Fabrication of a Charge-Conversion Polymer—Liposome for Enhancing Endosomal Escape of Drug Delivery System for α−Mangostin

Trang Thi Kieu Phan; Hoang Huy Nguyen; Xuan Thi Nguyen; Tung Van Nguyen; Linh Anh Duong; Linh Phuong Nguyen; Uyen Thu Pham; Hong Nhung Le; Toan Quoc Tran; Duong Thanh Nguyen; Dung Thuy Nguyen Pham

LAPSE

Living Archive for Process Systems Engineering

LAPSE:2023.36703

Published Article

LAPSE:2023.36703

Fabrication of a Charge-Conversion Polymer—Liposome for Enhancing Endosomal Escape of Drug Delivery System for α−Mangostin

Trang Thi Kieu Phan, Hoang Huy Nguyen, Xuan Thi Nguyen, Tung Van Nguyen, Linh Anh Duong, Linh Phuong Nguyen, Uyen Thu Pham, Hong Nhung Le, Toan Quoc Tran, Duong Thanh Nguyen, Dung Thuy Nguyen Pham

September 20, 2023

α−Mangostin, which is a natural xanthone compound, inhibits the metastasis and survival of various cancer cell types. However, its therapeutic effectiveness is limited by low water solubility and very poor absorption. There are several studies that developed the drug delivery system for α−mangostin, but they are still a remaining challenge. Drug delivery techniques are severely hampered by the breakdown of nanoparticles inside endosomes. The abrasive chemical environment in these compartments causes both the nanoparticles and the encapsulated α−mangostin to degrade throughout the course of the voyage. Intracellular defenses against external materials refer to this collective mechanism. A pH-responsive liposome named PAsp(DET-Cit)−Toc, made of lipids and a charge-conversion polymer (CCP), has been created for the targeted transport of α−mangostin in order to avoid this deteriorative outcome. The average hydrodynamic size of CCP−liposome particles is 98.59 ± 5.1 nm with a PDI of 0.098 ± 0.02 and a negative zeta potential of 22.31 ± 2.4 mV. TEM showed the shape of the spherical CCP−liposomes. α−Mangostin is successfully captured inside CCP−liposome and the loading yield reached the highest encapsulation efficiency of 83% with 150 μg/mL of α−mangostin. In the acidic condition of pH 5.0, an initial burst of α−mangostin reached 50% after 6 h in buffer solution. CCP−liposomes could escape from endosomes even after 3 h, and almost 80% of CCP−liposomes escaped after 24 h. The cell ability of α−mangostin-loaded-CCP−liposome incubated in buffer solutions of 5.0 decreased significantly and was close to free α−mangostin. Our data proved that α−mangostin-loaded CCP−liposome delivered more effectively α−mangostin into cells and prevented the degradation of α−mangostin inside cells, especially endosomal degradation.

Record ID

LAPSE:2023.36703

Keywords

charge-conversion polymer, DDS, liposome, α–mangostin

Subject

Materials

Suggested Citation

Phan TTK, Nguyen HH, Nguyen XT, Van Nguyen T, Duong LA, Nguyen LP, Pham UT, Le HN, Tran TQ, Nguyen DT, Pham DTN. Fabrication of a Charge-Conversion Polymer—Liposome for Enhancing Endosomal Escape of Drug Delivery System for α−Mangostin. (2023). LAPSE:2023.36703

Author Affiliations

Phan TTK: Graduate University of Science and Technology, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet St., Cau Giay Dist., Hanoi 10000, Vietnam; Institute of Genome Research, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Vi
Nguyen HH: Institute of Genome Research, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet St., Cau Giay Dist., Hanoi 10000, Vietnam
Nguyen XT: Institute of Genome Research, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet St., Cau Giay Dist., Hanoi 10000, Vietnam
Van Nguyen T: Institute of Genome Research, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet St., Cau Giay Dist., Hanoi 10000, Vietnam [ORCID]
Duong LA: Institute of Genome Research, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet St., Cau Giay Dist., Hanoi 10000, Vietnam
Nguyen LP: School of Preventive Medicine and Public Health, Hanoi Medical University, 1 Ton That Tung St., Dong Da Dist., Hanoi 10000, Vietnam
Pham UT: Institute for Tropical Technology, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet St., Cau Giay Dist., Hanoi 10000, Vietnam
Le HN: Graduate University of Science and Technology, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet St., Cau Giay Dist., Hanoi 10000, Vietnam; Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Ho
Tran TQ: Graduate University of Science and Technology, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet St., Cau Giay Dist., Hanoi 10000, Vietnam; Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Ho [ORCID]
Nguyen DT: Graduate University of Science and Technology, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet St., Cau Giay Dist., Hanoi 10000, Vietnam; Institute for Tropical Technology, Vietnam Academy of Science and Technology (VAST), 18 Hoang Qu [ORCID]
Pham DTN: NTT Institute of Applied Technology and Sustainable Development, Nguyen Tat Thanh University, Ho Chi Minh City 70000, Vietnam; Faculty of Environmental and Food Engineering, Nguyen Tat Thanh University, Ho Chi Minh City 70000, Vietnam [ORCID]

Journal Name

Processes

Volume

11

Issue

8

First Page

2344

Year

2023

Publication Date

2023-08-04