Earticle

초록

영어

Because human tumors have an acidic extracellular environment, nanoparticles (NP) undergoing physicochemical changes to release the enclosed drug at acidic pH conditions are promising vehicles for antitumor drug delivery. Among various drug carriers, high density lipoprotein (HDL)-like NPs have been shown to be beneficial for cancer chemotherapy, but have not been designed to be pH-responsive. In this study, we developed a pH-responsive HDL-like NP which selectively releases paclitaxel (PTX), a model antitumor drug, at acidic pH. While the well-known HDL-like NP that contained phospholipids phosphatidylcholine as well as apolipoprotein A-I (apoA-I) and PTX (PTX-PL-NP) was structurally robust at a wide range of pHs (3.8~10.0), the PTX-NP that only contained PTX and apoA-I as constituents uncoated its apoA-I shell and released the PTX into medium selectively at low pH. The pH-sensitivity was correlated to structural disorder of apoA-I shell. The PTX-NP was stable at physiological and basic pHs, and over a wide range of temperatures, which is a required feature for efficient cancer chemotherapy. The homogeneous assembly enabled high PTX loading per NP, which was 62.2 % (w/w). The molar ratio of apoA-I and PTX was 1:55, suggesting that a NP contains ~110 PTX in a spherical structure with a 9.2 nm diameter. Among several reconstitution methods applied, simple dilution following sonication enhanced reconstitution yield of a soluble PTX-NP, which was 0.66. This is the first pH-responsive NP that does not contain any synthetic polymer.

키워드

저자

• Jae-Yoon SHIN [ School of Life Science and Biotechnology, Sungkyunkwan University, Suwon 440-746. ]
• Dae-Hyuk KWEON [ School of Life Science and Biotechnology, Sungkyunkwan University, Suwon 440-746. ]

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발행기관

간행물

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• 간행물명

  한국생물공학회 학술대회

• 간기

  반년간

• 수록기간

  1985~2013

• 십진분류

  KDC 476 DDC 576