Abstract
Brain-targeted delivery of various drugs can be successfully achieved by chemical delivery systems (CDS) that contain a 1,4-dihydropyridine-based redox targetor moiety and undergo a sequential metabolism. However, the susceptibility of this moiety toward hydration in acidic media may limit the shelf-life of such compounds in aqueous formulation. Here, a systematic investigation of the chemical stability toward oxidation and hydration of ester and amide derivatives of 3-substituted 1,4-dihydropyridine, 1,4-dihydroquinoline, and 4-substituted 1,2-dihydroisoquinoline is reported, together with the in vitro stability and in vivo (rat) distribution of isoquinoline-based testosterone and hydrocortisone chemical delivery systems, which were selected as having the most suitable acid-resistant targetor moieties.
| Original language | English |
|---|---|
| Pages (from-to) | 63-71 |
| Number of pages | 9 |
| Journal | Journal of Drug Targeting |
| Volume | 10 |
| Issue number | 1 |
| DOIs | |
| State | Published - Mar 25 2002 |
| Externally published | Yes |
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Keywords
- Brain-targeted delivery
- Dihydropyridine
- Hydrocortisone
- Redox
- Testosterone
ASJC Scopus subject areas
- Pharmaceutical Science
Cite this
In vitro and in vivo evaluations of dihydroquinoline- and dihydroisoquinoline-based targetor moieties for brain-specific chemical delivery systems. / Bodor, Nicholas; Farag, Hassan H.; Barros, M. Dulce C; Wu, Whei Mei; Buchwald, Peter.
In: Journal of Drug Targeting, Vol. 10, No. 1, 25.03.2002, p. 63-71.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - In vitro and in vivo evaluations of dihydroquinoline- and dihydroisoquinoline-based targetor moieties for brain-specific chemical delivery systems
AU - Bodor, Nicholas
AU - Farag, Hassan H.
AU - Barros, M. Dulce C
AU - Wu, Whei Mei
AU - Buchwald, Peter
PY - 2002/3/25
Y1 - 2002/3/25
N2 - Brain-targeted delivery of various drugs can be successfully achieved by chemical delivery systems (CDS) that contain a 1,4-dihydropyridine-based redox targetor moiety and undergo a sequential metabolism. However, the susceptibility of this moiety toward hydration in acidic media may limit the shelf-life of such compounds in aqueous formulation. Here, a systematic investigation of the chemical stability toward oxidation and hydration of ester and amide derivatives of 3-substituted 1,4-dihydropyridine, 1,4-dihydroquinoline, and 4-substituted 1,2-dihydroisoquinoline is reported, together with the in vitro stability and in vivo (rat) distribution of isoquinoline-based testosterone and hydrocortisone chemical delivery systems, which were selected as having the most suitable acid-resistant targetor moieties.
AB - Brain-targeted delivery of various drugs can be successfully achieved by chemical delivery systems (CDS) that contain a 1,4-dihydropyridine-based redox targetor moiety and undergo a sequential metabolism. However, the susceptibility of this moiety toward hydration in acidic media may limit the shelf-life of such compounds in aqueous formulation. Here, a systematic investigation of the chemical stability toward oxidation and hydration of ester and amide derivatives of 3-substituted 1,4-dihydropyridine, 1,4-dihydroquinoline, and 4-substituted 1,2-dihydroisoquinoline is reported, together with the in vitro stability and in vivo (rat) distribution of isoquinoline-based testosterone and hydrocortisone chemical delivery systems, which were selected as having the most suitable acid-resistant targetor moieties.
KW - Brain-targeted delivery
KW - Dihydropyridine
KW - Hydrocortisone
KW - Redox
KW - Testosterone
UR - http://www.scopus.com/inward/record.url?scp=0036119336&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0036119336&partnerID=8YFLogxK
U2 - 10.1080/10611860290007540
DO - 10.1080/10611860290007540
M3 - Article
C2 - 11996088
AN - SCOPUS:0036119336
VL - 10
SP - 63
EP - 71
JO - Journal of Drug Targeting
JF - Journal of Drug Targeting
SN - 1061-186X
IS - 1
ER -