended) > Lipanthyl was established, with an increased likelihood of drug precipitation above SR(M) > 3. The in vitro performance, however, was not reproduced in vivo in a minipig model as the mean plasma concentration over time curves of all LbDDS were comparable, independent of the initial physical state of the drug. There was no correlation between the area under the solubilization-time curves (AUC(in vitro)) of the intestinal step and the AUC(in vivo). The study suggests careful interpretation of in vitro performance criteria and revision of LbDDS optimization towards increased solubilization. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 56 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 56 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 8 | 14% |
| Student > Master | 7 | 13% |
| Student > Bachelor | 5 | 9% |
| Researcher | 5 | 9% |
| Lecturer | 5 | 9% |
| Other | 9 | 16% |
| Unknown | 17 | 30% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 20 | 36% |
| Medicine and Dentistry | 5 | 9% |
| Chemistry | 3 | 5% |
| Agricultural and Biological Sciences | 2 | 4% |
| Biochemistry, Genetics and Molecular Biology | 1 | 2% |
| Other | 5 | 9% |
| Unknown | 20 | 36% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 05 April 2014.
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#18,370,767
of 22,753,345 outputs
Outputs from The AAPS Journal
#1,100
of 1,284 outputs
Outputs of similar age
#163,251
of 225,533 outputs
Outputs of similar age from The AAPS Journal
#10
of 15 outputs
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