Selective delivery of adapalene to the human hair follicle under finite dose conditions using polymeric micelle nanocarriers

Drug delivery systems that target the pilosebaceous unit (PSU) selectively could improve the clinical management of diseases that originate in the hair follicle. The aims of this study were (i) to prepare polymeric micelles using d-α-tocopheryl polyethylene glycol succinate diblock copolymer that in...

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Published in:Nanoscale 2018-01, Vol.10 (3), p.1099-1110
Main Authors: Kandekar, Somnath G, Del Río-Sancho, Sergio, Lapteva, Maria, Kalia, Yogeshvar N
Format: Article
Language:English
Subjects:
Acne
Adapalene - administration & dosage
Animals
Drug Delivery Systems
Drug dosages
Formulations
Gels
Hair
Hair Follicle - drug effects
Humans
Micelles
Nanoparticles
Polyethylene glycol
Polymers
Scanning microscopy
Skin
Skin Absorption
Skin Cream
Swine
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cited_by cdi_FETCH-LOGICAL-c315t-e29a2cee3f0f1cf5b2e3b6b1f04b0c327e5f717d20268ce43672a6c3b344e62f3
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creator Kandekar, Somnath G
Del Río-Sancho, Sergio
Lapteva, Maria
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description Drug delivery systems that target the pilosebaceous unit (PSU) selectively could improve the clinical management of diseases that originate in the hair follicle. The aims of this study were (i) to prepare polymeric micelles using d-α-tocopheryl polyethylene glycol succinate diblock copolymer that incorporated adapalene (ADA), a retinoid indicated for Acne vulgaris, and (ii) to investigate the feasibility of delivering ADA preferentially to the PSU under finite dose conditions - thereby better approximating actual conditions of use by patients. Incorporation of ADA into spherical micelles (d
doi_str_mv 10.1039/c7nr07706h
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The aims of this study were (i) to prepare polymeric micelles using d-α-tocopheryl polyethylene glycol succinate diblock copolymer that incorporated adapalene (ADA), a retinoid indicated for Acne vulgaris, and (ii) to investigate the feasibility of delivering ADA preferentially to the PSU under finite dose conditions - thereby better approximating actual conditions of use by patients. Incorporation of ADA into spherical micelles (d &lt;20 nm) increased aqueous solubility by ∼50 000-fold (from &lt;4 ng mL to 0.2 mg mL ). Optimized micelle solution and gel formulations (0.02% ADA) were stable after storage for 4 weeks at 4 °C. Finite dose experiments using full-thickness porcine and human skin revealed that ADA delivery efficiency from micelle solution and gel formulations was equivalent and was &gt;2- and 10-fold higher than that from Differin® gel and Differin® cream (products containing ADA at 0.1% (w/w)). Follicular delivery studies in human skin, using a punch biopsy technique to extract the intact PSU, demonstrated that the micelle solution and gel formulations did indeed enable preferential delivery of ADA to the PSU (4.5- and 3.3-fold higher, respectively, than that to PSU-free skin biopsies). Confocal laser scanning microscopy provided visual corroboration that ADA was uniformly distributed in the hair follicles. 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source Royal Society of Chemistry:Jisc Collections:Royal Society of Chemistry Read and Publish 2022-2024 (reading list)
subjects Acne
Adapalene - administration & dosage
Animals
Drug Delivery Systems
Drug dosages
Formulations
Gels
Hair
Hair Follicle - drug effects
Humans
Micelles
Nanoparticles
Polyethylene glycol
Polymers
Scanning microscopy
Skin
Skin Absorption
Skin Cream
Swine
title Selective delivery of adapalene to the human hair follicle under finite dose conditions using polymeric micelle nanocarriers
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