| Topical buparvaquone formulations for the treatment of cutaneous leishmaniasis. | |
| | |
MedLine Citation:
|
PMID: 17227619 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
As the part of a study to develop buparvaquone (BPQ) formulations for the treatment of cutaneous leishmaniasis, the topical delivery of BPQ and one of its prodrugs from a range of formulations was evaluated. In previous studies, BPQ and its prodrugs were shown to be potent antileishmanials in-vitro, with ED50 values in the nanomolar range. 3-Phosphono-oxymethyl-buparvaquone (3-POM-BPQ) was the most potent antileishmanial and was chosen, together with the parent drug, for further investigation. The ability of the parent and prodrug formulations to cross human and murine skin was tested in-vitro using the Franz diffusion cells. Formulations intended for topical application containing either BPQ or 3-POM-BPQ were developed using excipients that were either acceptable for topical use (GRAS or FDA inactive ingredients) or currently going through the regulatory process. BPQ was shown to penetrate both human epidermal membranes and full thickness BALB/c skin from a range of formulations (gels, emulsions). Similarly, 3-POM-BPQ penetrated full-thickness BALB/c skin from several gel formulations. In-vitro binding studies showed that BPQ bound melanin in a dose-dependent manner and preferably bound to delipidized skin over untreated BALB/c skin (on a weight to weight basis). The results confirm that BPQ and its prodrug 3-POM-BPQ can penetrate the skin from several formulations, making them potentially interesting candidates for further investigation of topical formulations using in-vivo models of cutaneous leishmaniasis. |
| | |
Authors:
|
Tracy Garnier; Antti Mäntylä; Tomi Järvinen; M Jayne Lawrence; Marc B Brown; Simon L Croft |
Related Documents
:
|
1895329 - The macaque model for in vitro fertilization: superovulation techniques and ultrasound-... 17981269 - Gonadotropin-releasing hormone agonist combined with a reduced dose of human chorionic ... 15955359 - The effect of gamete co-incubation time during in vitro fertilization with frozen-thawe... 16450409 - Mitochondrial organization in prepubertal goat oocytes during in vitro maturation and f... 16799739 - Correlation between number of retrieved oocytes and pregnancy rate after in vitro ferti... 9259959 - The human oocyte. genetic aspects. 8174719 - Serum progesterone predicts abnormal gestations in clomiphene citrate conception cycles... 14767249 - Interaction of step length and step rate during sprint running. 1172369 - Vitamin a transport in human fetal blood. |
Publication Detail:
|
Type: In Vitro; Journal Article |
Journal Detail:
|
Title: The Journal of pharmacy and pharmacology Volume: 59 ISSN: 0022-3573 ISO Abbreviation: J. Pharm. Pharmacol. Publication Date: 2007 Jan |
Date Detail:
|
Created Date: 2007-01-17 Completed Date: 2007-04-03 Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 0376363 Medline TA: J Pharm Pharmacol Country: England |
Other Details:
|
Languages: eng Pagination: 41-9 Citation Subset: IM |
Affiliation:
|
School of Pharmacy, University of Hertfordshire, College Lane, Hatfield AL10 9AB, UK. t.garnier@herts.ac.uk |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Administration, Cutaneous Animals Antiprotozoal Agents / chemistry, metabolism* Chemistry, Pharmaceutical Ethanol / chemistry Female Humans Leishmaniasis, Cutaneous Melanins / metabolism Mice Mice, Inbred BALB C Myristates / chemistry Naphthoquinones / chemistry, metabolism* Phosphoric Acid Esters / chemistry, metabolism* Polyethylene Glycols / chemistry Prodrugs / chemistry, metabolism* Propylene Glycol / chemistry Skin / metabolism Skin Absorption* |
| Chemical | |
Reg. No./Substance:
|
0/3-phosphonooxymethylbuparvaquone; 0/Antiprotozoal Agents; 0/Melanins; 0/Myristates; 0/Naphthoquinones; 0/Phosphoric Acid Esters; 0/Polyethylene Glycols; 0/Prodrugs; 110-27-0/isopropyl myristate; 57-55-6/Propylene Glycol; 64-17-5/Ethanol; 88426-33-9/buparvaquone |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Modification of the crystal habit of celecoxib for improved processability.
Next Document: Image analysis by pulse coupled neural networks (PCNN)--a novel approach in granule size characteriz...