Positively charged cholesterol derivative combined with liposomes as an efficient drug delivery system, in vitro and in vivo study

Bin Yang, Sheng Yong Geng, Xin Ming Liu, Jian Tao Wang, Yong Kui Chen, Yu Lu Wang, Jin Ye Wang

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

Liposomes are widely used as drug delivery systems. However, inefficient delivery limits their application in serum containing systems. In this study, two cholesterol derivatives were synthesized and incorporated into liposomes. The charge influence on drug delivery was investigated. The results indicated that the positively charged liposomes showed a higher delivery efficiency for drugs with both small molecular weight (DOX, doxorubicin) and macromolecular weight (polyethylene glycol 6000 conjugated with rhodamine B, PEG-RhB) into cells, compared with neutral liposomes even in the presence of serum. The cytotoxicity of the positive liposomes was lower than that of DOTAP (N-(1-(2,3-dioleoyloxy) propyl-N,N,N-trimethylammonium mesylate) liposomes. Moreover, results from confocal microscopy indicated that the positive DOX-liposomes underwent a quick binding process onto the cell membrane, followed by drug uptake by the cell. In vivo experiments also revealed that the positive DOX-liposomes had a higher drug delivery ability into rat retina than the neutral ones.

Original languageEnglish (US)
Pages (from-to)518-525
Number of pages8
JournalSoft Matter
Volume8
Issue number2
DOIs
StatePublished - Jan 14 2012

Fingerprint

cholesterol
Liposomes
delivery
drugs
Cholesterol
Derivatives
serums
Doxorubicin
rhodamine B
Drug delivery
retina
rhodamine
cells
rats
glycols
polyethylenes
molecular weight
Mesylates
Drug Delivery Systems
Confocal microscopy

ASJC Scopus subject areas

  • Chemistry(all)
  • Condensed Matter Physics

Cite this

Positively charged cholesterol derivative combined with liposomes as an efficient drug delivery system, in vitro and in vivo study. / Yang, Bin; Geng, Sheng Yong; Liu, Xin Ming; Wang, Jian Tao; Chen, Yong Kui; Wang, Yu Lu; Wang, Jin Ye.

In: Soft Matter, Vol. 8, No. 2, 14.01.2012, p. 518-525.

Research output: Contribution to journalArticle

Yang, Bin ; Geng, Sheng Yong ; Liu, Xin Ming ; Wang, Jian Tao ; Chen, Yong Kui ; Wang, Yu Lu ; Wang, Jin Ye. / Positively charged cholesterol derivative combined with liposomes as an efficient drug delivery system, in vitro and in vivo study. In: Soft Matter. 2012 ; Vol. 8, No. 2. pp. 518-525.
@article{ee8ee3d64ab941c28da07a0ac01bf146,
title = "Positively charged cholesterol derivative combined with liposomes as an efficient drug delivery system, in vitro and in vivo study",
abstract = "Liposomes are widely used as drug delivery systems. However, inefficient delivery limits their application in serum containing systems. In this study, two cholesterol derivatives were synthesized and incorporated into liposomes. The charge influence on drug delivery was investigated. The results indicated that the positively charged liposomes showed a higher delivery efficiency for drugs with both small molecular weight (DOX, doxorubicin) and macromolecular weight (polyethylene glycol 6000 conjugated with rhodamine B, PEG-RhB) into cells, compared with neutral liposomes even in the presence of serum. The cytotoxicity of the positive liposomes was lower than that of DOTAP (N-(1-(2,3-dioleoyloxy) propyl-N,N,N-trimethylammonium mesylate) liposomes. Moreover, results from confocal microscopy indicated that the positive DOX-liposomes underwent a quick binding process onto the cell membrane, followed by drug uptake by the cell. In vivo experiments also revealed that the positive DOX-liposomes had a higher drug delivery ability into rat retina than the neutral ones.",
author = "Bin Yang and Geng, {Sheng Yong} and Liu, {Xin Ming} and Wang, {Jian Tao} and Chen, {Yong Kui} and Wang, {Yu Lu} and Wang, {Jin Ye}",
year = "2012",
month = "1",
day = "14",
doi = "10.1039/c1sm06087b",
language = "English (US)",
volume = "8",
pages = "518--525",
journal = "Soft Matter",
issn = "1744-683X",
publisher = "Royal Society of Chemistry",
number = "2",

}

TY - JOUR

T1 - Positively charged cholesterol derivative combined with liposomes as an efficient drug delivery system, in vitro and in vivo study

AU - Yang, Bin

AU - Geng, Sheng Yong

AU - Liu, Xin Ming

AU - Wang, Jian Tao

AU - Chen, Yong Kui

AU - Wang, Yu Lu

AU - Wang, Jin Ye

PY - 2012/1/14

Y1 - 2012/1/14

N2 - Liposomes are widely used as drug delivery systems. However, inefficient delivery limits their application in serum containing systems. In this study, two cholesterol derivatives were synthesized and incorporated into liposomes. The charge influence on drug delivery was investigated. The results indicated that the positively charged liposomes showed a higher delivery efficiency for drugs with both small molecular weight (DOX, doxorubicin) and macromolecular weight (polyethylene glycol 6000 conjugated with rhodamine B, PEG-RhB) into cells, compared with neutral liposomes even in the presence of serum. The cytotoxicity of the positive liposomes was lower than that of DOTAP (N-(1-(2,3-dioleoyloxy) propyl-N,N,N-trimethylammonium mesylate) liposomes. Moreover, results from confocal microscopy indicated that the positive DOX-liposomes underwent a quick binding process onto the cell membrane, followed by drug uptake by the cell. In vivo experiments also revealed that the positive DOX-liposomes had a higher drug delivery ability into rat retina than the neutral ones.

AB - Liposomes are widely used as drug delivery systems. However, inefficient delivery limits their application in serum containing systems. In this study, two cholesterol derivatives were synthesized and incorporated into liposomes. The charge influence on drug delivery was investigated. The results indicated that the positively charged liposomes showed a higher delivery efficiency for drugs with both small molecular weight (DOX, doxorubicin) and macromolecular weight (polyethylene glycol 6000 conjugated with rhodamine B, PEG-RhB) into cells, compared with neutral liposomes even in the presence of serum. The cytotoxicity of the positive liposomes was lower than that of DOTAP (N-(1-(2,3-dioleoyloxy) propyl-N,N,N-trimethylammonium mesylate) liposomes. Moreover, results from confocal microscopy indicated that the positive DOX-liposomes underwent a quick binding process onto the cell membrane, followed by drug uptake by the cell. In vivo experiments also revealed that the positive DOX-liposomes had a higher drug delivery ability into rat retina than the neutral ones.

UR - http://www.scopus.com/inward/record.url?scp=83455205996&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=83455205996&partnerID=8YFLogxK

U2 - 10.1039/c1sm06087b

DO - 10.1039/c1sm06087b

M3 - Article

AN - SCOPUS:83455205996

VL - 8

SP - 518

EP - 525

JO - Soft Matter

JF - Soft Matter

SN - 1744-683X

IS - 2

ER -