New micelle-like polymer aggregates made from PEI-PLGA diblock copolymers: Micellar characteristics and cellular uptake

Yoon Sung Nam; Hyung Seok Kang; Ju Young Park; Tae Gwan Park; Sang Hoon Han; Ih Seop Chang

doi:10.1016/S0142-9612(02)00641-5

New micelle-like polymer aggregates made from PEI-PLGA diblock copolymers: Micellar characteristics and cellular uptake

Yoon Sung Nam, Hyung Seok Kang, Ju Young Park, Tae Gwan Park, Sang Hoon Han, Ih Seop Chang

Research output: Contribution to journal › Article › peer-review

118 Scopus citations

Abstract

New amphiphilic block copolymers based on oligomeric polyethylenimine and poly(D,L-lactide-co-glycolide) (PEI-PLGA) were synthesized by directly coupling PLGA with a carboxyl terminal group to PEI. The block copolymers were prepared by varying the length of the hydrophobic PLGA block (M_n=6, 10, and 21K), while that of the hydrophilic PEI block (M_n=423) was fixed. PEI-PLGA block copolymers were found to be self-assembled in water by using a PLGA segment as a hydrophobic aggregate block and a PEI segment as a hydrophilic corona-forming block. The block copolymers formed micelle-like aggregates with critical association concentration (cac) in the range of 1.54-2.57×10^-3g/l in water. It was found that the size and cac of the aggregates depended on the hydrophobic block length and the ionic state of the PEI block. The aggregate size decreased and the cac increased, when the PLGA block length decreased and the PEI block was protonated. As a general program aimed at the development of a new nanoscopic drug carrier, the cellular uptake behavior of PEI-PLGA aggregates was compared with that of plain PLGA nanoparticles by using confocal microscopy. The results showed that PEI-PLGA aggregates was readily adsorbed onto the cell surfaces and translocated into the cytoplasm, implying their versatile applicability as a drug carrier.

Original language	English
Pages (from-to)	2053-2059
Number of pages	7
Journal	Biomaterials
Volume	24
Issue number	12
DOIs	https://doi.org/10.1016/S0142-9612(02)00641-5
State	Published - May 2003
Externally published	Yes

Funding

We gratefully acknowledge the Ministry of Science and Technology (the National Research Laboratory (NRL) program, Project No. 2000-N-NL-01-C-270) and the Ministry of Health and Welfare (the IMT-2000 program, Project No. 01-PJ11-PG9-01NT00-0050) in Republic of Korea for financial supports. We would like to thank Su Jung Kim (NICEM) for the TEM analysis, So Hee Kwon (NICEM) for the CLSM analysis, and Yun Gyong Ahn (KBSI) for the DSC measurements.

Keywords

Amphiphilic copolymer
Biodegradable
Drug delivery
Polyethylenimine
Polymeric micelles

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10.1016/S0142-9612(02)00641-5

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title = "New micelle-like polymer aggregates made from PEI-PLGA diblock copolymers: Micellar characteristics and cellular uptake",

abstract = "New amphiphilic block copolymers based on oligomeric polyethylenimine and poly(D,L-lactide-co-glycolide) (PEI-PLGA) were synthesized by directly coupling PLGA with a carboxyl terminal group to PEI. The block copolymers were prepared by varying the length of the hydrophobic PLGA block (Mn=6, 10, and 21K), while that of the hydrophilic PEI block (Mn=423) was fixed. PEI-PLGA block copolymers were found to be self-assembled in water by using a PLGA segment as a hydrophobic aggregate block and a PEI segment as a hydrophilic corona-forming block. The block copolymers formed micelle-like aggregates with critical association concentration (cac) in the range of 1.54-2.57×10-3g/l in water. It was found that the size and cac of the aggregates depended on the hydrophobic block length and the ionic state of the PEI block. The aggregate size decreased and the cac increased, when the PLGA block length decreased and the PEI block was protonated. As a general program aimed at the development of a new nanoscopic drug carrier, the cellular uptake behavior of PEI-PLGA aggregates was compared with that of plain PLGA nanoparticles by using confocal microscopy. The results showed that PEI-PLGA aggregates was readily adsorbed onto the cell surfaces and translocated into the cytoplasm, implying their versatile applicability as a drug carrier.",

keywords = "Amphiphilic copolymer, Biodegradable, Drug delivery, Polyethylenimine, Polymeric micelles",

author = "Nam, \{Yoon Sung\} and Kang, \{Hyung Seok\} and Park, \{Ju Young\} and Park, \{Tae Gwan\} and Han, \{Sang Hoon\} and Chang, \{Ih Seop\}",

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T2 - Micellar characteristics and cellular uptake

AU - Nam, Yoon Sung

AU - Kang, Hyung Seok

AU - Park, Ju Young

AU - Park, Tae Gwan

AU - Han, Sang Hoon

AU - Chang, Ih Seop

PY - 2003/5

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N2 - New amphiphilic block copolymers based on oligomeric polyethylenimine and poly(D,L-lactide-co-glycolide) (PEI-PLGA) were synthesized by directly coupling PLGA with a carboxyl terminal group to PEI. The block copolymers were prepared by varying the length of the hydrophobic PLGA block (Mn=6, 10, and 21K), while that of the hydrophilic PEI block (Mn=423) was fixed. PEI-PLGA block copolymers were found to be self-assembled in water by using a PLGA segment as a hydrophobic aggregate block and a PEI segment as a hydrophilic corona-forming block. The block copolymers formed micelle-like aggregates with critical association concentration (cac) in the range of 1.54-2.57×10-3g/l in water. It was found that the size and cac of the aggregates depended on the hydrophobic block length and the ionic state of the PEI block. The aggregate size decreased and the cac increased, when the PLGA block length decreased and the PEI block was protonated. As a general program aimed at the development of a new nanoscopic drug carrier, the cellular uptake behavior of PEI-PLGA aggregates was compared with that of plain PLGA nanoparticles by using confocal microscopy. The results showed that PEI-PLGA aggregates was readily adsorbed onto the cell surfaces and translocated into the cytoplasm, implying their versatile applicability as a drug carrier.

AB - New amphiphilic block copolymers based on oligomeric polyethylenimine and poly(D,L-lactide-co-glycolide) (PEI-PLGA) were synthesized by directly coupling PLGA with a carboxyl terminal group to PEI. The block copolymers were prepared by varying the length of the hydrophobic PLGA block (Mn=6, 10, and 21K), while that of the hydrophilic PEI block (Mn=423) was fixed. PEI-PLGA block copolymers were found to be self-assembled in water by using a PLGA segment as a hydrophobic aggregate block and a PEI segment as a hydrophilic corona-forming block. The block copolymers formed micelle-like aggregates with critical association concentration (cac) in the range of 1.54-2.57×10-3g/l in water. It was found that the size and cac of the aggregates depended on the hydrophobic block length and the ionic state of the PEI block. The aggregate size decreased and the cac increased, when the PLGA block length decreased and the PEI block was protonated. As a general program aimed at the development of a new nanoscopic drug carrier, the cellular uptake behavior of PEI-PLGA aggregates was compared with that of plain PLGA nanoparticles by using confocal microscopy. The results showed that PEI-PLGA aggregates was readily adsorbed onto the cell surfaces and translocated into the cytoplasm, implying their versatile applicability as a drug carrier.

KW - Amphiphilic copolymer

KW - Biodegradable

KW - Drug delivery

KW - Polyethylenimine

KW - Polymeric micelles

UR - https://www.scopus.com/pages/publications/0037400585

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JO - Biomaterials

JF - Biomaterials

IS - 12

ER -

New micelle-like polymer aggregates made from PEI-PLGA diblock copolymers: Micellar characteristics and cellular uptake

Abstract

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Keywords

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