Here are a couple abstracts on RU that indicate that RU is a waste with alcohol/PP as e delivery vehicle,IIRC that is what most people on these boards have used for RU.
M question is,where can I buy such a liposomal carrier for RU?
I have RU sitting in my freezer and I'll provide a log with pics on this board when I get the carrier....
J Pharm Sci. 1997 May;86(5):573-8.
Importance of sebaceous glands in cutaneous penetration of an antiandrogen: target effect of liposomes.
Bernard E, Dubois JL, Wepierre J.
Laboratoire de dermophamacologie, Faculté de Pharmacie, Châtenay-Malabry, France.
The significance of the sebaceous gland pathway in the cutaneous permeation of an antiandrogen, 4-[3-(4-hydroxybutyl)-4,4-dimethyl -2,5-dioxo-1-imidazolidinyl]-2-(trifluoromethyl)benzonitrile (RU 58841), was studied with normal hairless rat skin and an induced scar hairless rat skin without sebaceous glands. RU 58841 was dissolved in an alcoholic solution and encapsulated in liposomes for comparison. After 24 h, the cumulative percentage of RU 58841 absorbed in vitro was 3-4-fold higher in the normal skin than in the scar skin; in the case of liposomes, the accumulation of the drug in the normal dermis was significantly higher than in the scar one. In the in vivo cutaneous distribution, the epidermis and dermis of the normal skin contained higher amounts of RU 58841 than the scar skin (ninefold with the solution and 16-fold with liposomes). An autoradiography study showed that with the solution, the drug was mainly localized in the stratum corneum/epidermis, and with the liposomes, the drug was mainly localized in the sebaceous glands. We concluded that the sebaceous glands constituted the main pathway for RU 58841. The alcoholic solution encouraged the localization of the drug into the stratum corneum, whereas liposomes targeted the sebaceous glands.
PMID: 9145381 [PubMed - indexed for MEDLINE]
Expert Opin Drug Deliv. 2008 Jun;5(6):665-79.
Novel vesicular and particulate drug delivery systems for topical treatment of acne.
Castro GA, Ferreira LA.
Federal University of Minas Gerais, Department of Pharmaceutics, 31270-901, Belo Horizonte, Minas Gerais, Brazil.
BACKGROUND: The efficacy of the antiacne topical drugs is well established. The local side effects, however, mainly cutaneous irritation, erythema, dryness, peeling and scaling, remain major problems. Novel vesicular and particulate drug delivery systems have been proposed to reduce the side effects of drugs commonly used in the topical treatment of acne. OBJECTIVE: This review focuses on the development and evaluation of antiacne drug-loaded vesicular and particulate delivery systems (liposomes, polymeric microspheres and solid lipid nanoparticles) for topical treatment, their advantages and challenges. METHODS: All the literature available was reviewed to highlight the potential of these novel systems for the topical treatment of acne. CONCLUSION: The encapsulation of antiacne drugs in vesicular and particulate delivery systems represents an innovative alternative to minimize side effects, while preserving their efficacy. This can be obtained by the capacity of these systems to provide controlled release or to improve the drug penetration into skin or even into the pilosebaceous unit.
PMID: 18532922 [PubMed - indexed for MEDLINE]
Ann N Y Acad Sci. 1995 Jun 12;761:56-65.
Local inhibition of sebaceous gland growth by topically applied RU 58841.
Matias JR, Gaillard M.
Nova Biosciences, Norrie Point Research Station, Staatsburg, New York 12553, USA.
The biological activity of a series of nonsteroidal, pure androgen receptor inhibitors was compared using the Syrian hamster ear skin sebaceous gland model. RU 58841, RU 56187, RU 38882 and cyproterone acetate were applied topically for 4 weeks on the ventral ear pinna of sexually mature male Syrian hamsters. Their order of efficacy was as follows: RU 58841 > RU 56187 > RU 38882 > cyproterone acetate. Maximal reduction of 60% in the size of the sebaceous glands was observed in hamsters treated with RU 58841 at a dose of 10 micrograms per day. This degree of inhibition occurred without any systemic side effects as shown by the absence of inhibition on the contralateral untreated ear pinna. Longer treatment did not produce greater inhibition since extending the treatment period from 4 weeks to 12 weeks showed similar data. The effect of RU 58841 was reversible since the inhibited sebaceous glands returned to normal size within 4 weeks after the cessation of the topical applications. The potent localized inhibition of sebaceous glands by RU 58841 demonstrates the excellent potential of this compound as a topical drug for the treatment of acne and other androgen-mediated disorders.
PMID: 7625751 [PubMed - indexed for MEDLINE]
J Steroid Biochem Mol Biol. 1994 Jan;48(1):55-60.
RU 58841, a new specific topical antiandrogen: a candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism.
Battmann T, Bonfils A, Branche C, Humbert J, Goubet F, Teutsch G, Philibert D.
Centre de Recherches Roussel Uclaf, Romainville, France.
A new topically active non-steroidal antiandrogen, RU 58841 has been synthesized. It displays high affinity for the hamster prostate and flank organ (F.O.) androgen receptors. In vivo, when topically applied, it exerts a potent dose-dependent regression of F.O. area at a dose as low as 1 microgram/animal while being devoid of antiandrogenic activity on deep accessory sex organs and of any effect on testosterone level up to 100 micrograms/animal. In the same species, after subcutaneous administration, it induces at the dose of 300 micrograms/animal, a small decrease in F.O. area equivalent to that of 1 microgram applied topically and a weak systemic activity. In intact rats, no effects were observed up to 1 microgram/animal whatever the route of administration. These results suggest that RU 58841 might useful for the topical treatment of androgen-dependent skin disorders such as acne, androgenetic alopecia and hirsutism.
PMID: 8136306 [PubMed - indexed for MEDLINE]
M question is,where can I buy such a liposomal carrier for RU?
I have RU sitting in my freezer and I'll provide a log with pics on this board when I get the carrier....
J Pharm Sci. 1997 May;86(5):573-8.
Importance of sebaceous glands in cutaneous penetration of an antiandrogen: target effect of liposomes.
Bernard E, Dubois JL, Wepierre J.
Laboratoire de dermophamacologie, Faculté de Pharmacie, Châtenay-Malabry, France.
The significance of the sebaceous gland pathway in the cutaneous permeation of an antiandrogen, 4-[3-(4-hydroxybutyl)-4,4-dimethyl -2,5-dioxo-1-imidazolidinyl]-2-(trifluoromethyl)benzonitrile (RU 58841), was studied with normal hairless rat skin and an induced scar hairless rat skin without sebaceous glands. RU 58841 was dissolved in an alcoholic solution and encapsulated in liposomes for comparison. After 24 h, the cumulative percentage of RU 58841 absorbed in vitro was 3-4-fold higher in the normal skin than in the scar skin; in the case of liposomes, the accumulation of the drug in the normal dermis was significantly higher than in the scar one. In the in vivo cutaneous distribution, the epidermis and dermis of the normal skin contained higher amounts of RU 58841 than the scar skin (ninefold with the solution and 16-fold with liposomes). An autoradiography study showed that with the solution, the drug was mainly localized in the stratum corneum/epidermis, and with the liposomes, the drug was mainly localized in the sebaceous glands. We concluded that the sebaceous glands constituted the main pathway for RU 58841. The alcoholic solution encouraged the localization of the drug into the stratum corneum, whereas liposomes targeted the sebaceous glands.
PMID: 9145381 [PubMed - indexed for MEDLINE]
Expert Opin Drug Deliv. 2008 Jun;5(6):665-79.
Novel vesicular and particulate drug delivery systems for topical treatment of acne.
Castro GA, Ferreira LA.
Federal University of Minas Gerais, Department of Pharmaceutics, 31270-901, Belo Horizonte, Minas Gerais, Brazil.
BACKGROUND: The efficacy of the antiacne topical drugs is well established. The local side effects, however, mainly cutaneous irritation, erythema, dryness, peeling and scaling, remain major problems. Novel vesicular and particulate drug delivery systems have been proposed to reduce the side effects of drugs commonly used in the topical treatment of acne. OBJECTIVE: This review focuses on the development and evaluation of antiacne drug-loaded vesicular and particulate delivery systems (liposomes, polymeric microspheres and solid lipid nanoparticles) for topical treatment, their advantages and challenges. METHODS: All the literature available was reviewed to highlight the potential of these novel systems for the topical treatment of acne. CONCLUSION: The encapsulation of antiacne drugs in vesicular and particulate delivery systems represents an innovative alternative to minimize side effects, while preserving their efficacy. This can be obtained by the capacity of these systems to provide controlled release or to improve the drug penetration into skin or even into the pilosebaceous unit.
PMID: 18532922 [PubMed - indexed for MEDLINE]
Ann N Y Acad Sci. 1995 Jun 12;761:56-65.
Local inhibition of sebaceous gland growth by topically applied RU 58841.
Matias JR, Gaillard M.
Nova Biosciences, Norrie Point Research Station, Staatsburg, New York 12553, USA.
The biological activity of a series of nonsteroidal, pure androgen receptor inhibitors was compared using the Syrian hamster ear skin sebaceous gland model. RU 58841, RU 56187, RU 38882 and cyproterone acetate were applied topically for 4 weeks on the ventral ear pinna of sexually mature male Syrian hamsters. Their order of efficacy was as follows: RU 58841 > RU 56187 > RU 38882 > cyproterone acetate. Maximal reduction of 60% in the size of the sebaceous glands was observed in hamsters treated with RU 58841 at a dose of 10 micrograms per day. This degree of inhibition occurred without any systemic side effects as shown by the absence of inhibition on the contralateral untreated ear pinna. Longer treatment did not produce greater inhibition since extending the treatment period from 4 weeks to 12 weeks showed similar data. The effect of RU 58841 was reversible since the inhibited sebaceous glands returned to normal size within 4 weeks after the cessation of the topical applications. The potent localized inhibition of sebaceous glands by RU 58841 demonstrates the excellent potential of this compound as a topical drug for the treatment of acne and other androgen-mediated disorders.
PMID: 7625751 [PubMed - indexed for MEDLINE]
J Steroid Biochem Mol Biol. 1994 Jan;48(1):55-60.
RU 58841, a new specific topical antiandrogen: a candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism.
Battmann T, Bonfils A, Branche C, Humbert J, Goubet F, Teutsch G, Philibert D.
Centre de Recherches Roussel Uclaf, Romainville, France.
A new topically active non-steroidal antiandrogen, RU 58841 has been synthesized. It displays high affinity for the hamster prostate and flank organ (F.O.) androgen receptors. In vivo, when topically applied, it exerts a potent dose-dependent regression of F.O. area at a dose as low as 1 microgram/animal while being devoid of antiandrogenic activity on deep accessory sex organs and of any effect on testosterone level up to 100 micrograms/animal. In the same species, after subcutaneous administration, it induces at the dose of 300 micrograms/animal, a small decrease in F.O. area equivalent to that of 1 microgram applied topically and a weak systemic activity. In intact rats, no effects were observed up to 1 microgram/animal whatever the route of administration. These results suggest that RU 58841 might useful for the topical treatment of androgen-dependent skin disorders such as acne, androgenetic alopecia and hirsutism.
PMID: 8136306 [PubMed - indexed for MEDLINE]
