Læknablaðið - 15.03.1993, Page 16

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LÆKNABLAÐIÐ
molecule, or some part of it, into the cavity.
Such encapsulation of a drug molecule will
affect many of its physicochemical properties.
Cyclodextrins are shown to have effect on the
aqueous solubility of drugs and their delivery
through biological mentbranes, e.g. transcorneal
delivery of acetazolamide. Also, they can
increase both solubility and chemical stability
of many anticancer drugs. There are basically
two methods which can be used to increase the
transdermal delivery of drugs, i.e. by changing the
barrier function of the skin and by increasing the
availability of drugs at the skin surface. Penetration
enhancers, such as oleic acid and lauroylcholine
iodide, alter the skin barrier and thereby increase
the permeability of drugs into and through the
skin. Cyclodextrins do not penetrate the skin
barrier. Drug-cyclodextrin complexes deliver
drug molecules to the skin surface where they are
released before they partition into the skin.
HEIMILDIR
1. Korolkovas A. Essentials of Medicinal Chemistry,
2nd ed. New York: John Wily & Sons, 1988: 53-139.
2. Ariens EJ. A General Introduction to the Field of
Drug Design. In: Ariéns EJ. ed. Drug Design, Vol.
I. New York: Academic Press, 1971: 1-270.
3. Albert A. Selective Toxicity. New York: John Wily &
Sons, 1964: 57-63.
4. Ellmer R. Acetylsalicylsaure. Chem Labor Betr 1978;
7: 82.
5. Loftsson T, Kaminski JJ, Bodor N. Improved
Delivery through Biological Membranes VIII. Design,
Synthesis and In Vivo Testing of True Prodrugs of
Aspirin. J Pharm Sci 1981; 70: 743-9.
6. Loftsson T. Bodor N. Improved Delivery through
Biological Membranes IX. The Kinetics and
Mechanism of Hydrolysis of Methylsulfinylmethyl
2-Acetoxybenzoate and Related Aspirin Prodrugs. J
Pharm Sci 1981; 70: 750-5.
7. Loftsson T, Bodor N. Improved Delivery through
Biological Membranes VIII. Percutaneous absorption
and Metabolism of the Methylsulfinylmethyl 2-
Acetoxybenzoate and Related Aspirin Prodrugs. J
Pharm Sci 1981; 70: 756-8.
8. Raghavan K, Loftsson T, Brewster ME, Bodor N.
Improved Delivery Through Biological Membranes
XLV. Synthesis, Physical-Chemical Evaluation, and
Brain Uptake Studies of 2-Chloroethyl Nitrosourea
Delivery System. Pharm Res 1992; 9: 743-9.
9. Pop E, Loftsson T, Bodor N. Novel Central Nervous
System Targeted Semisynthetic Penicillins. Drug
Design Del 1990; 5: 221-37.
10. Bodor N, Loftsson T. Novel Chemical Approaches
for Sustained Drug Delivery. In: Robinson JR, Lee
VHL, ed. Controlled Drug Delivery: Fundamentals
and Applications, 2nd ed. New York: Marcel Dekker,
1987: 337-71.
11. Bodor N. The Application of Soft Dmg Approaches
to the Design of Safer Corticosteroids. In:
Christophers E, Kligman AM, Schopf E, Stoughton
RB, cds. Topical Corticosteroid Therapy: A Novel
Approach to Safer Drugs. New York: Raven Press,
1988: 13-25.
12. Bodor N, Loftsson T, Wu W. Metabolism,
Distribution, and Transdermal Permeation of a Soft
Corticosteroid, Loteprednol Etabonate. Pharm Res
1992; 9: 1275-8.
13. Bodor N, Oshiro Y, Loftsson T. Katovich M,
Caldwell W. Soft Drugs VI. The Application of the
Inactive Metabolite Approach for Design of Soft /3-
Blockers. Pharm Res 1984; 1: 120-5.
14. Loftsson T, Brewster ME, Derendorf H, Bodor N. 2-
Hydroxypropyl-/3-cyclodextrin: Properties and Usage
in Pharmaceutical Formulations. Pharni Ztg Wiss
1991; 4/136: 5-10.
15. Loftsson T, Bodor N. Effects of 2-Hydroxypropyl-
/3-cyclodestrin on Aqueous Solubility of Drugs and
Transdermal Delivery of 17/3-Estradiol. Acta Pharm
Nord 1989; 1: 185-94.
16. Loftsson T, Ólafsdóttir BJ, Friðriksdóttir H.
Comparative Study on Inclusion Complexation of
Acetylsalicylic Acid, Cholecalciferol and Melphalan
with /3- and 7-Cyclodextrin and some of their
Derivatives. Acta Pharm Nord 1990; 2: 303-12.
17. Brewster ME, Loftsson T, Baldvinsdóttir J, Bodor
N. Stabilization of Aspartame by Cyclodextrins. Int J
Pharm 1991; 75: R5-R8.
18. Loftsson T, Friðriksdóttir H, Ólafsdóttir BJ,
Guðmundsson Ö. Solubilization and Stabilization
of Drugs through Cyclodextrin Complexation. Acta
Pharm Nord 1991; 3: 215-17.
19. Loftsson T. Stefánsdóttir Ó, Friðriksdóttir,
Gupmundsson Ö. Interactions between Preservatives
and 2-Hydroxypropyl-/3-cyclodextrin. Drug Dev Ind
Pharm 1992; 18: 1477-84.
20. Kristmundsdóttir T, Loftsson T, Holbrook WP,
Ingvarsdóttir K, Friðriksdóttir H. Hönnun og klínískt
mat á hýdrókortisón lausn til meðhöndlunar á
bólgusjúkdómum í munnholi. Læknablaðið 1992;
78/Fylgirit 22: 66.
21. Friðriksdóttir H, Þórisdóttir S, Sigurðardóttir
AM, Loftsson T, Stefánsson E. Áhrif
karbóanhýdrasablokkara á augnþrýsting í kanínum.
Læknablaðið 1992; 78/ Fylgirit 22: 85.
22. Loftsson T, Björnsdóttir S, Pálsdóttir G, Bodor N.
The Effects of 2-Hydroxypropyl-/3-cyclodextrin on
the Solubility and Stability of Chlorambucil and
Melphalan in Aqueous Solution. Int J Pharm 1989;
57: 63-72.
23. Loftsson T, Ólafsdóttir BJ. The Effect of 2-
Hydroxypropyl-/3-cyclodextrin on the Simultaneous
Dissolution and Degradation of Chlorambucil. Int J
Pharm 1990; 66: 289-92.
24. Brewster ME, Loftsson T, Estes KS, Lin JL,
Friðriksdóttir H, Bodor N. Effect of Various
Cyclodextrins on Solution Stability and Dissolution
Rate of Doxorubicin Hydrochloride. Int J Pharm
1992; 79: 289-99.
25. Loftsson T, Friðriksdóttir H. Degradation of
Lomustine (CCNU) in Aqueous Solutions. Int J
Pharm 1990; 62: 243-7.
26. Loftsson T, Ólafsdóttir BJ, Baldvinsdóttir J.
Estramustine: Hydrolysis, Solubilization, and
Stabilization in Aqueous Solutions. Int J Pharm 1992;
79: 107-12.
27. Loftsson T, Baldvinsdóttir J. Degradation of
Tauromustine (TCNU) in Aqueous Solutions. Acta
Pharm Nord 1992; 4: 129-32.
28. Loftsson T, Ólafsdóttir BJ. Cyclodextrin-accelerated
Degradation of /3-Lactam Antibiotics in Aqueous
Solutions. Int J Pharm 1991; 67: R5-R7.
29. Pop E, Loftsson T, Bodor N. Solubilization and