RU 58841-myristate - Prodrug development for topical treatment of acne and androgenetic alopecia

Pharmazie

Volumn 60, Issue 1, 2005, Pages 8-12

  Munster U ^a   Nakamura, C ^a   Haberland, A ^a   Jores, K ^a   Mehnert, W ^a   Rummel, S ^a   Schaller, M ^b   Korting, H C ^b   Zouboulis, Ch C ^c   Blume Peytavi, U ^d   Schäfer Korting, Monika ^a  

^a FREIE UNIVERSITÄT BERLIN   (Germany)

^b UNIVERSITY OF MUNICH   (Germany)

^c CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN   (Germany)

^d HUMBOLDT UNIVERSITY   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

4 (4,4 DIMETHYL 2,5 DIOXO 1 IMIDAZOLIDINYL) 2 (TRIFLUOROMETHYL)BENZONITRILE; 4 [3 (4 HYDROXYBUTYL) 4,4 DIMETHYL 2,5 DIOXO 1 IMIDAZOLIDINYL] 2 TRIFLUOROMETHYLBENZONITRILE; 4 [4,4 DIMETHYL 2,5 DIOXO 3 (4 HYDROXYBUTYL) 1 IMIDAZOLIDINYL] 2 (TRIFLUOROMETHYL)BENZONITRILE; 4 [4,4 DIMETHYL 2,5 DIOXO 3 (CARBOXYPROPYL) 1 IMIDAZOLIDINYL] 2 (TRIFLUOROMETHYL)BENZONITRILE; 4 [4,4 DIMETHYL 3 (2 HYDROXYETHYL) 5 OXO 2 THIOXO 1 IMIDAZOLIDINYL] 2 TRIFLUOROMETHYLBENZONITRILE; ANDROGEN RECEPTOR; ANDROSTANOLONE; ANTIANDROGEN; GLYCEROL BEHENATE; GLYCEROL PALMITOSTEARATE; MIGLYOL; POLOXAMER; PRODRUG; RU 56279; RU 57073; RU 59416; SOLID LIPID NANOPARTICLE; UNCLASSIFIED DRUG;

ACNE; ARTICLE; CONTROLLED STUDY; DIFFUSION; DRUG PENETRATION; DRUG RECEPTOR BINDING; EPIDERMIS; FIBROBLAST; HAIR FOLLICLE; HUMAN; HUMAN CELL; KERATINOCYTE; MALE TYPE ALOPECIA; PREPUCE; SCALP; SEBACEOUS GLAND; SKIN CELL; TRANSMISSION ELECTRON MICROSCOPY;

ACNE VULGARIS; ALOPECIA; CELL DIVISION; CELL LINE; CHEMISTRY, PHARMACEUTICAL; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; HAIR FOLLICLE; HUMANS; IMIDAZOLES; LIPOSOMES; MICROSCOPY, ELECTRON, TRANSMISSION; MICROSCOPY, FLUORESCENCE; MICROSPHERES; MYRISTATES; NITRILES; PRODRUGS; RECEPTORS, ANDROGEN; SKIN ABSORPTION; SPECTROPHOTOMETRY, ULTRAVIOLET;

EID: 19944432512     PISSN: 00317144     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (20)

1. Akamatsu H, Zouboulis CC, Orfanos CE (1992) Control of human sebocyte proliferation in vitro by testosterone and 5α-dihydrotestosterone is dependent on the localization of the sebaceous glands. J Invest Dermatol 99: 509-511.
2. Ando Y, Yamaguchi Y, Hamada K, Yoshikawa K, Itami S (1999) Expression of mRNA for androgen receptor, 5α-reductase and 17β-hydroxysteroid dehydrogenase in human dermal papilla cells. Br J Dermatol 141: 840-845.
3. Battmann T, Bonfils A, Branche C, Humbert J, Goubet F, Teutsch G, Philibert D (1994) RU 58841, a new specific topical antiandrogen: a candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism. J Steroid Biochem Mol Biol 48: 55-60.
4. Bernard E, Dubois JL, Wepierre J (1997) Importance of sebaceous glands in cutaneous penetration of an antiandrogen: target effect of liposomes. J Pharm Sci 86: 573-578.
5. Chen W, Zouboulis CC, Fritsch M, Blume-Peytavi U, Kodelja V, Goerdt S, Luu-The V, Orfanos CE (1998) Evidence of heterogeneity and quantitative differences of the type 1 5α-reductase expression in cultured human skin cells - evidence of its presence in melanocytes. J Invest Dermatol 110: 84-89.
6. Cousty-Berlin D, Bergaud B, Bruyant MC, Battmann T, Branche C, Philibert D (1994) Preliminary pharmacokinetics and metabolism of novel non-steroidal antiandrogens in the rat: relation of their systemic activity to the formation of a common metabolite. J Steroid Biochem Mol Biol 51: 47-55.
7. Fritsch M, Orfanos CE, Zouboulis CC (2001) Sebocytes are the key regulators of androgen homeostasis in human skin. J Invest Dermatol 116: 793-800.
8. Gysler A, Lange K, Korting HC, Schäfer-Korting M (1997) Prednicarbate biotransformation in human foreskin keratinocytes and fibroblasts. Pharm Res 14: 793-797.
9. Hamilton JB (1942) Male hormone stimulation is prerequisite and an incitant in common baldness. Am J Anat 71: 451-480.
10. Lauer AC, Lieb LM, Ramachandran C, Flynn GL, Weiner ND (1995) Transfollicular drug delivery. Pharm Res 12: 179-186.
11. Leyden JJ (1997) Therapy for acne vulgaris. N Engl J Med 336: 1156-1162.
12. Ludwig E (1977) Classification of the types of androgenetic alopecia (common baldness) occurring in the female sex. Br J Dermatol 97: 247-254.
13. Masini V, Bonte F, Meybeck A, Wepierre J (1993) Cutaneous bioavailability in hairless rats of tretinoin in liposomes or gel. J Pharm Sci 82: 17-21.
14. Mehnert W, Mäder K (2001) Solid lipid nanoparticles: production, characterization and applications. Adv Drug Deliv Rev 47: 165-196.
15. Millikan LE (2000) Adapalene: an update on newer comparative studies between the various retinoids. Int J Dermatol 39: 784-788.
16. Müller RH, Radtke M, Wissing SA (2002) Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and atological preparations. Adv Drug Deliv Rev 54 Suppl 1: S131-155.
17. Münster U, Hammer S, Blume-Peytavi U, Schäfer-Korting M (2003) Testosterone metabolism in human skin cells in vitro and its interaction with estradiol and dutasteride. Skin Pharm Appl Skin Physiol 16: 356-366.
18. Santos Maia C, Mehnert W, Schaller M, Korting HC, Gysler A, Haberland A, Schäfer-Korting M (2002) Drug targeting by solid lipid nanoparticles for dermal use. J Drug Target 10: 489-495.
19. Schaller M, Steinle R, Korting HC (1997) Light and electron microscopic findings in human epidermis reconstructed in vitro upon topical application of liposomal tretinoin. Acta Derm Venereol 77: 122-126.
20. Zouboulis CC, Seltmann H, Neitzel H, Orfanos CE (1999) Establishment and characterization of an immortalized human sebaceous gland cell line (SZ95). J Invest Dermatol 113: 1011-1020.