Review and analysis of FDA approved drugs using lipid-based formulations
Open accessAbstract
Lipid-based drug delivery systems (LBDDS) are one of the most studied bioavailability enhancement technologies and are utilized in a number of U.S. Food and Drug Administration (FDA) approved drugs. While researchers have used several general rules of thumb to predict which compounds are likely to benefit from LBDDS, formulation of lipid systems is primarily an empiric endeavor. One of the challenges is that these rules of thumb focus in different areas and are used independently of each other. The Developability Classification System attempts to link physicochemical characteristics with possible formulation strategies. Although it provides a starting point, the formulator still has to empirically develop the formulation. This article provides a review and quantitative analysis of the molecular properties of these approved drugs formulated as lipid systems and starts to build an approach that provides more directed guidance on which type of lipid system is likely to be the best for a particular drug molecule.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Lipid-based drug delivery systems improve oral absorption of poorly water-soluble drugs through mechanisms including increasing solubility, reducing food-induced exposure variability and improving overall intestinal uptake.
“With numerous commercial successes, lipid-based drug delivery systems (LBDDS) have a proven track record to improve oral absorption of poorly water-soluble drugs (PWSDs) through a variety of mechanisms including increasing solubility, reducing food-induced exposure variability and improving overall intestinal uptake (Savla et al., 2017).”
From Exploring impact of supersaturated lipid-based drug delivery systems of celecoxib on in vitro permeation across PermeapadⓇ membrane and in vivo absorption (2020) · cites this paper as Savla et al., 2017
Cites
Lipinski, C. A., Lombardo, F., Dominy, B. W., & Feeney, P. J. (2001) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(00)00129-0 · Cited by 18,139 · see citing works
Molecular properties that influence the oral bioavailability of drug candidates
Veber, D. F., Johnson, S. R., Cheng, H.-Y., Smith, B. R., Ward, K. W., & Kopple, K. D. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm020017n · Cited by 8,420 · see citing works
Amidon, G. L., Lennernäs, H., Shah, V. P., & Crison, J. R. (1995) · Pharmaceutical Research · doi:10.1023/a:1016212804288 · Cited by 5,430 · see citing works
DrugBank: a comprehensive resource for in silico drug discovery and exploration
Wishart, D. S. (2006) · Nucleic Acids Research · doi:10.1093/nar/gkj067 · Cited by 3,892 · see citing works
The influence of drug-like concepts on decision-making in medicinal chemistry
Leeson, P. D., & Springthorpe, B. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2445 · Cited by 2,403 · see citing works
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 · see citing works
Solubilizing Excipients in Oral and Injectable Formulations
Strickley, R. G. (2004) · Pharmaceutical Research · doi:10.1023/b:pham.0000016235.32639.23 · Cited by 1,417 · see citing works
Pouton, C. W. (2006) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2006.04.016 · Cited by 1,306 · see citing works
(2017) · Arzneimittelforschung · doi:10.1055/s-00000175 · Cited by 1,134 · see citing works
Pouton, C. W., & Porter, C. J. H. (2007) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.10.010 · Cited by 887 · see citing works
Hauss, D. J. (2007) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.05.006 · Cited by 597 · see citing works
Handbook of Aqueous Solubility Data
Yalkowsky, S. H. (2003) · CRC Press eBooks · doi:10.1201/9780203490396 · Cited by 586 · see citing works
Drug, Meal and Formulation Interactions Influencing Drug Absorption After Oral Administration
Fleisher, D., Li, C., Zhou, Y., Pao, L., & Karim, A. (1999) · Clinical Pharmacokinetics · doi:10.2165/00003088-199936030-00004 · Cited by 507 · see citing works
ChemMine tools: an online service for analyzing and clustering small molecules
Backman, T. W. H., Cao, Y., & Girke, T. (2011) · Nucleic Acids Research · doi:10.1093/nar/gkr320 · Cited by 502 · see citing works
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 · see citing works
Butler, J., & Dressman, J. (2010) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.22217 · Cited by 426 · see citing works
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 · see citing works
Wacher, V. J., Silverman, J. A., Zhang, Y., & Benet, L. Z. (1998) · Journal of Pharmaceutical Sciences · doi:10.1021/js980082d · Cited by 423 · see citing works
Martins, S., Sarmento, B. F. C. C., Ferreira, D., & Souto, E. B. (2007) · PubMed Central · Cited by 399 · see citing works
Dahan, A., & Hoffman, A. (2008) · Journal of Controlled Release · doi:10.1016/j.jconrel.2008.03.021 · Cited by 343 · see citing works
Lindmark, T., Kimura, Y., & Artursson, P. (1998) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)37216-7 · Cited by 333 · see citing works
Absorption Enhancers: Applications and Advances
Aungst, B. J. (2011) · The AAPS Journal · doi:10.1208/s12248-011-9307-4 · Cited by 309 · see citing works
Lemke, A., Kiderlen, A. F., & Kayser, O. (2005) · Applied Microbiology and Biotechnology · doi:10.1007/s00253-005-1955-9 · Cited by 307 · see citing works
Müllertz, A., Ogbonna, A., Ren, S., & Rades, T. (2010) · Journal of Pharmacy and Pharmacology · doi:10.1111/j.2042-7158.2010.01107.x · Cited by 295 · see citing works
Intestinal lymphatic transport for drug delivery
Yáñez, J. A., Wang, S. W. J., Knemeyer, I. W., Wirth, M., & Alton, K. B. (2011) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2011.05.019 · Cited by 280 · see citing works
Dahan, A., & Hoffman, A. (2007) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2007.01.017 · Cited by 232 · see citing works
Čerpnjak, K., Pobirk, A. Z., Gašperlin, M., & Vrečer, F. (2013) · Acta Pharmaceutica · doi:10.2478/acph-2013-0040 · Cited by 227 · see citing works
Unusual lipid structures selectively reduce the toxicity of amphotericin B.
Janoff, A. S., Boni, L. T., Popescu, M. C., Minchey, S. R., Cullis, P. R., Madden, T. D., Taraschi, T. F., Gruner, S. M., Shyamsunder, E., & Täte, M. W. (1988) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.85.16.6122 · Cited by 223 · see citing works
Influence of lipolysis on drug absorption from the gastro-intestinal tract
MacGregor, K. J., Embleton, J. K., Lacy, J. E., Perry, E., Solomon, L. J., Seager, H., & Pouton, C. W. (1997) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(96)00489-9 · Cited by 220 · see citing works
Porter, C. J. H., Kaukonen, A. M., Taillardat‐Bertschinger, A., Boyd, B. J., O'Connor, J. M., Edwards, G. A., & Charman, W. N. (2004) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.20039 · Cited by 216 · see citing works
Kahan, B. D., Dunn, J. L., Fitts, C. T., Buren, D. V., Wombolt, D. G., Pollak, R., Carson, R. W., Alexander, W. J., Choc, M. G., Wong, R., et al. (1995) · Transplantation · doi:10.1097/00007890-199502270-00011 · Cited by 215 · see citing works
Constantinides, P. P., & Wasan, K. M. (2006) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.20780 · Cited by 209 · see citing works
Self-citationHou, T., Zhang, W., Xia, K., Qiao, X. B., & Xu, X. J. (2004) · Journal of Chemical Information and Computer Sciences · doi:10.1021/ci049884m · Cited by 201 · see citing works
Computational prediction of formulation strategies for beyond-rule-of-5 compounds
Bergström, C. A. S., Charman, W. N., & Porter, C. J. H. (2016) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2016.02.005 · Cited by 190 · see citing works
Formulation of amphotericin B as nanosuspension for oral administration
Kayser, O. (2003) · International Journal of Pharmaceutics · doi:10.1016/s0378-5173(02)00686-5 · Cited by 187 · see citing works
Molecular inflation, attrition and the rule of five
Leeson, P. D. (2016) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2016.01.018 · Cited by 182 · see citing works
Saquinavir, an HIV Protease Inhibitor, Is Transported by P-Glycoprotein
Kim, A. E., Dintaman, J. M., Waddell, D. S., & Silverman, J. A. (1998) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)37742-0 · Cited by 177 · see citing works
Predicting Effect of Food on Extent of Drug Absorption Based on Physicochemical Properties
Gu, C., Li, H., Levons, J. K., Lentz, K. A., Gandhi, R. B., Raghavan, K. S., & Smith, R. L. (2007) · Pharmaceutical Research · doi:10.1007/s11095-007-9236-1 · Cited by 154 · see citing works
Soft Gelatin Capsules (Softgels)
Gullapalli, R. P. (2010) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.22151 · Cited by 149 · see citing works
In vivo evaluation of an oral self-microemulsifying drug delivery system (SMEDDS) for leuprorelin
Hintzen, F., Perera, G., Hauptstein, S., Muller, C. R., Laffleur, F., & Bernkop‐Schnürch, A. (2014) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2014.05.047 · Cited by 147 · see citing works
Perloff, M. D., Moltke, L. L., Marchand, J. E., & Greenblatt, D. J. (2001) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.1133 · Cited by 135 · see citing works
The emerging role of P-glycoprotein inhibitors in drug delivery: a patent review
Akhtar, N., Ahad, A., Khar, R. K., Jaggi, M., Aqil, M., Iqbal, Z., Ahmad, F. J., & Talegaonkar, S. (2011) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.2011.561784 · Cited by 133 · see citing works
Zgair, A., Wong, J. C. M., Lee, J. B., Mistry, J., Sivak, O., Wasan, K. M., Hennig, I. M., Barrett, D. A., Constantinescu, C. S., Fischer, P. M., et al. (2016) · Europe PMC (PubMed Central) · Cited by 130 · see citing works
Self-citationEfficacy of Orally Delivered Cochleates Containing Amphotericin B in a Murine Model of Aspergillosis
Delmas, G., Park, S., Chen, Z. W., Tan, F., Kashiwazaki, R., Zarif, L., & Perlin, D. S. (2002) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.46.8.2704-2707.2002 · Cited by 110 · see citing works
Yang, Z., Tan, Y., Chen, M., Dian, L., Shan, Z., Peng, X., & Wu, C. (2012) · AAPS PharmSciTech · doi:10.1208/s12249-012-9876-2 · Cited by 99 · see citing works
Does Lipid Emulsion Reduce Amphotericin B Nephrotoxicity? A Systematic Review and Meta-analysis
Mistro, S., Maciel, I. D. M., de Menezes, R. G., Maia, Z. P. G., Schooley, R. T., & Badaró, R. (2012) · Clinical Infectious Diseases · doi:10.1093/cid/cis290 · Cited by 92 · see citing works
Gershkovich, P., Wasan, E. K., Lin, M., Sivak, O., Leon, C. G., Clement, J. G., & Wasan, K. M. (2009) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dkp140 · Cited by 81 · see citing works
Self-citationKang, S. P., & Ratain, M. J. (2010) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-10-0663 · Cited by 79 · see citing works
Xu, P., Yang, Z., Chen, M., Yang, M., Chen, J., & Fang, W. (2014) · International Journal of Nanomedicine · doi:10.2147/ijn.s54967 · Cited by 79 · see citing works
Amphotericin B lipid soluble formulations versus amphotericin B in cancer patients with neutropenia
Johansen, H. K., & Gøtzsche, P. C. (2014) · Cochrane Database of Systematic Reviews · doi:10.1002/14651858.cd000969.pub2 · Cited by 77 · see citing works
Sachs‐Barrable, K., Lee, S. D., Wasan, E. K., Thornton, S. J., & Wasan, K. M. (2007) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.08.042 · Cited by 76 · see citing works
Self-citationAdkins, J. C., & Faulds, D. M. (1998) · Drugs · doi:10.2165/00003495-199855060-00015 · Cited by 74 · see citing works
Wasan, E. K., Gershkovich, P., Zhao, J., Zhu, X., Werbovetz, K. A., Tidwell, R. R., Clement, J. G., Thornton, S. J., & Wasan, K. M. (2010) · PLoS neglected tropical diseases · doi:10.1371/journal.pntd.0000913 · Cited by 63 · see citing works
Self-citationAgrawal, S., Giri, T. K., Tripathi, D. K., Ajazuddin, M., & Alexander, A. (2012) · American Journal of Drug Discovery and Development · doi:10.3923/ajdd.2012.143.183 · Cited by 63 · see citing works
Application of Lipid-Based Formulations in Drug Discovery
Chen, X., Gudmundsson, O. S., & Hageman, M. J. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm3006433 · Cited by 62 · see citing works
Drug permeability across a phospholipid vesicle-based barrier
Flaten, G. E., Luthman, K., Vasskog, T., & Brandl, M. (2008) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2008.04.001 · Cited by 59 · see citing works
Flushing Oral Oncology Drugs Down the Toilet
Ratain, M. J. (2011) · Journal of Clinical Oncology · doi:10.1200/jco.2011.37.1617 · Cited by 53 · see citing works
Effect of Polyoxyl 35 Castor Oil and Polysorbate 80 on the Intestinal Absorption of Digoxin in vitro
Cornaire, G., Woodley, J. F., Saivin, S., Legendre, J., Decourt, S., Cloarec, A., & Houin, G. (2011) · Arzneimittelforschung · doi:10.1055/s-0031-1300252 · Cited by 53 · see citing works
Currently Marketed Oral Lipid-Based Dosage Forms: Drug Products and Excipients
Strickley, R. G. (2007) · CRC Press eBooks · doi:10.3109/9781420017267-4 · Cited by 52 · see citing works
Katneni, K., Charman, S. A., & Porter, C. J. H. (2006) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.20779 · Cited by 49 · see citing works
Amphotericin B colloidal dispersion: an improved antifungal therapy
Guo, L. S. S. (2001) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(01)00104-1 · Cited by 49 · see citing works
Risovic, V., Boyd, M. C., Choo, E., & Wasan, K. M. (2003) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.47.10.3339-3342.2003 · Cited by 48 · see citing works
Self-citationSheu, M., Chen, Y., Su, C.-Y., Jhan, H.-J., & Ho, H.-O. (2015) · International Journal of Nanomedicine · doi:10.2147/ijn.s95194 · Cited by 40 · see citing works
Schmitt, C., Kaeser, B., Riek, M., Bech, N., & Kreuzer, C. (2010) · International Journal of Clinical Pharmacology and Therapeutics · doi:10.5414/cpp48192 · Cited by 38 · see citing works
Liu, D., Kobayashi, T., Russo, S. M., Li, F., Plevy, S. E., Gambling, T. M., Carson, J. L., & Mumper, R. J. (2012) · The AAPS Journal · doi:10.1208/s12248-012-9441-7 · Cited by 35 · see citing works
In vitro activity of amphotericin B cochleates against Leishmania chagasi
Sesana, A. M., Monti-Rocha, R., Vinhas, S. A., Morais, C. G., Dietze, R., & Lemos, E. M. (2011) · Memórias do Instituto Oswaldo Cruz · doi:10.1590/s0074-02762011000200022 · Cited by 33 · see citing works
Rao, S., Tan, A., Thomas, N., & Prestidge, C. A. (2014) · Journal of Controlled Release · doi:10.1016/j.jconrel.2014.05.013 · Cited by 33 · see citing works
Softgels: Consumer perceptions and market impact relative to other oral dosage forms
Jones, W. J., & Francis, J. J. (2000) · Advances in Therapy · doi:10.1007/bf02853160 · Cited by 28 · see citing works
Sivak, O., Gershkovich, P., Lin, M., Wasan, E. K., Zhao, J., Owen, D., Clement, J. G., & Wasan, K. M. (2011) · Lipids in Health and Disease · doi:10.1186/1476-511x-10-135 · Cited by 27 · see citing works
Self-citationPreliminary evaluation of a novel oral delivery system for rhPTH1-34: In vitro and in vivo
Guo, L., Erli, M., Zhao, H., Long, Y., Zheng, C., & Duan, M. (2011) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2011.08.029 · Cited by 24 · see citing works
Gershkovich, P., Wasan, E. K., Sivak, O., Li, R.-N., Zhu, X., Werbovetz, K. A., Tidwell, R. R., Clement, J. G., Thornton, S. J., & Wasan, K. M. (2009) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dkp465 · Cited by 23 · see citing works
Self-citationAmphotericin B cochleates: a vehicle for oral delivery.
Perlin, D. S. (2004) · PubMed · Cited by 18 · see citing works
Gupta, P. K., Jaiswal, A. K., Asthana, S., Venkatesh Teja, B., Shukla, P., Shukla, M., Sagar, N., Dube, A., Rath, S. K., & Mishra, P. R. (2015) · British Journal of Pharmacology · doi:10.1111/bph.13149 · Cited by 18 · see citing works
Risovic, V., Rosland, M., Sivak, O., Wasan, K. M., & Bartlett, K. H. (2007) · Drug Development and Industrial Pharmacy · doi:10.1080/03639040601077349 · Cited by 17 · see citing works
Self-citationMendez, R., Abboud, H. E., Burdick, J. F., Copley, B., Freeman, R. B., Batiuk, T. D., Cooney, G. F., & Barbeito, R. (1999) · Clinical Therapeutics · doi:10.1016/s0149-2918(00)88276-4 · Cited by 17 · see citing works
Flagged first, then by citations
Cited by
Sorted by citations
Advances in Oral Drug Delivery
Alqahtani, M. S., Kazi, M., Alsenaidy, M. A., & Ahmad, M. Z. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.618411 · Cited by 886 · see citing works
Azman, M., Sabri, A. H. B., Anjani, Q. K., Mustaffa, M. F., & Hamid, K. A. (2022) · Pharmaceuticals · doi:10.3390/ph15080975 · Cited by 255 · see citing works
Nguyen, T., Duong, V., & Maeng, H. (2021) · Pharmaceutics · doi:10.3390/pharmaceutics13071103 · Cited by 262 · see citing works
Gold Complexes in Anticancer Therapy: From New Design Principles to Particle‐Based Delivery Systems
Moreno‐Alcántar, G., Picchetti, P., & Casini, A. (2023) · Angewandte Chemie International Edition · doi:10.1002/anie.202218000 · Cited by 204 · see citing works
Pharmaceutical approaches for enhancing solubility and oral bioavailability of poorly soluble drugs
Nyamba, I., Sombié, C. B., Yabré, M., Zimé-Diawara, H., Yaméogo, J. B. G., Ouédraogo, S., Lechanteur, A., Semdé, R., & Évrard, B. (2024) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2024.114513 · Cited by 188 · see citing works
Ditzinger, F., Price, D. J., Ilie, A.-R., Koehl, N. J., Janković, S., Τσακιρίδου, Γ., Aleandri, S., Kalantzi, L., Holm, R., Nair, A., et al. (2018) · Journal of Pharmacy and Pharmacology · doi:10.1111/jphp.12984 · Cited by 144 · see citing works
A Recent Update: Solid Lipid Nanoparticles for Effective Drug Delivery
Pandey, S. S., Shaikh, F. I., Gupta, A. R., Tripathi, P., & Yadav, J. S. (2021) · Advanced Pharmaceutical Bulletin · doi:10.34172/apb.2022.007 · Cited by 109 · see citing works
Huang, Y., Yu, Q., Chen, Z., Wu, W., Zhu, Q., & Lü, Y. (2021) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2021.03.025 · Cited by 104 · see citing works
Trends in small molecule drug properties: A developability molecule assessment perspective
Agarwal, P., Huckle, J. E., Newman, J., & Reid, D. L. (2022) · Drug Discovery Today · doi:10.1016/j.drudis.2022.103366 · Cited by 96 · see citing works
Yadav, P., Rastogi, V., & Verma, A. K. (2020) · Future Journal of Pharmaceutical Sciences · doi:10.1186/s43094-020-00023-3 · Cited by 99 · see citing works
Salunke, S., O’Brien, F., Tan, D. C. T., Harris, D., Math, M.-C., Ariën, T., Klein, S., & Timpe, C. (2022) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2022.114507 · Cited by 93 · see citing works
Garner, L. C., Klenerman, P., & Provine, N. M. (2018) · Frontiers in Immunology · doi:10.3389/fimmu.2018.01478 · Cited by 88 · see citing works
Pharmacokinetic investigation of synthetic cannabidiol oral formulations in healthy volunteers
Izgelov, D., Davidson, E. M., Barasch, D., Regev, A., Domb, A. J., & Hoffman, A. (2020) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2020.06.021 · Cited by 88 · see citing works
Nyamba, I., Lechanteur, A., Semdé, R., & Évrard, B. (2020) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2020.11.004 · Cited by 88 · see citing works
Mehata, A. K., Setia, A., Vikas, Malik, A., Hassani, R., Dailah, H., Alhazmi, H., Albarraq, A. A., Mohan, S., & Muthu, M. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15030722 · Cited by 73 · see citing works
Lipid-Based Oral Formulation Strategies for Lipophilic Drugs
Patel, V., Lalani, R., Bardoliwala, D., Ghosh, S., & Misra, A. R. (2018) · AAPS PharmSciTech · doi:10.1208/s12249-018-1188-8 · Cited by 80 · see citing works
Stegemann, S., Moreton, C., Svanbäck, S., Box, K. J., Motte, G., & Paudel, A. (2022) · Drug Discovery Today · doi:10.1016/j.drudis.2022.103344 · Cited by 81 · see citing works
Advances in delivery methods of Arthrospira platensis (spirulina) for enhanced therapeutic outcomes
ElFar, O. A., Billa, N., Lim, H. R., Chew, K. W., Cheah, W. Y., Munawaroh, H. S. H., Deepanraj, B., & Show, P. L. (2022) · Bioengineered · doi:10.1080/21655979.2022.2100863 · Cited by 84 · see citing works
Self-microemulsifying drug-delivery system: ongoing challenges and future ahead
Rajpoot, K., Tekade, M., Pandey, V., Sreeharsha, N., Youngren-Ortiz, S. R., & Tekade, R. K. (2019) · Elsevier eBooks · doi:10.1016/b978-0-12-814487-9.00009-0 · Cited by 76 · see citing works
Lipid–oligonucleotide conjugates for bioapplications
Li, X., Feng, K., Li, L., Yang, L., Pan, X., Yazd, H. S., Cui, C., Li, J., Moroz, L. L., Sun, Y., et al. (2020) · National Science Review · doi:10.1093/nsr/nwaa161 · Cited by 74 · see citing works
Gout therapeutics and drug delivery
Peng, X., Li, X., Xie, B., Lai, Y., Sosnik, A., Boucetta, H., Chen, Z., & He, W. (2023) · Journal of Controlled Release · doi:10.1016/j.jconrel.2023.09.011 · Cited by 75 · see citing works
Holm, R., Kuentz, M., Ilie, A.-R., & Griffin, B. T. (2023) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2023.106556 · Cited by 69 · see citing works
Lipid nanoparticles for enhancing oral bioavailability
Gangavarapu, A., Tapia-Lopez, L. V., Sarkar, B., Pena‐Zacarias, J., Badruddoza, A. Z. M., & Nurunnabi, M. (2024) · Nanoscale · doi:10.1039/d4nr01487a · Cited by 64 · see citing works
Hatton, G. B., Madla, C. M., Rabbie, S. C., & Basit, A. W. (2018) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2018.06.054 · Cited by 64 · see citing works
Engineering Biomaterials with Micro/Nanotechnologies for Cell Reprogramming
Fang, J., Hsueh, Y., Soto, J., Sun, W., Wang, J., Gu, Z., Khademhosseini, A., & Li, S. (2020) · ACS Nano · doi:10.1021/acsnano.9b04837 · Cited by 60 · see citing works
Innovations in Thermal Processing: Hot-Melt Extrusion and KinetiSol® Dispersing
Tan, D. K., Davis, D. A., Miller, D. A., Williams, R. O., & Nokhodchi, A. (2020) · AAPS PharmSciTech · doi:10.1208/s12249-020-01854-2 · Cited by 60 · see citing works
Holm, R. (2019) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2019.01.009 · Cited by 59 · see citing works
Al-Ali, A. A. A., Nielsen, R. B., Steffansen, B., Holm, R., & Nielsen, C. U. (2019) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2019.05.033 · Cited by 58 · see citing works
Ellenberger, D., Miller, D. A., & Williams, R. O. (2018) · AAPS PharmSciTech · doi:10.1208/s12249-018-1007-2 · Cited by 54 · see citing works
Silmore, L. H., Willmer, A. R., Capparelli, E. V., & Rosania, G. R. (2021) · Pharmacotherapy The Journal of Human Pharmacology and Drug Therapy · doi:10.1002/phar.2512 · Cited by 52 · see citing works
Bennett-Lenane, H., Griffin, B. T., & O’Shea, J. P. (2021) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2021.106018 · Cited by 51 · see citing works
Nanostructured lipid carrier potentiated oral delivery of raloxifene for breast cancer treatment
Soni, N. K., Sonali, L., Singh, A., Mangla, B., Neupane, Y. R., & Kohli, K. (2020) · Nanotechnology · doi:10.1088/1361-6528/abaf81 · Cited by 50 · see citing works
Thakur, S., Singh, A., Sharma, R., Aurora, R., & Jain, S. K. (2020) · Current Drug Metabolism · doi:10.2174/1389200221666201008143238 · Cited by 47 · see citing works
Bordes, C., Leguelinel, G., Lavigne, J.-P., Mauboussin, J. M., Laureillard, D., Faure, H., Rouanet, I., Sotto, A., & Loubet, P. (2020) · Clinical Microbiology and Infection · doi:10.1016/j.cmi.2020.04.019 · Cited by 47 · see citing works
Nano- and Microencapsulation - Techniques and Applications
Abu-Thabit, N. Y. (2020) · IntechOpen eBooks · doi:10.5772/intechopen.88590 · Cited by 46 · see citing works
de Oliveira, I. F., Barbosa, E. J., Peters, M. C. C., Henostroza, M. A. B., Yukuyama, M. N., Neto, E. D. S., Löbenberg, R., & Bou‐Chacra, N. A. (2020) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2020.119831 · Cited by 45 · see citing works
Rocha, S., Lucas, M., Ribeiro, D., Corvo, M. L., Fernandes, E. G. R., & Freitas, M. (2021) · Pharmacological Research · doi:10.1016/j.phrs.2021.105604 · Cited by 45 · see citing works
RNA Nanotechnology to Solubilize Hydrophobic Antitumor Drug for Targeted Delivery
Piao, X., Yin, H., Guo, S., Wang, H., & Guo, P. (2019) · Advanced Science · doi:10.1002/advs.201900951 · Cited by 44 · see citing works
Zidar, A., Kristl, J., Kocbek, P., & Zupančič, Š. (2021) · Expert Opinion on Drug Delivery · doi:10.1080/17425247.2021.1908260 · Cited by 44 · see citing works
Vasoya, J. M., Desai, H. H., Gumaste, S. G., Tillotson, J., Kelemen, D. W., Dalrymple, D. M., & Serajuddin, A. T. M. (2018) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2018.09.019 · Cited by 43 · see citing works
Sharma, T., Jain, A., Kaur, R., Saini, S., Katare, O. P., & Singh, B. (2020) · Drug Delivery and Translational Research · doi:10.1007/s13346-020-00772-x · Cited by 42 · see citing works
Abla, K. K., & Mehanna, M. M. (2023) · Journal of Controlled Release · doi:10.1016/j.jconrel.2023.08.018 · Cited by 41 · see citing works
Baghel, P., Roy, A. K., Verma, S., Satapathy, T., & Bahadur, S. (2020) · Future Journal of Pharmaceutical Sciences · doi:10.1186/s43094-020-00042-0 · Cited by 41 · see citing works
Kambayashi, A., Kiyota, T., Fujiwara, M., & Dressman, J. (2019) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2019.05.013 · Cited by 40 · see citing works
Alambiaga-Caravaca, A. M., Calatayud-Pascual, M. A., Rodilla, V., Concheiro, A., López-Castellano, A., & Alvarez-Lorenzo, C. (2020) · Pharmaceutics · doi:10.3390/pharmaceutics12080702 · Cited by 38 · see citing works
Bennett-Lenane, H., O’Shea, J. P., O’Driscoll, C. M., & Griffin, B. T. (2020) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2020.08.008 · Cited by 37 · see citing works
Ngwuluka, N. C., Abu-Thabit, N. Y., Uwaezuoke, O. J., Erebor, J. O., Ilomuanya, M. O., Mohamed, R. R., Soliman, S. M. A., Elella, M. H. A., & Ebrahim, N. A. A. (2021) · IntechOpen eBooks · doi:10.5772/intechopen.94856 · Cited by 37 · see citing works
Jadhav, A., & Nagaraj, K. (2025) · Pharmaceutics · doi:10.3390/pharmaceutics17060779 · Cited by 35 · see citing works
Lenkavská, L., Blaščáková, Ľ., Jurašeková, Z., Máčajová, M., Bilčı́k, B., Čavarga, I., Miškovský, P., & Huntošová, V. (2018) · Photodiagnosis and Photodynamic Therapy · doi:10.1016/j.pdpdt.2018.12.013 · Cited by 34 · see citing works
Dombach, J. L., Quintana, J. L. J., Nagy, T. A., Wan, C., Crooks, A. L., Yu, H., Su, C., Yu, E. W., Shen, J., & Detweiler, C. S. (2020) · PLoS Pathogens · doi:10.1371/journal.ppat.1009119 · Cited by 34 · see citing works
Ilie, A.-R., Griffin, B. T., Brandl, M., Bauer-Brandl, A., Jacobsen, A.-C., Vertzoni, M., Kuentz, M., Kolakovic, R., & Holm, R. (2020) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2020.105452 · Cited by 33 · see citing works
“excipients plus a co-solvent, it would be preferable to consider less complex LBDDS that can be rapidly screened in an industrial drug development setting (Holm, 2019; Savla et al., 2017; Müllertz et al., 2010).”
BackgroundKim, J. S., Park, H., Kang, K., Ha, E., Kim, M., & Hwang, S. (2022) · Journal of Pharmaceutical Investigation · doi:10.1007/s40005-022-00565-z · Cited by 33 · see citing works
Okonogi, S., Phumat, P., Khongkhunthian, S., Chaijareenont, P., Rades, T., & Müllertz, A. (2021) · Pharmaceutics · doi:10.3390/pharmaceutics13020167 · Cited by 32 · see citing works
Stengel, D., Demirel, B. H., Knoll, P., Truszkowska, M., Laffleur, F., & Bernkop‐Schnürch, A. (2023) · Journal of Colloid and Interface Science · doi:10.1016/j.jcis.2023.05.079 · Cited by 32 · see citing works
Polyphosphate coatings: A promising strategy to overcome the polycation dilemma
Le, N. N., Steinbring, C., Le‐Vinh, B., Jalil, A., Matuszczak, B., & Bernkop‐Schnürch, A. (2020) · Journal of Colloid and Interface Science · doi:10.1016/j.jcis.2020.12.019 · Cited by 32 · see citing works
Arbeiter, D., Reske, T., Teske, M., Bajer, D., Senz, V., Schmitz, K., Grabow, N., & Oschatz, S. (2021) · Polymers · doi:10.3390/polym13020292 · Cited by 31 · see citing works
Ilie, A.-R., Griffin, B. T., Kolakovic, R., Vertzoni, M., Kuentz, M., & Holm, R. (2020) · Drug Development and Industrial Pharmacy · doi:10.1080/03639045.2020.1721526 · Cited by 30 · see citing works
Shuddhodana, S., & Judeh, Z. M. A. (2019) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2019.04.020 · Cited by 29 · see citing works
Nanoparticle technologies: Recent state of the art and emerging opportunities
Parupudi, A., Mulagapati, S. H. R., & Subramony, J. A. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-820757-4.00009-0 · Cited by 31 · see citing works
Katdare, A., Thakkar, S., Dhepale, S., Khunt, D., & Misra, M. (2019) · Nutrition · doi:10.1016/j.nut.2019.03.008 · Cited by 29 · see citing works
Lee, Y.-C., Dalton, C. R., Regler, B. P., & Harris, D. (2018) · Drug Development and Industrial Pharmacy · doi:10.1080/03639045.2018.1483395 · Cited by 28 · see citing works
Desai, H. H., Bu, P., Shah, A. V., Cheng, X., & Serajuddin, A. T. M. (2020) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2020.01.031 · Cited by 28 · see citing works
Suitability of Artificial Membranes in Lipolysis-Permeation Assays of Oral Lipid-Based Formulations
Hedge, O. J., & Bergström, C. A. S. (2020) · Pharmaceutical Research · doi:10.1007/s11095-020-02833-9 · Cited by 28 · see citing works
Xiong, H., Liu, L., Wang, Y., Jiang, H., & Wang, X. (2021) · Small · doi:10.1002/smll.202104341 · Cited by 27 · see citing works
The structural fate of lipid nanoparticles in the extracellular matrix
Bandara, S. R., Molley, T. G., Kim, H., Bharath, P., Kilian, K. A., & Leal, C. (2019) · Materials Horizons · doi:10.1039/c9mh00835g · Cited by 27 · see citing works
Ahiwale, R. J., Bothiraja, C., & Pawar, A. (2020) · AAPS PharmSciTech · doi:10.1208/s12249-020-01801-1 · Cited by 26 · see citing works
Viglianisi, G., Santonocito, S., Lupi, S. M., Amato, M., Spagnuolo, G., Pesce, P., & Isola, G. (2023) · Therapeutic Advances in Chronic Disease · doi:10.1177/20406223231191043 · Cited by 26 · see citing works
Early evaluation of opportunities in oral delivery of PROTACs to overcome their molecular challenges
Yang, W., Saboo, S., Zhou, L., Askin, S., & Bak, A. (2023) · Drug Discovery Today · doi:10.1016/j.drudis.2023.103865 · Cited by 24 · see citing works
Fiolka, T., Αbeele, J. V. D., Augustijns, P., Arora, S., & Dressman, J. (2020) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2020.04.023 · Cited by 24 · see citing works
Satapathy, S. K., & Patro, C. S. (2021) · Advanced Pharmaceutical Bulletin · doi:10.34172/apb.2022.041 · Cited by 27 · see citing works
Praphanwittaya, P., Saokham, P., Jansook, P., & Loftsson, Þ. (2019) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2019.101462 · Cited by 24 · see citing works
Murakami, T., Bodor, E. T., & Bodor, N. S. (2023) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1080/17425255.2023.2203858 · Cited by 23 · see citing works
A recent update on therapeutic potential of vesicular system against fungal keratitis
Sanap, S. N., Kedar, A. S., Bisen, A. C., Agrawal, S., & Bhatta, R. S. (2022) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2022.103721 · Cited by 23 · see citing works
Guruge, A. G., Warren, D. B., Pouton, C. W., & Chalmers, D. K. (2023) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.3c00049 · Cited by 24 · see citing works
Lu, X., Fan, L., Song, C., Xu, Z., Hu, Y., & Guo, R. H. (2021) · Langmuir · doi:10.1021/acs.langmuir.1c00659 · Cited by 22 · see citing works
Koilpillai, J., & Narayanasamy, D. (2022) · Journal of Liposome Research · doi:10.1080/08982104.2022.2069809 · Cited by 22 · see citing works
Yang, L., Zhang, Y., Xie, J., Zhong, C., He, D., Wang, T., Li, K., Li, Y., Shi, D., Abagyan, R. A., et al. (2020) · Nanoscale · doi:10.1039/d0nr02651d · Cited by 22 · see citing works
A dataset of formulation compositions for self-emulsifying drug delivery systems
Zaslavsky, J., & Allen, C. J. (2023) · Scientific Data · doi:10.1038/s41597-023-02812-w · Cited by 22 · see citing works
Vincent, M., Simon, L., Brabet, P., Legrand, P., Dorandeu, C., Lai‐Kee‐Him, J., Durand, T., Crauste, C., & Bégu, S. (2022) · Pharmaceutics · doi:10.3390/pharmaceutics14051029 · Cited by 21 · see citing works
Effect of excipients on oral absorption process according to the different gastrointestinal segments
Ruiz-Picazo, A., Lozoya-Agulló, I., González‐Álvarez, I., Bermejo, M., & González‐Álvarez, M. (2020) · Expert Opinion on Drug Delivery · doi:10.1080/17425247.2020.1813108 · Cited by 22 · see citing works
Falavigna, M., Klitgaard, M., Berthelsen, R., Müllertz, A., & Flaten, G. E. (2020) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2020.08.026 · Cited by 21 · see citing works
Swarnakar, N. K., Venkatesan, N., & Betageri, G. V. (2018) · AAPS PharmSciTech · doi:10.1208/s12249-018-1239-1 · Cited by 20 · see citing works
Murakami, T., Bodor, E. T., & Bodor, N. S. (2021) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1080/17425255.2021.1902986 · Cited by 20 · see citing works
Interplay of lipid and surfactant: Impact on nanoparticle structure
Pink, D. L., Loruthai, O., Ziolek, R. M., Terry, A. E., Barlow, D. J., Lawrence, M. J., & Lorenz, C. D. (2021) · Journal of Colloid and Interface Science · doi:10.1016/j.jcis.2021.03.136 · Cited by 20 · see citing works
Nanostructured Lipid Carriers Can Enhance Oral Absorption of Khellin, a Natural Pleiotropic Molecule
Vanti, G., Muti, L., D’Ambrosio, M., Grifoni, L., Bergonzi, M. C., Luceri, C., & Bilia, A. R. (2021) · Molecules · doi:10.3390/molecules26247657 · Cited by 20 · see citing works
Sirvi, A., Debaje, S., Guleria, K., & Sangamwar, A. T. (2023) · Advances in Colloid and Interface Science · doi:10.1016/j.cis.2023.103028 · Cited by 20 · see citing works
Filament-based 3D-printing of placebo dosage forms using brittle lipid-based excipients
Abdelhamid, M., Koutsamanis, I., Corzo, C., Maisriemler, M., Ocampo, A. B., Slama, E., Alva, C., Lochmann, D., Reyer, S., Freichel, T., et al. (2022) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2022.122013 · Cited by 19 · see citing works
Aggarwal, K., Joshi, S., Jindal, P., Patel, P., & Kurmi, B. D. (2025) · AAPS PharmSciTech · doi:10.1208/s12249-025-03185-6 · Cited by 18 · see citing works
Almasri, R., Joyce, P., Schultz, H. B., Thomas, N., Bremmell, K. E., & Prestidge, C. A. (2020) · Pharmaceutics · doi:10.3390/pharmaceutics12070687 · Cited by 18 · see citing works
Jaromin, A., Parapini, S., Basilico, N., Zaremba-Czogalla, M., Lewińska, A., Zagórska, A., Walczak, M., Tyliszczak, B., Grzeszczak, A., Łukaszewicz, M., et al. (2020) · Bioactive Materials · doi:10.1016/j.bioactmat.2020.10.004 · Cited by 18 · see citing works
Stanczyk, F. Z., Matharu, H., & Winer, S. A. (2021) · Climacteric · doi:10.1080/13697137.2020.1862079 · Cited by 18 · see citing works
Gold Complexes in Anticancer Therapy: From New Design Principles to Particle‐Based Delivery Systems
Moreno‐Alcántar, G., Picchetti, P., & Casini, A. (2023) · Angewandte Chemie · doi:10.1002/ange.202218000 · Cited by 18 · see citing works
Multicomponent-Loaded Vesosomal Drug Carrier for Controlled and Sustained Compound Release
Lee, D., Song, S., Kim, S., Lee, M., Kim, E., Yoon, S., Kim, H., Son, S., Jung, H. S., Huh, Y. S., et al. (2023) · Biomacromolecules · doi:10.1021/acs.biomac.3c00528 · Cited by 17 · see citing works
Izgelov, D., Regev, A., Domb, A. J., & Hoffman, A. (2020) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.0c00141 · Cited by 18 · see citing works
Falavigna, M., Brurok, S., Klitgaard, M., & Flaten, G. E. (2021) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2021.120258 · Cited by 17 · see citing works
Zhang, H., Yao, J., Jiang, Q., Shi, Y.-R., Ge, W., & Xu, X. (2024) · Pharmaceutics · doi:10.3390/pharmaceutics16070935 · Cited by 16 · see citing works
Mechanisms of drug solubilization by polar lipids in biorelevant media
Katev, V., Vinarov, Z., & Tcholakova, S. S. (2021) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2021.105733 · Cited by 17 · see citing works
Lipid-based formulations of microemulsion-loaded oleogels for the oral delivery of carvedilol
Hamed, R., Seder, B. Y., Bardaweel, S. K., & Qawass, H. (2021) · Journal of Dispersion Science and Technology · doi:10.1080/01932691.2021.1964987 · Cited by 16 · see citing works
Low-surfactant microemulsion, a smart strategy intended for curcumin oral delivery
Dourado, D., de Oliveira, M. C., de Araújo, G. R. S., Amaral-Machado, L., Porto, D. L., Aragão, C. F. S., Alencar, É. D. N., & do Egito, E. S. T. (2022) · Colloids and Surfaces A Physicochemical and Engineering Aspects · doi:10.1016/j.colsurfa.2022.129720 · Cited by 15 · see citing works
Conjugates of amphotericin B to resolve challenges associated with its delivery
Jain, V. K., Jain, K., & Popli, H. (2024) · Expert Opinion on Drug Delivery · doi:10.1080/17425247.2024.2308073 · Cited by 15 · see citing works
- Authors
- Savla, R., Browne, J., Plassat, V., Wasan, K. M., & Wasan, E. K.
- Affiliations
- Catalent (United States) (US)
- Cerenis Therapeutics (France) (FR)
- University of Saskatchewan (CA)
- Corresponding author
- Savla, Ronak
- Venue
- Drug Development and Industrial Pharmacy
- Publisher
- Informa UK Limited
- Published
- 2017-07-06
- Volume
- 43
- Issue
- 11
- Pages
- 1743-1758
- ISSN
- 0363-9045 (ISSN-L)
- 1520-5762
- OpenAlex
- W2732877934
- Cited by
- 225
- References
- 75
- Citations by year
- 2026: 12 · 2025: 24 · 2024: 23 · 2023: 23 · 2022: 27 · 2021: 39 · 2020: 42 · 2019: 21 · 2018: 14
- FWCI
- 10.88
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Drug Development and Industrial Pharmacy (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- Figshare (submittedVersion, cc-by)
- Figshare (cc-by)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Keywords
- lipid-based drug delivery, bioavailability enhancement, FDA-approved drugs, physicochemical properties, molecular properties
- MeSH terms
- Biological Availability, Chemistry, Pharmaceutical, Humans, Lipids, United States, Drug Delivery Systems, Drug Approval
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