Authors: Mi Kyong Yoo, You Kyoung Kim, Hwan Jeong Jeong, Hee Seung Bom, Chong Su Cho
Abstract: To improve the specific accumulation in tumor sites and aqueous solubility of atRA, the
core-shell type of folate-PEG-g-PEI/atRA nanoparticles were prepared by complexation between
cationic PEI segments in the copolymers and anionic charged atRA, and then characterized by 1HNMR,
ELS, XRD, and TEM. In vitro atRA release from the nanoparticles was investigated as a
function of drug content in sink condition. Cytotocicity of atRA against HepG2, KB cell lines were
also evaluated by MTT assay. The lower the drug content, the faster atRA release. atRA
incorporated in folate-PEG-g-PEI/atRA nanoparticles showed much higher cytotoxic effect
compared with atRA itself.
509
Authors: Rohidas B. Arote, Tae Hee Kim, You Kyoung Kim, Dhananjay Jere, Hu Lin Jiang, In Young Park, Myung Haing Cho, Jae Woon Nah, Chong Su Cho
Abstract: Novel, biodegradable poly(ester amine)s (PEAs) were synthesized using hydrophobic
polycaprolactone diacrylate (PCLDA) and highly cationic polyethylenimine (PEI). This novel gene
carrier can form stable DNA complexes with particle sizes around 200 nm, and showing excellent
transfection efficiency and relatively low cytotoxicity compared with PEI 25K. Effect of
hydrophobicity on transfection efficiency and cytotoxicity was profound and was relatively
important parameter for the success of gene delivery.
453
Authors: You Kyoung Kim, In Kyu Park, Hu Lin Jiang, Rohidas B. Arote, Hwan Jeong Jeong, Eun Mi Kim, Myung Haing Cho, Hee Seung Bom, Chong Su Cho
Abstract: Polypropylenimine (PPI) dendrimers have been used by many researchers as gene
delivery carriers due to their high functionality. Glucose as a kind of carbohydrate is biocompatible
and hydrophilic. In this study, we synthesized glucosylated PPI (G-PPI) dendrimers to reduce
cytotoxicity. Glucose substitution of G-PPI dendrimers was determined by the sulfuric acid micromethod.
The G-PPI dendrimer was complexed with plasmid DNA in various N/P ratios, and the
complex was characterized. G-PPI dendrimers showed good DNA binding ability and high
protection of DNA from nuclease attack. The G-PPI dendrimer had low cytotoxicity compared to
PPI dendrimer by cytotoxicity assay. Also, transfection efficiency was influenced by glucosylation
degree and the transfection efficiency for the G-PPI-5 was slightly higher than that of PPI
dendrimer in HeLa cell line.
457
Authors: In Young Park, Tae Hee Kim, You Kyoung Kim, Yun Jaie Choi, Jae Woon Nah, Chong Su Cho
Abstract: The strategies developed for gene delivery are generally classified into two categories of
viral and non-viral vectors. The limitation of viral vectors, which have problems including toxicity,
immunogenicity and inflammatory response has led to the development of a novel, synthetic vectors
based on non-viral vectors. Chitosan, one of non-viral vectors, has been a good candidate in gene
delivery field. Moreover, galactosylated chitosan (GC) had the specific recognition of hepatocytes
by galactose in the GC. Also, carbonate apatite increased the rate of DNA endocytosis and the
efficiency of gene transfer. We describe here a new concept for improving cell specificity and
transfection efficiency by hybridization of carbonate apatite (CAp) with GC. The complex
formation was confirmed by agarose gel electrophoresis. The complex optimized through
controlling calcium ion and charge ratio was evaluated on the cell specificity and transfection
efficiency.
437
Authors: Hu Lin Jiang, Rohidas B. Arote, Ji Shan Quan, Mi Kyong Yoo, You Kyoung Kim, In Yong Kim, Zhong Shan Hong, Hong Gu Lee, Xun Jin, Yun Jaie Choi, Chong Su Cho
Abstract: Thiolated polymers have been studied by many researchers because of the mucoadhesive
properties of thiol group. Alginate is a natural and biocompatible polymer that has been widely used
in drug delivery. In this study, thiolated chitosan microspheres (TCMs) were prepared by ionic
gelation process with tripolyphosphate and then, the bovine growth hormone (BGH) was loaded as
a model drug. Finally, the BGH-loaded TCMs (BTCMs) were coated with alginate to improve the
stability in gastrointestinal (GI) track. The alginate-coated BTCMs (ABTCMs) were observed as
spherical shapes. The average particle sizes of ABTCMs were 6.97±0.55 -m and the sizedistribution
was shown uniformly. Release of BGH from ABTCMs was decreased by coating with
alginate and increased rapidly with the change in medium pH from 1.2 to 7.4. Results indicate that
the ABTCMs have a potential as a drug carrier for oral drug delivery.
433