Title |
Liposome-mediated delivery of the p21 activated kinase-1 (PAK-1) inhibitor IPA-3 limits prostate tumor growth in vivo
|
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Published in |
Nanomedicine: Nanotechnology, Biology and Medicine, March 2016
|
DOI | 10.1016/j.nano.2016.01.003 |
Pubmed ID | |
Authors |
Ahmad Al-Azayzih, Wided N. Missaoui, Brian S. Cummings, Payaningal R. Somanath |
Abstract |
P21 activated kinases-1 (PAK-1)is implicated in various diseases. It is inhibited by thesmall molecule 'Inhibitor targeting PAK1 activation-3' (IPA-3), which is highly specific but metabolically unstable. To address this limitation we encapsulatedIPA-3 in sterically stabilized liposomes (SSL). SSL-IPA-3 averaged 139 nm in diameter,polydispersity index (PDI) of 0.05, and a zeta potential of -28.1, neither of which changed over 14 days; however, the PDI increased to 0.139. Analysis of liposomal IPA-3 levels demonstrated good stability, with 70% of IPA-3 remaining after 7 days. SSL-IPA-3 inhibited prostate cancer cell growth in vitro with comparable efficacy to free IPA-3. Excitingly, only a 2 day/week dose of SSL-IPA-3 was needed to inhibit the growth of prostate xenografts in vivo, while a similar dose of free IPA-3 was ineffective. These data demonstrate the development and clinical utility of a novel liposomal formulationfor the treatment of prostate cancer. |
X Demographics
Geographical breakdown
Country | Count | As % |
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Tunisia | 1 | 33% |
Unknown | 2 | 67% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 3 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Unknown | 26 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Ph. D. Student | 4 | 15% |
Student > Bachelor | 4 | 15% |
Professor > Associate Professor | 3 | 12% |
Professor | 3 | 12% |
Lecturer | 2 | 8% |
Other | 6 | 23% |
Unknown | 4 | 15% |
Readers by discipline | Count | As % |
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Pharmacology, Toxicology and Pharmaceutical Science | 6 | 23% |
Biochemistry, Genetics and Molecular Biology | 3 | 12% |
Medicine and Dentistry | 3 | 12% |
Chemistry | 2 | 8% |
Computer Science | 1 | 4% |
Other | 5 | 19% |
Unknown | 6 | 23% |