Availability of Liposomes as Drug Carriers to the Brain

Kazuko Kobayashi, Mei Han, Shinobu Watarai, Tatsuji Yasuda

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Phospholipid vesicles, also known as liposomes, were examined for their ability to act as a drug carrier to the brain. 9-Amino-1,2,3,4-tetrahydroacridine (THA), a centrally acting acetylcholinesterase inhibitor, was used as a model drug. THA was encapsulated in dehydration-rehydration vesicles (DRV) composed of egg yolk phosphatidylcholine, cholesterol and dipalmitoylphosphatidic acid (molar ratio, 10/10/1) and injected into the heart of mice. The toxicity and side effects of THA were reduced by encapsulation in liposomes. The THA concentration in the mouse brain after injection of THA-encapsulated DRV at a dose of 2mg/kg remained higher than that of free THA at the same dose. Effective concentration of THA in the brain was also prolonged by the use of liposomes, although accumulation of THA in the spleen and kidney was observed. We, therefore, concluded that liposomes are useful as carriers of drugs to the brain.

Original languageEnglish
Pages (from-to)67-72
Number of pages6
JournalActa Medica Okayama
Volume50
Issue number2
Publication statusPublished - Apr 1996

Fingerprint

Tacrine
Drug Carriers
Liposomes
Brain
Availability
Fluid Therapy
Dehydration
Egg Yolk
Cholinesterase Inhibitors
Phosphatidylcholines
Encapsulation
Toxicity
Phospholipids
Spleen
Cholesterol
Kidney
Injections

Keywords

  • Brain targeting
  • Liposomes
  • Mouse
  • THA (9-amino-1,2,3,4-tetrahydroacridine)

ASJC Scopus subject areas

  • Surgery
  • Medicine(all)
  • Biochemistry, Genetics and Molecular Biology(all)

Cite this

Kobayashi, K., Han, M., Watarai, S., & Yasuda, T. (1996). Availability of Liposomes as Drug Carriers to the Brain. Acta Medica Okayama, 50(2), 67-72.

Availability of Liposomes as Drug Carriers to the Brain. / Kobayashi, Kazuko; Han, Mei; Watarai, Shinobu; Yasuda, Tatsuji.

In: Acta Medica Okayama, Vol. 50, No. 2, 04.1996, p. 67-72.

Research output: Contribution to journalArticle

Kobayashi, K, Han, M, Watarai, S & Yasuda, T 1996, 'Availability of Liposomes as Drug Carriers to the Brain', Acta Medica Okayama, vol. 50, no. 2, pp. 67-72.
Kobayashi, Kazuko ; Han, Mei ; Watarai, Shinobu ; Yasuda, Tatsuji. / Availability of Liposomes as Drug Carriers to the Brain. In: Acta Medica Okayama. 1996 ; Vol. 50, No. 2. pp. 67-72.
@article{f042892eb4c94691b605e9c6a1ec16f9,
title = "Availability of Liposomes as Drug Carriers to the Brain",
abstract = "Phospholipid vesicles, also known as liposomes, were examined for their ability to act as a drug carrier to the brain. 9-Amino-1,2,3,4-tetrahydroacridine (THA), a centrally acting acetylcholinesterase inhibitor, was used as a model drug. THA was encapsulated in dehydration-rehydration vesicles (DRV) composed of egg yolk phosphatidylcholine, cholesterol and dipalmitoylphosphatidic acid (molar ratio, 10/10/1) and injected into the heart of mice. The toxicity and side effects of THA were reduced by encapsulation in liposomes. The THA concentration in the mouse brain after injection of THA-encapsulated DRV at a dose of 2mg/kg remained higher than that of free THA at the same dose. Effective concentration of THA in the brain was also prolonged by the use of liposomes, although accumulation of THA in the spleen and kidney was observed. We, therefore, concluded that liposomes are useful as carriers of drugs to the brain.",
keywords = "Brain targeting, Liposomes, Mouse, THA (9-amino-1,2,3,4-tetrahydroacridine)",
author = "Kazuko Kobayashi and Mei Han and Shinobu Watarai and Tatsuji Yasuda",
year = "1996",
month = "4",
language = "English",
volume = "50",
pages = "67--72",
journal = "Acta Medica Okayama",
issn = "0386-300X",
publisher = "Okayama University",
number = "2",

}

TY - JOUR

T1 - Availability of Liposomes as Drug Carriers to the Brain

AU - Kobayashi, Kazuko

AU - Han, Mei

AU - Watarai, Shinobu

AU - Yasuda, Tatsuji

PY - 1996/4

Y1 - 1996/4

N2 - Phospholipid vesicles, also known as liposomes, were examined for their ability to act as a drug carrier to the brain. 9-Amino-1,2,3,4-tetrahydroacridine (THA), a centrally acting acetylcholinesterase inhibitor, was used as a model drug. THA was encapsulated in dehydration-rehydration vesicles (DRV) composed of egg yolk phosphatidylcholine, cholesterol and dipalmitoylphosphatidic acid (molar ratio, 10/10/1) and injected into the heart of mice. The toxicity and side effects of THA were reduced by encapsulation in liposomes. The THA concentration in the mouse brain after injection of THA-encapsulated DRV at a dose of 2mg/kg remained higher than that of free THA at the same dose. Effective concentration of THA in the brain was also prolonged by the use of liposomes, although accumulation of THA in the spleen and kidney was observed. We, therefore, concluded that liposomes are useful as carriers of drugs to the brain.

AB - Phospholipid vesicles, also known as liposomes, were examined for their ability to act as a drug carrier to the brain. 9-Amino-1,2,3,4-tetrahydroacridine (THA), a centrally acting acetylcholinesterase inhibitor, was used as a model drug. THA was encapsulated in dehydration-rehydration vesicles (DRV) composed of egg yolk phosphatidylcholine, cholesterol and dipalmitoylphosphatidic acid (molar ratio, 10/10/1) and injected into the heart of mice. The toxicity and side effects of THA were reduced by encapsulation in liposomes. The THA concentration in the mouse brain after injection of THA-encapsulated DRV at a dose of 2mg/kg remained higher than that of free THA at the same dose. Effective concentration of THA in the brain was also prolonged by the use of liposomes, although accumulation of THA in the spleen and kidney was observed. We, therefore, concluded that liposomes are useful as carriers of drugs to the brain.

KW - Brain targeting

KW - Liposomes

KW - Mouse

KW - THA (9-amino-1,2,3,4-tetrahydroacridine)

UR - http://www.scopus.com/inward/record.url?scp=0030123952&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0030123952&partnerID=8YFLogxK

M3 - Article

C2 - 8744931

AN - SCOPUS:0030123952

VL - 50

SP - 67

EP - 72

JO - Acta Medica Okayama

JF - Acta Medica Okayama

SN - 0386-300X

IS - 2

ER -