| Site-specific drug delivery to pilosebaceous structures using polymeric microspheres. | |
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MedLine Citation:
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PMID: 8302759 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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In order to improve the therapeutic index of adapalene, a new drug under development for the treatment of acne, site-specific delivery to the hair follicles using 50:50 poly(DL-lactic-co-glycolic acid) microspheres as particulate carriers was investigated in vitro and in vivo. The percutaneous penetration pathway of the microspheres was shown to be dependent on their mean diameter. Thus, after topical application onto hairless rat or human skin, adapalene-loaded microspheres (5-microns diameter) were specifically targeted to the follicular ducts and did not penetrate via the stratum corneum. The in vitro release of adapalene from the microspheres into artificial sebum at 37 degrees C was controlled and faster than the in vivo sebum excretion in humans. Aiming to reduce either the applied dose of drug or the frequency of administration, different formulations of adapalene-loaded microspheres were evaluated in vivo in the rhino mouse model. A dose-related comedolytic activity of topical formulations of adapalene-loaded microspheres was observed in this model. Furthermore, by applying a site-specific drug delivery system (0.1% adapalene) every other day or by administering a 10-fold less concentrated targeted formulation (0.01%) every day, a pharmacological activity equivalent to a daily application of an aqueous gel containing drug crystals (0.1% adapalene) was observed. Since an aqueous gel containing 10% adapalene-loaded microspheres was not irritating in a rabbit skin irritancy test, this formulation was applied onto forearms of human volunteers. Site-specific drug delivery was further evidenced by follicular biopsy. Since an aqueous gel containing 10% adapalene-loaded microspheres was not irritating in a rabbit skin irritancy test, this formulation was applied onto forearms of human volunteers. Site-specific drug delivery was further evidenced by follicular biopsy.(ABSTRACT TRUNCATED AT 250 WORDS) |
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Authors:
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A Rolland; N Wagner; A Chatelus; B Shroot; H Schaefer |
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Publication Detail:
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Type: In Vitro; Journal Article |
Journal Detail:
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Title: Pharmaceutical research Volume: 10 ISSN: 0724-8741 ISO Abbreviation: Pharm. Res. Publication Date: 1993 Dec |
Date Detail:
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Created Date: 1994-03-04 Completed Date: 1994-03-04 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8406521 Medline TA: Pharm Res Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 1738-44 Citation Subset: IM |
Affiliation:
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Cird Galderma, Sophia Antipolis, Valbonne, France. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Topical Animals Dermatologic Agents / administration & dosage, adverse effects, pharmacokinetics* Drug Carriers Female Hair / metabolism* Humans Irritants / adverse effects Lactic Acid* Male Mice Microspheres Naphthalenes / administration & dosage, adverse effects, pharmacokinetics* Polyglycolic Acid* Polymers Rabbits Rats Sebaceous Glands / metabolism* Skin / drug effects Skin Absorption / drug effects |
| Chemical | |
Reg. No./Substance:
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0/Dermatologic Agents; 0/Drug Carriers; 0/Irritants; 0/Naphthalenes; 0/Polymers; 0/polylactic acid-polyglycolic acid copolymer; 106685-40-9/adapalene; 26009-03-0/Polyglycolic Acid; 50-21-5/Lactic Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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