The DOI matches its Crossref record; 8 of the 8 references it cites were found in a registry or an index.
Lipid-Based Delivery Systems for Improving the Bioavailability and Lymphatic Transport of a Poorly Water-Soluble LTB4 Inhibitor
Abstract
Ontazolast is a potent inhibitor (IC50 = 1 nm) of calcium ionophore A23187-stimulated leukotriene B4 (LTB4) biosynthesis in human peripheral blood leukocytes. The compound is practically insoluble in water (0.14 microgram/mL) and previous studies in animals have demonstrated extensive presystemic drug clearance through hepatic first-pass metabolism. Bioavailability of a suspension formulation in rats was less than 1%, but increased to approximately 9% when administered as a 20% soybean oil-in-water emulsion. The emulsion formulation and three additional lipid-based formulations were administered by gavage to conscious, minimally restrained rats in a novel, double-cannulated model to determine the effects of formulation on systemic blood absorption and mesenteric lymph transport of ontazolast. The bioavailability of ontazolast was significantly and substantially enhanced by all of the lipid-based formulations. While these formulations also significantly increased the amount of ontazolast transported by the lymph, the total amounts transported were insufficient to account for the improvement in bioavailability, which may be due to the elimination or reduction of the barriers of poor aqueous solubility and slow dissolution to absorption of ontazolast from the gastrointestinal tract, or the effects of lipid on the gastrointestinal membrane permeability, transit time, or metabolism of ontazolast. Semisolid SEDDS formulations, composed of Peceol and Gelucire 44/14, produced bioavailability similar to the emulsion formulation. The total amount of ontazolast transported by the lymph varied directly with the amount of concurrent triglyceride transport and appeared to be favored by formulations that prolong gastric emptying time or promote rapid absorption of ontazolast from the gastrointestinal tract.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
Statistical Estimates and Transformed Beta-Variables.
Minton, P. D., & Blom, G. (1960) · The American Mathematical Monthly · doi:10.2307/2308690 · Cited by 1,166
Lipid Digestion and Absorption
Carey, M. C., Small, D. M., & Bliss, C. M. (1983) · Annual Review of Physiology · doi:10.1146/annurev.ph.45.030183.003251 · Cited by 874
Shah, N. H., Carvajal, M. T., Patel, C. I., Infeld, M. H., & Malick, A. W. (1994) · International Journal of Pharmaceutics · doi:10.1016/0378-5173(94)90271-2 · Cited by 481
Estimating the Maximal Potential for Intestinal Lymphatic Transport of Lipophilic Drug Molecules
Charman, W. N. A., & Stella, V. J. (1986) · International Journal of Pharmaceutics · doi:10.1016/0378-5173(86)90027-x · Cited by 217
Statistical Estimates and Transformed Beta-Variables.
David, F. N., & Blom, G. (1960) · Biometrika · doi:10.2307/2332984 · Cited by 127
In Vitro Model for Ciclosporin Intestinal Absorption in Lipid Vehicles
Reymond, J.-P., & Sucker, H. (1988) · Pharmaceutical Research · doi:10.1023/a:1015987223407 · Cited by 85
In Vivo Model for Ciclosporin Intestinal Absorption in Lipid Vehicles
Reymond, J.-P., Sucker, H., & Vonderscher, J. (1988) · Pharmaceutical Research · doi:10.1023/a:1015939307478 · Cited by 47
Chronic Collection of Mesenteric Lymph From Conscious, Tethered Rats.
Hauss, D. J., Fogal, S. E., & FICORILLI, J. V. (1998) · PubMed · Cited by 24
Self-citation
Cited by
Lipids and Lipid-Based Formulations: Optimizing the Oral Delivery of Lipophilic Drugs
Porter, C. J. H., Trevaskis, N. L., & Charman, W. N. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2197 · Cited by 1,824
Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs
Neslihan Gursoy, R., & Benita, S. (2004) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2004.02.001 · Cited by 1,358
Self-Nanoemulsifying Drug Delivery Systems: Formulation Insights, Applications and Advances
Date, A. A., Desai, N., Dixit, R., & Nagarsenker, M. (2010) · Nanomedicine · doi:10.2217/nnm.10.126 · Cited by 498
Oral lipid-based drug delivery systems – an overview
Kalepu, S., Manthina, M., & Padavala, V. (2013) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2013.10.001 · Cited by 494
Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs
Gershanik, T. (2000) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/s0939-6411(00)00089-8 · Cited by 477
Lipid-Based Delivery Systems and Intestinal Lymphatic Drug Transport: A Mechanistic Update
Trevaskis, N. L., Charman, W. N., & Porter, C. J. H. (2008) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.09.007 · Cited by 442
50 years of oral lipid-based formulations: provenance, progress and future perspectives
Feeney, O. M., Crum, M. F., McEvoy, C. L., Trevaskis, N. L., Williams, H. D., Pouton, C. W., Charman, W. N., Bergström, C. A. S., & Porter, C. J. H. (2016) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2016.04.007 · Cited by 426
Stable drug encapsulation in micelles and microemulsions
NARANG, A., DELMARRE, D., & GAO, D. (2007) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2007.08.057 · Cited by 419
Self-emulsifying drug delivery systems: an approach to enhance oral bioavailability
Kohli, K., Chopra, S., Dhar, D., Arora, S., & Khar, R. K. (2010) · Drug Discovery Today · doi:10.1016/j.drudis.2010.08.007 · Cited by 411
Development of solid self-emulsifying drug delivery systems: preparation techniques and dosage forms
Tang, B., Cheng, G., Gu, J.-C., & Xu, C.-H. (2008) · Drug Discovery Today · doi:10.1016/j.drudis.2008.04.006 · Cited by 393
Approaches for the development of solid and semi-solid lipid-based formulations
Jannin, V., Musakhanian, J., & Marchaud, D. (2008) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.09.006 · Cited by 388
Phospholipids and Lipid-Based Formulations in Oral Drug Delivery
Fricker, G., Kromp, T., Wendel, A., Blume, A., Zirkel, J., Rebmann, H., Setzer, C., Quinkert, R.-O., Martin, F., & Müller-Goymann, C. (2010) · Pharmaceutical Research · doi:10.1007/s11095-010-0130-x · Cited by 326
Intestinal lymphatic transport for drug delivery
Yáñez, J. A., Wang, S. W. J., Knemeyer, I. W., Wirth, M. A., & Alton, K. B. (2011) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2011.05.019 · Cited by 278
Overcoming poor oral bioavailability using nanoparticle formulations – opportunities and limitations
Desai, P. P., Date, A. A., & Patravale, V. B. (2012) · Drug Discovery Today: Technologies · doi:10.1016/j.ddtec.2011.12.001 · Cited by 199
Iwanaga, K., Kushibiki, T., Miyazaki, M., & Kakemi, M. (2006) · Biological and Pharmaceutical Bulletin · doi:10.1248/bpb.29.508 · Cited by 38
Metadata
- Authors
- Hauss, D. J., Fogal, S. E., Ficorilli, J. V., Price, C. A., Roy, T., Jayaraj, A. A., & Keirns, J. J.
- Venue
- Journal of Pharmaceutical Sciences
- Publisher
- American Geophysical Union (AGU)
- Published
- 1998-02
- Volume
- 87
- Issue
- 2
- Pages
- 164-169
- ISSN
- 0022-3549 (ISSN-L)
- OpenAlex
- W2159713677
- Cited by
- 316
- References
- 8
- FWCI
- 5.26
- Type
- journal article
- Language
- en
- Open access
- closed
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
