Nanolipidic particles improve the bioavailability and α-secretase inducing ability of epigallocatechin-3-gallate (EGCG) for the treatment of Alzheimer's disease
Open accessAbstract
Prevention of amyloidogenic processing of amyloid precursor protein with the use of natural phytochemicals capable of enhancing alpha-secretase activity may be a therapeutic approach for treatment of neurodegenerative diseases including Alzheimer's disease (AD) and HIV-associated dementia (HAD). We have recently shown promising preclinical results with the use of green tea polyphenol, (-)-epigallocatechin-3-gallate (EGCG) in mouse models of both diseases, however the translation into clinical use has been problematic primarily as a result of poor bioavailability and inefficient delivery to the central nervous system (CNS). While the antioxidant properties of EGCG are well known, we have shown that it is able to promote non-amyloidogenic processing of amyloid precursor protein (APP) by upregulating alpha-secretase, thus preventing brain beta amyloid plaque formation, a hallmark of AD pathology and common finding in HIV infection. In this preliminary study, we investigated the ability of one preformulation method to improve the oral bioavailability of EGCG. We found that forming nanolipidic EGCG particles improves the neuronal (SweAPP N2a cells) alpha-secretase enhancing ability in vitro by up to 91% (P<001) and it's oral bioavailability in vivo by more than two-fold over free EGCG.
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Nanolipid epigallocatechin-3-gallate particles increase epigallocatechin-3-gallate's oral bioavailability by greater than two-fold.
“One notable example has been that of nanolipid epigallocatechin-3-gallate particles, which have demonstrated the ability to increase α-secretase, enhancing their ability in vitro and increasing epigallocatechin-3-gallate’s oral bioavailability by greater than two-fold [206].”
From The Multifaceted Role of Neuroprotective Plants in Alzheimer’s Disease Treatment (2022) · cites this paper as [206]
Nanolipid epigallocatechin-3-gallate particles have demonstrated the ability to increase α-secretase.
“One notable example has been that of nanolipid epigallocatechin-3-gallate particles, which have demonstrated the ability to increase α-secretase, enhancing their ability in vitro and increasing epigallocatechin-3-gallate’s oral bioavailability by greater than two-fold [206].”
From The Multifaceted Role of Neuroprotective Plants in Alzheimer’s Disease Treatment (2022) · cites this paper as [206]
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Cites
Maeda, H. (2001) · Advances in Enzyme Regulation · doi:10.1016/s0065-2571(00)00013-3 · Cited by 2,495 · see citing works
Solid lipid nanoparticles for parenteral drug delivery
Wissing, S. A., Kayser, O., & Müller, R. H. (2004) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2003.12.002 · Cited by 1,494 · see citing works
Rezai-Zadeh, K., Shytle, D., Sun, N., Mori, T., Hou, H., Jeanniton, D., Ehrhart, J., Townsend, K., Zeng, J., Morgan, D., et al. (2005) · The Journal of Neuroscience · doi:10.1523/jneurosci.1521-05.2005 · Cited by 713 · see citing works
Self-citationLipid nanocapsules: A new platform for nanomedicine
Huynh, N. T., Passirani, C., Saulnier, P., & Benoît, J. (2009) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2009.04.026 · Cited by 596 · see citing works
Chow, H. ‐. S., Cai, Y., Alberts, D. S., Hakim, I. A., Dorr, R. T., Shahi, F., Crowell, J. A., Yang, C. S., & Hara, Y. (2001) · PubMed · Cited by 419 · see citing works
Siddiqui, I. A., Adhami, V. M., Bharali, D. J., et al. (2009) · Cancer Research · doi:10.1158/0008-5472.can-08-3978 · Cited by 378 · see citing works
Lambert, J. D., Lee, M., Lu, H., Meng, X., Hong, J. J. J., Seril, D. N., Yang, C. S., & Sturgill, M. G. (2003) · Journal of Nutrition · doi:10.1093/jn/133.12.4172 · Cited by 318 · see citing works
Yokoyama, M. (1998) · Journal of Controlled Release · doi:10.1016/s0168-3659(97)00115-6 · Cited by 308 · see citing works
Metabolism of Green Tea Catechins: An Overview
Feng, W. Y. (2006) · Current Drug Metabolism · doi:10.2174/138920006778520552 · Cited by 301 · see citing works
A Single Ascending Dose Study of Epigallocatechin Gallate in Healthy Volunteers
Ullmann, U., Haller, J., Decourt, J., Girault, N., Girault, J., Richard-Caudron, A., Pineau, B., & Weber, P. (2003) · Journal of International Medical Research · doi:10.1177/147323000303100205 · Cited by 299 · see citing works
Allen, T. M. (1998) · Drugs · doi:10.2165/00003495-199856050-00001 · Cited by 285 · see citing works
Polymer micelles with cross-linked polyanion core for delivery of a cationic drug doxorubicin
Kim, J. O., Kabanov, A. V., & Bronich, T. K. (2009) · Journal of Controlled Release · doi:10.1016/j.jconrel.2009.04.019 · Cited by 255 · see citing works
Piperine Enhances the Bioavailability of the Tea Polyphenol (−)-Epigallocatechin-3-gallate in Mice
Lambert, J. D., Hong, J., Kim, D. H., Mishin, V. M., & Yang, C. S. (2004) · Journal of Nutrition · doi:10.1093/jn/134.8.1948 · Cited by 245 · see citing works
Burns, A. S., & Iliffe, S. (2009) · BMJ · doi:10.1136/bmj.b75 · Cited by 230 · see citing works
Cerebral pattern of pro- and anti-inflammatory cytokines in dementias
Tarkowski, E., Liljeroth, A.-M., Minthon, L., Tarkowski, A., Wallin, A., & Blennow, K. (2003) · Brain Research Bulletin · doi:10.1016/s0361-9230(03)00088-1 · Cited by 219 · see citing works
Khajuria, A., Thusu, N., & Zutshi, U. (2002) · Phytomedicine · doi:10.1078/0944-7113-00114 · Cited by 219 · see citing works
HIV-1 associated dementia: symptoms and causes
Ghafouri, M., Amini, S., Khalili, K., & Sawaya, B. E. (2006) · Retrovirology · doi:10.1186/1742-4690-3-28 · Cited by 215 · see citing works
Kumar, V. V., Durairaj, C., Sistla, R., Veerabrahma, K., Rao, Y. M., & Diwan, P. V. (2006) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2006.11.004 · Cited by 213 · see citing works
Lin, L.-C., Wang, M.-N., Tseng, T.-Y., Sung, & Tsai, T. (2007) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf062816a · Cited by 211 · see citing works
Obregon, D. F., Rezai-Zadeh, K. P., Bai, Y., Sun, N., Hou, H., Ehrhart, J. C., Zeng, J., Mori, T., Arendash, G. W., Shytle, D., et al. (2006) · Journal of Biological Chemistry · doi:10.1074/jbc.m600617200 · Cited by 210 · see citing works
Self-citationBano, G., Raina, R. K., Zutshi, U., Bedi, K. L., Johri, R. K., & Sharma, S. (1991) · European Journal of Clinical Pharmacology · doi:10.1007/bf00314996 · Cited by 208 · see citing works
Polymer micelles with cross-linked ionic cores for delivery of anticancer drugs
Bontha, S., Kabanov, A. V., & Bronich, T. K. (2006) · Journal of Controlled Release · doi:10.1016/j.jconrel.2006.06.015 · Cited by 196 · see citing works
Nano-encapsulation of azole antifungals: Potential applications to improve oral drug delivery
Pandey, R., Ahmad, Z., Sharma, S., & Khuller, G. K. (2005) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2005.05.027 · Cited by 193 · see citing works
Zhang, L., Zheng, Y., Chow, M. S. S., & Zuo, Z. (2004) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2004.08.020 · Cited by 189 · see citing works
Lambert, J. D., Sang, S., Hong, J., Kwon, S.-J., Lee, M., Ho, C., & Yang, C. S. (2006) · Drug Metabolism and Disposition · doi:10.1124/dmd.106.011460 · Cited by 165 · see citing works
Tian, Y., Bromberg, L. E., Lin, S. N., Hatton, T. A., & Tam, K. C. (2007) · Journal of Controlled Release · doi:10.1016/j.jconrel.2007.05.010 · Cited by 163 · see citing works
Flavonoid‐mediated presenilin‐1 phosphorylation reduces Alzheimer's disease β‐amyloid production
Rezai-Zadeh, K. P., Shytle, R. D., Bai, Y., Tian, J., Hou, H., Mori, T., Zeng, J., Obregon, D. F., Town, T., & Tan, J. (2008) · Journal of Cellular and Molecular Medicine · doi:10.1111/j.1582-4934.2008.00344.x · Cited by 153 · see citing works
Self-citationLambert, J. D., Lee, M., Diamond, L., et al. (2005) · Drug Metabolism and Disposition · doi:10.1124/dmd.104.003434 · Cited by 146 · see citing works
Formulation of Drugs in Block Copolymer Micelles: Drug Loading and Release
Liu, J. J., Lee, H., & Allen, C. J. (2006) · Current Pharmaceutical Design · doi:10.2174/138161206779026263 · Cited by 143 · see citing works
Self-nanoemulsifying drug delivery system (SNEDDS) for oral delivery of protein drugs
Rao, S. V. R., Yajurvedi, K., & Shao, J. (2008) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2008.05.015 · Cited by 122 · see citing works
Ullmann, Haller, Decourt, et al. (2004) · International Journal for Vitamin and Nutrition Research · doi:10.1024/0300-9831.74.4.269 · Cited by 115 · see citing works
Cai, Y., Anavy, N. D., & Chow, H. ‐. S. (2002) · Drug Metabolism and Disposition · doi:10.1124/dmd.30.11.1246 · Cited by 115 · see citing works
Wang, Y. (2004) · Journal of Chromatography B · doi:10.1016/j.jchromb.2004.05.006 · Cited by 112 · see citing works
Effect of piperine on the steady‐state pharmacokinetics of phenytoin in patients with epilepsy
Pattanaik, S., Hota, D., Prabhakar, S. K., et al. (2006) · Phytotherapy Research · doi:10.1002/ptr.1937 · Cited by 109 · see citing works
Influence of piperine on rifampicin blood levels in patients of pulmonary tuberculosis.
Rk, Z., Singh, R., Zutshi, U., et al. (1985) · PubMed · Cited by 103 · see citing works
Nongallated Compared with Gallated Flavan-3-ols in Green and Black Tea Are More Bioavailable
Henning, S. M., Choo, J. J., & Heber, D. (2008) · Journal of Nutrition · doi:10.1093/jn/138.8.1529s · Cited by 98 · see citing works
Microglial cells in neurodegenerative disorders.
Wojtera, M., Sikorska, B., Sobów, T., & Liberski, P. P. (2005) · PubMed · Cited by 77 · see citing works
Giunta, B. N., Obregon, D. F., Hou, H., Zeng, J., Sun, N., Nikolic, V., Ehrhart, J. C., Shytle, R. D., Fernandez, F., & Tan, J. (2006) · Brain Research · doi:10.1016/j.brainres.2006.09.057 · Cited by 75 · see citing works
Self-citationBailey, A. R., Giunta, B. N., Obregon, D. F., Nikolic, W. V., Tian, J., Sanberg, C. D., Sutton, D. T., & Tan, J. (2008) · PubMed Central · Cited by 74 · see citing works
Self-citationImproved bioavailability of orally administered mifepristone from PLGA nanoparticles
HE, W., HORN, S., & HUSSAIN, M. (2006) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2006.10.025 · Cited by 67 · see citing works
Wang, M., & Miksa, I. R. (2007) · Journal of Chromatography B · doi:10.1016/j.jchromb.2007.06.037 · Cited by 65 · see citing works
The coming problem of HIV-associated Alzheimer’s disease
Alisky, J. M. (2007) · Medical Hypotheses · doi:10.1016/j.mehy.2007.02.030 · Cited by 56 · see citing works
Intestinal efflux transport kinetics of green tea catechins in Caco-2 monolayer model
Chan, K. Y., Zhang, L., & Zuo, Z. (2007) · Journal of Pharmacy and Pharmacology · doi:10.1211/jpp.59.3.0009 · Cited by 52 · see citing works
Meeuwsen, E. J., Melis, R. J. F., Adang, E., Golüke-Willemse, G. A., Krabbe, P. F. M., de Leest, B. J., van Raak, F. H. J. M., Schölzel-Dorenbos, C. J. M., Visser, M. C., Wolfs, C. A. G., et al. (2009) · The journal of nutrition health & aging · doi:10.1007/s12603-009-0066-1 · Cited by 43 · see citing works
Italia, J. L., Datta, P., Ankola, D. D., et al. (2008) · Journal of Biomedical Nanotechnology · doi:10.1166/jbn.2008.341 · Cited by 41 · see citing works
HIV-1 TAT inhibits microglial phagocytosis of Abeta peptide.
(2008) · PubMed Central · Cited by 37 · see citing works
Liposome targeting to rat brain: effect of osmotic opening of the blood-brain barrier
Sakamoto, A., & Ido, T. (1993) · Brain Research · doi:10.1016/0006-8993(93)90499-d · Cited by 36 · see citing works
Enhanced oral delivery of antimony from meglumine antimoniate/β-cyclodextrin nanoassemblies
Frézard, F., Martins, P. S., Bahia, A. P. C. O., et al. (2007) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2007.06.029 · Cited by 35 · see citing works
Bruce, J. E., Anderson, G., Lin, C.-Y., Gorshkov, M. V., Rockwood, A. L., & Smith, R. D. (2000) · Journal of Mass Spectrometry · doi:10.1002/(sici)1096-9888(200001)35:1 · Cited by 31 · see citing works
Sparidans, R. W., Lagas, J. S., Schinkel, A. H., et al. (2007) · Journal of Chromatography B · doi:10.1016/j.jchromb.2007.05.008 · Cited by 16 · see citing works
Flagged first, then by citations
Research works printed but not linked: 2
- [5]Burns A Iliffe S Dementia BMJ 2009 338 b75 19196746
- [25]Wang Z Hop CE Leung KH Pang J Determination of in vitro permeability of drug candidates through a caco-2 cell monolayer by liquid chromatography/tandem mass spectrometry J Mass Spectrom 2000 1 35 1 71 6 10633236
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Neuroprotective Natural Products for Alzheimer’s Disease
Chen, X., Drew, J., Berney, W., & Lei, W. (2021) · Cells · doi:10.3390/cells10061309 · Cited by 236 · see citing works
Neurotherapeutic applications of nanoparticles in Alzheimer’s disease
Sahni, J. K., Doggui, S., Ali, J., Baboota, S., Dao, L., & Ramassamy, C. (2011) · Journal of Controlled Release · doi:10.1016/j.jconrel.2010.11.033 · Cited by 219 · see citing works
Agis-Torres, A., Sollhuber, M., Fernandez, M., & Sanchez-Montero, J. M. (2014) · Current Neuropharmacology · doi:10.2174/1570159x113116660047 · Cited by 202 · see citing works
Rahman, M. H., Bajgai, J., Fadriquela, A., Sharma, S., Trinh, T. T., Akter, R., Jeong, Y. J., Goh, S. H., Kim, C.-S., & Lee, K.-J. (2021) · Molecules · doi:10.3390/molecules26175327 · Cited by 182 · see citing works
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Henríquez, G., Gomez, A., Guerrero, E., & Narayan, M. (2020) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.0c00381 · Cited by 83 · see citing works
Zhang, S., Zhu, Q., Chen, J.-Y., OuYang, D., & Lu, J.-H. (2020) · Phytomedicine · doi:10.1016/j.phymed.2020.153316 · Cited by 74 · see citing works
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“One notable example has been that of nanolipid epigallocatechin-3-gallate particles, which have demonstrated the ability to increase α-secretase, enhancing their ability in vitro and increasing epigallocatechin-3gallate’s oral bioavailability by greater than two-fold [206].”
Background
- Authors
- Smith, A., Giunta, B., Bickford, P. C., Fountain, M., Tan, J., & Shytle, R. D.
- Affiliations
- University of South Florida (US)
- United States Department of Veterans Affairs (US)
- Corresponding author
- Tan, Jun
- Shytle, R. Douglas
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2010-04
- Volume
- 389
- Issue
- 1-2
- Pages
- 207-212
- ISSN
- 0378-5173 (ISSN-L)
- PMC
- PMC5831366
- OpenAlex
- W2092057906
- Cited by
- 280
- References
- 50
- Citations by year
- 2026: 3 · 2025: 14 · 2024: 25 · 2023: 19 · 2022: 18 · 2021: 20 · 2020: 25 · 2019: 19 · 2018: 23 · 2017: 15 · 2016: 12 · 2015: 13 · 2014: 14 · 2013: 19 · 2012: 18
- FWCI
- 13.21
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institute on Aging (R21AG031037, R01AG032432)
- National Institute of Mental Health (R01MH098737, K08MH082642)
- National Center for Complementary and Integrative Health (R43AT004871)
- Topics
- Health Sciences › Medicine › Pathology and Forensic Medicine › Tea Polyphenols and Effects
- Health Sciences › Medicine › Physiology › Alzheimer's disease research and treatments
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- epigallocatechin gallate, Alzheimer's disease, HIV-associated dementia, alpha-secretase, amyloid precursor protein, oral bioavailability, green tea polyphenols, amyloid plaques, brain drug delivery, preformulation
- MeSH terms
- Alzheimer Disease, Animals, Biological Availability, Catechin, Enzyme Induction, Humans, Lipids, Male, Neurons, Rats, Sprague-Dawley, Neuroprotective Agents, Cell Line, Tumor, Mice, Rats, Nanoparticles, Amyloid Precursor Protein Secretases
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