[PMID]: | 28119103 |
[Au] Autor: | Csongradi C; du Plessis J; Aucamp ME; Gerber M |
[Ad] Endereço: | Centre of Excellence for Pharmaceutical Sciences (Pharmacen), North-West University, Private Bag X6001, Potchefstroom 2520, South Africa. |
[Ti] Título: | Topical delivery of roxithromycin solid-state forms entrapped in vesicles. |
[So] Source: | Eur J Pharm Biopharm;114:96-107, 2017 May. |
[Is] ISSN: | 1873-3441 |
[Cp] País de publicação: | Netherlands |
[La] Idioma: | eng |
[Ab] Resumo: | Recently, considerable interest developed in using newer/improved antibiotics for the treatment of Acne vulgaris. During this study, different roxithromycin solid-state forms (i.e. crystalline and amorphous) were encapsulated into vesicle systems (niosomes, proniosomes, ufosomes and pro-ufosomes) for dermis targeted delivery. Characterization of the vesicles was done with transmission electron microscopy, light microscopy, droplet size, droplet size distribution, pH, zeta-potential and entrapment efficiency percentage. Finally, comparative release and topical diffusion studies were performed, to evaluate if targeted topical delivery was obtained and if the roxithromycin solid-state amorphous forms resulted in improved topical delivery. Vesicle systems containing different roxithromycin (2%) solid-state forms were successfully prepared and characterized. The vesicles showed optimal properties for topical delivery. All carrier systems had topical delivery to the epidermis-dermis, whilst no roxithromycin was found in the receptor compartment or stratum corneum-epidermis. The niosomes were the leading formulation and the two amorphous forms had better topical delivery than the crystalline form. Successful targeted delivery of roxithromycin was obtained in the dermis, where the activity against Propionibacterium acnes is needed. The amorphous forms seemed to have held their solid-state form during formulation and in the vesicles, showing improved topical delivery in comparison to the crystalline form. |
[Mh] Termos MeSH primário: |
Antibacterianos/administração & dosagem Roxitromicina/administração & dosagem
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[Mh] Termos MeSH secundário: |
Administração Tópica Vesículas Revestidas Cristalização Difusão Portadores de Fármacos Composição de Medicamentos Sistemas de Liberação de Medicamentos Seres Humanos Técnicas In Vitro Lipossomos Testes de Sensibilidade Microbiana Tamanho da Partícula Propionibacterium acnes/efeitos dos fármacos Pele/metabolismo
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[Pt] Tipo de publicação: | JOURNAL ARTICLE |
[Nm] Nome de substância:
| 0 (Anti-Bacterial Agents); 0 (Drug Carriers); 0 (Liposomes); 21KOF230FA (Roxithromycin) |
[Em] Mês de entrada: | 1708 |
[Cu] Atualização por classe: | 170815 |
[Lr] Data última revisão:
| 170815 |
[Sb] Subgrupo de revista: | IM |
[Da] Data de entrada para processamento: | 170126 |
[St] Status: | MEDLINE |
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