Literature DB >> 10888312

Pharmacologic response of a controlled-release PLGA formulation for the alpha-melanocyte stimulating hormone analog, Melanotan-I.

R Bhardwaj1, M E Hadley, R T Dorr, K Dvorakova, C Brooks, J Blanchard.   

Abstract

PURPOSE: The objective of this study was to evaluate in vitro and in vivo the melanogenic activity of one-month duration Melanotan-I (MT-I) implants prepared using poly (D,L lactide-co-glycolide) polymer.
METHODS: The biological activity of the samples of MT-I released in vitro from the non-irradiated or gamma irradiated implants was measured using a frog skin bioassay. The effect of MT-I on skin pigmentation was measured using a Chroma meter (reflectometer) after subcutaneous administration of implants containing 4 mg MT-I to guinea pigs. Eumelanin, the black/brown melanin pigment, was quantified in skin biopsies as pyrrole-2, 3, 5-tricarboxylic acid using HPLC.
RESULTS: The MT-I released in vitro from implants after 24 hours exhibited 100% melanotropic activity in frog skins compared to an identical concentration of a freshly prepared MT-I standard. The reflectance readings demonstrated a prolonged skin darkening for up to three months as evidenced by the decrease in the luminance values from 0 to -4.82. A 2.5-fold increase in eumelanin levels was observed after one month and the increased pigmentation lasted for 3 months.
CONCLUSIONS: The melanogenic response to MT-I implants persisted for three months and the increase in pigmentation, especially the increased eumelanin levels, could provide protection from ultraviolet radiation.

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Year:  2000        PMID: 10888312     DOI: 10.1023/a:1007525117894

Source DB:  PubMed          Journal:  Pharm Res        ISSN: 0724-8741            Impact factor:   4.200


  19 in total

1.  Effect of alpha- and betamelanocyte stimulating hormones on the skin colour of man.

Authors:  A B LERNER; J S MCGUIRE
Journal:  Nature       Date:  1961-01-21       Impact factor: 49.962

2.  Skin pigmentation and pharmacokinetics of melanotan-I in humans.

Authors:  S O Ugwu; J Blanchard; R T Dorr; N Levine; C Brooks; M E Hadley; M Aickin; V J Hruby
Journal:  Biopharm Drug Dispos       Date:  1997-04       Impact factor: 1.627

3.  A comparison of HPLC and bioassay methods for plasma melanotan-II (MT-II) determination: application to a pharmacokinetic study in rats.

Authors:  S O Ugwu; J Blanchard; L D Nguyen; M E Hadley; R T Dorr
Journal:  Biopharm Drug Dispos       Date:  1994-07       Impact factor: 1.627

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Review 5.  Current update and trends in melanin pigmentation and melanin biology.

Authors:  K Jimbow
Journal:  Keio J Med       Date:  1995-03

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Authors:  B A Gilchrest; H Y Park; M S Eller; M Yaar
Journal:  Photochem Photobiol       Date:  1996-01       Impact factor: 3.421

7.  Microanalysis of eumelanin and pheomelanin in hair and melanomas by chemical degradation and liquid chromatography.

Authors:  S Ito; K Fujita
Journal:  Anal Biochem       Date:  1985-02-01       Impact factor: 3.365

8.  [Nle4, D-Phe7]-alpha-MSH: a superpotent melanotropin with prolonged action on vertebrate chromatophores.

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Journal:  Comp Biochem Physiol A Comp Physiol       Date:  1985

9.  4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity.

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Journal:  Proc Natl Acad Sci U S A       Date:  1980-10       Impact factor: 11.205

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Authors:  J T Bagnara; J D Taylor; M E Hadley
Journal:  J Cell Biol       Date:  1968-07       Impact factor: 10.539

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  1 in total

Review 1.  Pharmacokinetics and Pharmacodynamics of Afamelanotide and its Clinical Use in Treating Dermatologic Disorders.

Authors:  Elisabeth I Minder; Jasmin Barman-Aksoezen; Xiaoye Schneider-Yin
Journal:  Clin Pharmacokinet       Date:  2017-08       Impact factor: 6.447

  1 in total

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