| Novel transdermal delivery of Timolol maleate using sugar esters: preclinical and clinical studies. | |
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MedLine Citation:
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PMID: 19126429 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The feasibility of matrix controlled transdermal patch based on sugar fatty acid ester (SE) as penetration and absorption enhancer containing Timolol maleate (TM) was investigated. The influence of fatty acid type, chain length and hydrophile-lipophile balance (HLB) on the in vitro drug release as well as its permeation across hairless rat skin were studied and compared aiming to select a patch formula for clinical performance. Skin irritation induced by SE patch was evaluated by visual scoring, color reflectance measurements and non-invasive transepidermal water loss (TEWL) technique. The results indicated that among different SEs tried, laurate SE with shorter fatty acid chain length and higher HLB value significantly increased the amount of TM liberated from the patch (99+/-2.1%) and its permeation across rat skin (86+/-4.3%). The total drug permeation and flux values were approximately 5-fold greater compared to SE free patch. The extent of absorption of TM-SE patch expressed by AUC was 64% larger as compared to the oral solution with steady plasma concentration over 18 h and relative bioavailability (F(rel)) of 163%. The developed patch was well tolerated by all the subjects with only moderate skin irritation, which was recovered in 24h after patch removal. The results are very encouraging and offer an alternative approach to maintain higher, prolonged and controlled blood level profile of the drug over 18-24h. |
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Authors:
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Hanan M El-Laithy |
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Publication Detail:
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Type: Journal Article Date: 2008-12-24 |
Journal Detail:
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Title: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V Volume: 72 ISSN: 1873-3441 ISO Abbreviation: Eur J Pharm Biopharm Publication Date: 2009 May |
Date Detail:
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Created Date: 2009-03-31 Completed Date: 2009-09-21 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9109778 Medline TA: Eur J Pharm Biopharm Country: Netherlands |
Other Details:
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Languages: eng Pagination: 239-45 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutics and Industrial Pharmacy, Cairo University, Cairo, Egypt. hmellaithy@soficom.com.eg |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Adrenergic beta-Antagonists / administration & dosage Animals Biological Availability Carbohydrates / chemistry Chromatography, High Pressure Liquid Drug Delivery Systems Esters / chemistry Hydrogen-Ion Concentration Rats Rats, Wistar Skin / drug effects* Time Factors Timolol / administration & dosage* Water / chemistry |
| Chemical | |
Reg. No./Substance:
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0/Adrenergic beta-Antagonists; 0/Carbohydrates; 0/Esters; 26839-75-8/Timolol; 7732-18-5/Water |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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