Abstract
Major limitations in the use of liposomes for oral formulation relate to their physical and chemical instability in the GI tract. In this study, the conjugate (PAA-DSPE) of poly(acrylic acid) and distearoylphosphatidylethanolamine (DSPE) was synthesized, and liposomes were prepared with the mixture of PAA-DSPE and DSPE to improve the stability of liposomes in the GI tract. The prepared PAA-DSPE was characterized by FT-IR and 13C-NMR to confirm the coupling between PAA and DSPE. In the elemental analysis, the coupling ratio of PAA and DSPE in PAA-DSPE was calculated as 1:1.73. The average size of a PAA-DSPE/DSPE liposome, measured by dynamic light scattering, was in the range of 300-500 nm, and the minimum average size was 320 nm at 6 mol% of PAA-DSPE. The stability of the prepared liposomes was evaluated in different pH (2, 5, 7.4) solutions, and in different concentrations of bile acid (0, 0.1, 1, 10%) and pancreatin solutions (0, 0.03, 0.3, 3%). The stability of liposomes in different conditions was determined by measuring the fluorescence intensity of 5(6)-CF leaked from liposomes. The amount of the 5(6)-CF leakage from the PAA-DSPE/DSPE liposomes of 6 mol% PAA-DSPE was the lowest in all the cases of acidic, bile, and pancreatin solutions. In conclusion, the optimum amount of PAA-DSPE in liposome was 6 mol%, and PAA-DSPE/DSPE liposomes could improve the stability in the GI tract.
| Original language | English |
|---|---|
| Pages (from-to) | 13-18 |
| Number of pages | 6 |
| Journal | Drug Development Research |
| Volume | 61 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - 2004 Jan 1 |
| Externally published | Yes |
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Keywords
- Bile solution
- Liposome
- PAA-DSPE
- Pancreatic solution
- PH
- Stability
ASJC Scopus subject areas
- Drug Discovery
Cite this
Stability of Poly(Acrylic Acid)-Grafted Phospholipid Liposomes in Gastrointestinal Conditions. / Lee, Hyun Sup; Kim, Kwang Meyung; Jeong, Bong Hyun; Moon, Hyun Tae; Byun, Youngro.
In: Drug Development Research, Vol. 61, No. 1, 01.01.2004, p. 13-18.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Stability of Poly(Acrylic Acid)-Grafted Phospholipid Liposomes in Gastrointestinal Conditions
AU - Lee, Hyun Sup
AU - Kim, Kwang Meyung
AU - Jeong, Bong Hyun
AU - Moon, Hyun Tae
AU - Byun, Youngro
PY - 2004/1/1
Y1 - 2004/1/1
N2 - Major limitations in the use of liposomes for oral formulation relate to their physical and chemical instability in the GI tract. In this study, the conjugate (PAA-DSPE) of poly(acrylic acid) and distearoylphosphatidylethanolamine (DSPE) was synthesized, and liposomes were prepared with the mixture of PAA-DSPE and DSPE to improve the stability of liposomes in the GI tract. The prepared PAA-DSPE was characterized by FT-IR and 13C-NMR to confirm the coupling between PAA and DSPE. In the elemental analysis, the coupling ratio of PAA and DSPE in PAA-DSPE was calculated as 1:1.73. The average size of a PAA-DSPE/DSPE liposome, measured by dynamic light scattering, was in the range of 300-500 nm, and the minimum average size was 320 nm at 6 mol% of PAA-DSPE. The stability of the prepared liposomes was evaluated in different pH (2, 5, 7.4) solutions, and in different concentrations of bile acid (0, 0.1, 1, 10%) and pancreatin solutions (0, 0.03, 0.3, 3%). The stability of liposomes in different conditions was determined by measuring the fluorescence intensity of 5(6)-CF leaked from liposomes. The amount of the 5(6)-CF leakage from the PAA-DSPE/DSPE liposomes of 6 mol% PAA-DSPE was the lowest in all the cases of acidic, bile, and pancreatin solutions. In conclusion, the optimum amount of PAA-DSPE in liposome was 6 mol%, and PAA-DSPE/DSPE liposomes could improve the stability in the GI tract.
AB - Major limitations in the use of liposomes for oral formulation relate to their physical and chemical instability in the GI tract. In this study, the conjugate (PAA-DSPE) of poly(acrylic acid) and distearoylphosphatidylethanolamine (DSPE) was synthesized, and liposomes were prepared with the mixture of PAA-DSPE and DSPE to improve the stability of liposomes in the GI tract. The prepared PAA-DSPE was characterized by FT-IR and 13C-NMR to confirm the coupling between PAA and DSPE. In the elemental analysis, the coupling ratio of PAA and DSPE in PAA-DSPE was calculated as 1:1.73. The average size of a PAA-DSPE/DSPE liposome, measured by dynamic light scattering, was in the range of 300-500 nm, and the minimum average size was 320 nm at 6 mol% of PAA-DSPE. The stability of the prepared liposomes was evaluated in different pH (2, 5, 7.4) solutions, and in different concentrations of bile acid (0, 0.1, 1, 10%) and pancreatin solutions (0, 0.03, 0.3, 3%). The stability of liposomes in different conditions was determined by measuring the fluorescence intensity of 5(6)-CF leaked from liposomes. The amount of the 5(6)-CF leakage from the PAA-DSPE/DSPE liposomes of 6 mol% PAA-DSPE was the lowest in all the cases of acidic, bile, and pancreatin solutions. In conclusion, the optimum amount of PAA-DSPE in liposome was 6 mol%, and PAA-DSPE/DSPE liposomes could improve the stability in the GI tract.
KW - Bile solution
KW - Liposome
KW - PAA-DSPE
KW - Pancreatic solution
KW - PH
KW - Stability
UR - http://www.scopus.com/inward/record.url?scp=0347988095&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0347988095&partnerID=8YFLogxK
U2 - 10.1002/ddr.10331
DO - 10.1002/ddr.10331
M3 - Article
AN - SCOPUS:0347988095
VL - 61
SP - 13
EP - 18
JO - Drug Development Research
JF - Drug Development Research
SN - 0272-4391
IS - 1
ER -