In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs

Research output: Contribution to journalJournal article

Standard

In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs. / Borkar, Nrupa Nitin; Holm, René; Yang, Mingshi; Müllertz, Anette; Mu, Huiling.

In: International Journal of Pharmaceutics, Vol. 513, No. 1-2, 09.09.2016, p. 211-217.

Research output: Contribution to journalJournal article

Harvard

Borkar, NN, Holm, R, Yang, M, Müllertz, A & Mu, H 2016, 'In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs', International Journal of Pharmaceutics, vol. 513, no. 1-2, pp. 211-217. https://doi.org/10.1016/j.ijpharm.2016.09.024

APA

Borkar, N. N., Holm, R., Yang, M., Müllertz, A., & Mu, H. (2016). In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs. International Journal of Pharmaceutics, 513(1-2), 211-217. https://doi.org/10.1016/j.ijpharm.2016.09.024

Vancouver

Borkar NN, Holm R, Yang M, Müllertz A, Mu H. In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs. International Journal of Pharmaceutics. 2016 Sep 9;513(1-2):211-217. https://doi.org/10.1016/j.ijpharm.2016.09.024

Author

Borkar, Nrupa Nitin ; Holm, René ; Yang, Mingshi ; Müllertz, Anette ; Mu, Huiling. / In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs. In: International Journal of Pharmaceutics. 2016 ; Vol. 513, No. 1-2. pp. 211-217.

Bibtex

@article{cfe53f95d77d4f149a55ad2b74ea30e4,
title = "In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs",
abstract = "In the present study, the differences in oral absorption of apomorphine and its diester prodrugs and the effect of lipid-based formulations on the absorption of apomorphine or its prodrugs were investigated. Apomorphine, dilauroyl apomorphine (DLA) and dipalmitoyl apomorphine (DPA) were orally administered (0.24mmol/kg) to rats as: DLA-o/w emulsion, DPA-o/w emulsion, apomorphine-o/w emulsion, apomorphine aqueous suspension, DLA-Maisine, DLA-soybean oil, DLA-self-emulsifying drug delivery systems (SEDDS), and DLA-w/o emulsion. The o/w and w/o emulsion consisted of Maisine 35-1 emulsified with water in 1:3 and 4:1 ratio, respectively. Tmax of diesters was significantly increased (p≤0.05) compared to apomorphine in o/w emulsion, suggesting that esterification yielded prolonged drug absorption. Cmax, AUC and the relative bioavailability of apomorphine after DLA-SEDDS administration was higher (p≤0.05) than after DLA-w/o administration, indicating that triglycerides and surfactants improved the oral absorption of DLA. Similarly, Cmax and AUC after dosing apomorphine-o/w were significantly higher (p≤0.05) than that of aqueous suspension. This suggested that lipids and lipolysis products possibly aided apomorphine micellar solubilization in intestinal fluids. A combination of prodrug strategy and lipid-based formulations facilitated a higher and prolonged absorption of apomorphine from its diester prodrugs.",
author = "Borkar, {Nrupa Nitin} and Ren{\'e} Holm and Mingshi Yang and Anette M{\"u}llertz and Huiling Mu",
year = "2016",
month = "9",
day = "9",
doi = "10.1016/j.ijpharm.2016.09.024",
language = "English",
volume = "513",
pages = "211--217",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

RIS

TY - JOUR

T1 - In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs

AU - Borkar, Nrupa Nitin

AU - Holm, René

AU - Yang, Mingshi

AU - Müllertz, Anette

AU - Mu, Huiling

PY - 2016/9/9

Y1 - 2016/9/9

N2 - In the present study, the differences in oral absorption of apomorphine and its diester prodrugs and the effect of lipid-based formulations on the absorption of apomorphine or its prodrugs were investigated. Apomorphine, dilauroyl apomorphine (DLA) and dipalmitoyl apomorphine (DPA) were orally administered (0.24mmol/kg) to rats as: DLA-o/w emulsion, DPA-o/w emulsion, apomorphine-o/w emulsion, apomorphine aqueous suspension, DLA-Maisine, DLA-soybean oil, DLA-self-emulsifying drug delivery systems (SEDDS), and DLA-w/o emulsion. The o/w and w/o emulsion consisted of Maisine 35-1 emulsified with water in 1:3 and 4:1 ratio, respectively. Tmax of diesters was significantly increased (p≤0.05) compared to apomorphine in o/w emulsion, suggesting that esterification yielded prolonged drug absorption. Cmax, AUC and the relative bioavailability of apomorphine after DLA-SEDDS administration was higher (p≤0.05) than after DLA-w/o administration, indicating that triglycerides and surfactants improved the oral absorption of DLA. Similarly, Cmax and AUC after dosing apomorphine-o/w were significantly higher (p≤0.05) than that of aqueous suspension. This suggested that lipids and lipolysis products possibly aided apomorphine micellar solubilization in intestinal fluids. A combination of prodrug strategy and lipid-based formulations facilitated a higher and prolonged absorption of apomorphine from its diester prodrugs.

AB - In the present study, the differences in oral absorption of apomorphine and its diester prodrugs and the effect of lipid-based formulations on the absorption of apomorphine or its prodrugs were investigated. Apomorphine, dilauroyl apomorphine (DLA) and dipalmitoyl apomorphine (DPA) were orally administered (0.24mmol/kg) to rats as: DLA-o/w emulsion, DPA-o/w emulsion, apomorphine-o/w emulsion, apomorphine aqueous suspension, DLA-Maisine, DLA-soybean oil, DLA-self-emulsifying drug delivery systems (SEDDS), and DLA-w/o emulsion. The o/w and w/o emulsion consisted of Maisine 35-1 emulsified with water in 1:3 and 4:1 ratio, respectively. Tmax of diesters was significantly increased (p≤0.05) compared to apomorphine in o/w emulsion, suggesting that esterification yielded prolonged drug absorption. Cmax, AUC and the relative bioavailability of apomorphine after DLA-SEDDS administration was higher (p≤0.05) than after DLA-w/o administration, indicating that triglycerides and surfactants improved the oral absorption of DLA. Similarly, Cmax and AUC after dosing apomorphine-o/w were significantly higher (p≤0.05) than that of aqueous suspension. This suggested that lipids and lipolysis products possibly aided apomorphine micellar solubilization in intestinal fluids. A combination of prodrug strategy and lipid-based formulations facilitated a higher and prolonged absorption of apomorphine from its diester prodrugs.

U2 - 10.1016/j.ijpharm.2016.09.024

DO - 10.1016/j.ijpharm.2016.09.024

M3 - Journal article

C2 - 27615708

VL - 513

SP - 211

EP - 217

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -

ID: 166159342