Dean and Professor of College of Pharmacy, Ajou University, Korea

Beom-Jin Lee is the Dean of, and full professor in the College of Pharmacy, Ajou University. He was awarded his BSc and MSc from the College of Pharmacy, Seoul National University, Republic of Korea, and his PhD from the College of Pharmacy, Oregon State University, Corvallis, USA. His research interests include pharmaceutical sciences and drug development focusing on the “i) Controlled bioavailability of poorly soluble and poorly absorbable drugs; ii) Solubilization, formulation and development of patient-centered drug delivery system; iii) Advanced nano-based delivery systems using fattigation (fatty acid conjugation) and click chemistry in a biomimetic condition, iv) Narcotic issues and abuse-deterrent system, v) Pharmacy practice and outcome based education system”. He has authored 200 peer-reviewed papers, 28 book chapters, and numerous oral and poster presentations. He has received more than 35 outstanding achievement awards from government and other organizations. He is currently president of the Asian Association of Schools of Pharmacy (AASP) and Immediate President of Korean Society of Pharmaceutical Science and Technology (KSPST), and Academic Institution Members (AIM) advisory committee and a delegate of the International Pharmaceutical Federation (FIP). He also serves as an editorial board member of several peer-reviewed journals.


Fattigation strategy and improved drug delivery via conjugation of peptide drug with fatty acids by forming self-assembled nanoparticles

Beom-Jin Leea, Hai V. Ngoa

aCollege of Pharmacy, Ajou University, Suwon 16499, Republic of Korea

A synthetic peptide analog (LEU) has been used as first-line treatment of advanced prostate cancer. However, the short half-life and low druggability of LEU was limited due to the action of proteolytic enzymes, resulting in its effectiveness and long-acting performance for the cancer treatment. To improve its drug delivery potentials, LEU conjugates with different chain lengths of saturated fatty acids (lauric acid; C12, palmitic acid; C16 and stearic acid, C18) as a novel self-assembled biomedicine. The physicochemical properties of LFNs, such as particle size (~100 nm), surface charge (positively charged), and morphology, were characterized. The degradation kinetics of LFC solutions against human plasma at 37 °C were determined, showing that the conjugate of LEU with shortest chain length (LLC, C12) was rapidly converted to active LEU, with 95.5 ± 6.1% within 21 days. LEU-palmitic acid conjugate (LPC, C16) and LEU-stearic acid conjugate (LSC, C18) were converted 92.4 ± 6.5% and 90.7 ± 7.7% within 21 and 28 days, respectively, to the active LEU. Interestingly, all LFNs showed a superior direct antiproliferative effect on prostate cancer cells (PC3, an androgen-insensitive cell line) in the following order: LSNs (98.9%) > LPNs (86.7%) > LLNs (75.0%) > LEU (8.9%) after repeated daily of the same dose strength of LEU for 4 days. Furthermore, the three-dimensional (3D) spheroid invasion study indicates that all LFNs with a one-time treatment performed a long-acting inhibitory effect on tumor growth by preventing cancer cells invading from the spheroid body and promoting cell death inside the spheroid, as compared to in LEU with a one-time or daily treatment after 7 days. In conclusion, the conjugation of LEU with different chain length of FAs could provide a novel and long-acting strategy by exerting a direct inhibitory effect in addition to the GnRH-triggered effect for the treatment of several hormone-responsive tumor systems using therapeutic peptides. Supported by a grant from the National Research Foundation of Korea (NRF) funded by the Ministry of Science and ICT (2020R1A2C2008307) and the Korea Evaluation Institute of Industrial Technology (KEIT) funded by the Ministry of Trade, Industry and Energy, Republic of Korea (20008840), Republic of Korea.

Keywords: peptide drug, fattigation, drug-fatty acid conjugate, self-assembled nanoparticles, enhanced permeability, improved drug delivery, cancer targeting

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