title: Topical delivery of roxithromycin solid-state forms entrapped in vesicles.
abstract: 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.
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences (Pharmacen), North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Candice
authors.initials: C
authors.lastname: Csongradi
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences (Pharmacen), North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Jeanetta
authors.initials: J
authors.lastname: du Plessis
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences (Pharmacen), North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Marique Elizabeth
authors.initials: ME
authors.lastname: Aucamp
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences (Pharmacen), North-West University, Private Bag X6001, Potchefstroom 2520, South Africa. Electronic address: Minja.Gerber@nwu.ac.za.
authors.forename: Minja
authors.initials: M
authors.lastname: Gerber
mesh_terms: D000287:Administration, Topical; D000900:Anti-Bacterial Agents / Q000008:administration & dosage*; D018699:Coated Vesicles; D003460:Crystallization; D004058:Diffusion; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems; D006801:Humans; D066298:In Vitro Techniques; D008081:Liposomes; D008826:Microbial Sensitivity Tests; D010316:Particle Size; D011425:Propionibacterium acnes / Q000187:drug effects; D015575:Roxithromycin / Q000008:administration & dosage*; D012867:Skin / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D008081:Liposomes; D015575:Roxithromycin
keywords: Amorphous; Pro-vesicles; Roxithromycin; Targeted delivery; Topical delivery; Vesicles