In Vivo Performance of Fenofibrate Formulated With Ordered Mesoporous Silica Versus 2-Marketed Formulations: A Comparative Bioavailability Study in Beagle Dogs
2016
Аутори
Bukara, KatarinaSchueller, Laurent
Rosier, Jan
Daems, Tinne
Verheyden, Loes
Eelen, Siemon
Martens, Johan A.
Van den Mooter, Guy
Bugarski, Branko
Kiekens, Filip
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
The present study aims to evaluate the in vitro and in vivo performance of ordered mesoporous silica (OMS) as a carrier for the poorly water-soluble compound fenofibrate. Fenofibrate was loaded into OMS via incipient wetness impregnation to obtain a 29% drug load and formulated into capsules. Two capsule dosage forms (containing 33.5 and 16.75 mg fenofibrate, respectively) were compared with the commercially available forms-Lipanthyl (R) (fenofibrate microcrystals) and Tricor (R) (fenofibrate nanocrystals). In vitro dissolution tests showed that the amount of fenofibrate released from Lipanthyl (R) and Tricor (R) was approximately 30%, whereas approximately 66% and 60% of the drug was released from OMS capsules containing 33.5 and 16.75 mg of fenofibrate, respectively. Storage of OMS capsules loaded with 33.5 mg of fenofibrate at 25 degrees C/60% relative humidity (RH) or 40 degrees C/75% RH did not alter the release kinetics, nor the physical state of the compound, pointing the stabil...ity of the present formulation. The in vivo study in dogs confirmed satisfying level of safety and tolerability of fenofibrate-OMS formulation (eq. 33.5 mg) with the potential to improve the absorption of fenofibrate. Though some variability in the data, this formulation is promising to be further investigated in a clinical trial setting.
Кључне речи:
ordered mesoporous silica / fenofibrate / poor solubility / dissolution / oral bioavailabilityИзвор:
Journal of Pharmaceutical Sciences, 2016, 105, 8, 2381-2385Издавач:
- Wiley-Blackwell, Hoboken
Финансирање / пројекти:
- Formac Pharmaceuticals NV, Gaston Geenslaan, Leuven, Belgium
DOI: 10.1016/j.xphs.2016.05.019
ISSN: 0022-3549
PubMed: 27364460
WoS: 000381770400017
Scopus: 2-s2.0-84979041804
Институција/група
Tehnološko-metalurški fakultetTY - JOUR AU - Bukara, Katarina AU - Schueller, Laurent AU - Rosier, Jan AU - Daems, Tinne AU - Verheyden, Loes AU - Eelen, Siemon AU - Martens, Johan A. AU - Van den Mooter, Guy AU - Bugarski, Branko AU - Kiekens, Filip PY - 2016 UR - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/3240 AB - The present study aims to evaluate the in vitro and in vivo performance of ordered mesoporous silica (OMS) as a carrier for the poorly water-soluble compound fenofibrate. Fenofibrate was loaded into OMS via incipient wetness impregnation to obtain a 29% drug load and formulated into capsules. Two capsule dosage forms (containing 33.5 and 16.75 mg fenofibrate, respectively) were compared with the commercially available forms-Lipanthyl (R) (fenofibrate microcrystals) and Tricor (R) (fenofibrate nanocrystals). In vitro dissolution tests showed that the amount of fenofibrate released from Lipanthyl (R) and Tricor (R) was approximately 30%, whereas approximately 66% and 60% of the drug was released from OMS capsules containing 33.5 and 16.75 mg of fenofibrate, respectively. Storage of OMS capsules loaded with 33.5 mg of fenofibrate at 25 degrees C/60% relative humidity (RH) or 40 degrees C/75% RH did not alter the release kinetics, nor the physical state of the compound, pointing the stability of the present formulation. The in vivo study in dogs confirmed satisfying level of safety and tolerability of fenofibrate-OMS formulation (eq. 33.5 mg) with the potential to improve the absorption of fenofibrate. Though some variability in the data, this formulation is promising to be further investigated in a clinical trial setting. PB - Wiley-Blackwell, Hoboken T2 - Journal of Pharmaceutical Sciences T1 - In Vivo Performance of Fenofibrate Formulated With Ordered Mesoporous Silica Versus 2-Marketed Formulations: A Comparative Bioavailability Study in Beagle Dogs EP - 2385 IS - 8 SP - 2381 VL - 105 DO - 10.1016/j.xphs.2016.05.019 ER -
@article{ author = "Bukara, Katarina and Schueller, Laurent and Rosier, Jan and Daems, Tinne and Verheyden, Loes and Eelen, Siemon and Martens, Johan A. and Van den Mooter, Guy and Bugarski, Branko and Kiekens, Filip", year = "2016", abstract = "The present study aims to evaluate the in vitro and in vivo performance of ordered mesoporous silica (OMS) as a carrier for the poorly water-soluble compound fenofibrate. Fenofibrate was loaded into OMS via incipient wetness impregnation to obtain a 29% drug load and formulated into capsules. Two capsule dosage forms (containing 33.5 and 16.75 mg fenofibrate, respectively) were compared with the commercially available forms-Lipanthyl (R) (fenofibrate microcrystals) and Tricor (R) (fenofibrate nanocrystals). In vitro dissolution tests showed that the amount of fenofibrate released from Lipanthyl (R) and Tricor (R) was approximately 30%, whereas approximately 66% and 60% of the drug was released from OMS capsules containing 33.5 and 16.75 mg of fenofibrate, respectively. Storage of OMS capsules loaded with 33.5 mg of fenofibrate at 25 degrees C/60% relative humidity (RH) or 40 degrees C/75% RH did not alter the release kinetics, nor the physical state of the compound, pointing the stability of the present formulation. The in vivo study in dogs confirmed satisfying level of safety and tolerability of fenofibrate-OMS formulation (eq. 33.5 mg) with the potential to improve the absorption of fenofibrate. Though some variability in the data, this formulation is promising to be further investigated in a clinical trial setting.", publisher = "Wiley-Blackwell, Hoboken", journal = "Journal of Pharmaceutical Sciences", title = "In Vivo Performance of Fenofibrate Formulated With Ordered Mesoporous Silica Versus 2-Marketed Formulations: A Comparative Bioavailability Study in Beagle Dogs", pages = "2385-2381", number = "8", volume = "105", doi = "10.1016/j.xphs.2016.05.019" }
Bukara, K., Schueller, L., Rosier, J., Daems, T., Verheyden, L., Eelen, S., Martens, J. A., Van den Mooter, G., Bugarski, B.,& Kiekens, F.. (2016). In Vivo Performance of Fenofibrate Formulated With Ordered Mesoporous Silica Versus 2-Marketed Formulations: A Comparative Bioavailability Study in Beagle Dogs. in Journal of Pharmaceutical Sciences Wiley-Blackwell, Hoboken., 105(8), 2381-2385. https://doi.org/10.1016/j.xphs.2016.05.019
Bukara K, Schueller L, Rosier J, Daems T, Verheyden L, Eelen S, Martens JA, Van den Mooter G, Bugarski B, Kiekens F. In Vivo Performance of Fenofibrate Formulated With Ordered Mesoporous Silica Versus 2-Marketed Formulations: A Comparative Bioavailability Study in Beagle Dogs. in Journal of Pharmaceutical Sciences. 2016;105(8):2381-2385. doi:10.1016/j.xphs.2016.05.019 .
Bukara, Katarina, Schueller, Laurent, Rosier, Jan, Daems, Tinne, Verheyden, Loes, Eelen, Siemon, Martens, Johan A., Van den Mooter, Guy, Bugarski, Branko, Kiekens, Filip, "In Vivo Performance of Fenofibrate Formulated With Ordered Mesoporous Silica Versus 2-Marketed Formulations: A Comparative Bioavailability Study in Beagle Dogs" in Journal of Pharmaceutical Sciences, 105, no. 8 (2016):2381-2385, https://doi.org/10.1016/j.xphs.2016.05.019 . .