Hydrogels containing redispersible spray-dried melatonin-loaded nanocapsules: a formulation for transdermal-controlled d
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NANO EXPRESS
Open Access
Hydrogels containing redispersible spray-dried melatonin-loaded nanocapsules: a formulation for transdermal-controlled delivery Cristiane RD Hoffmeister1, Taís L Durli1, Scheila R Schaffazick2, Renata P Raffin1,3, Eduardo A Bender1, Ruy CR Beck1*, Adriana R Pohlmann1,4 and Sílvia S Guterres1
Abstract The aim of the present study was to develop a transdermal system for controlled delivery of melatonin combining three strategies: nanoencapsulation of melatonin, drying of melatonin-loaded nanocapsules, and incorporation of nanocapsules in a hydrophilic gel. Nanocapsules were prepared by interfacial deposition of the polymer and were spray-dried using water-soluble excipients. In vitro drug release profiles were evaluated by the dialysis bag method, and skin permeation studies were carried out using Franz cells with porcine skin as the membrane. The use of 10% (w/v) water-soluble excipients (lactose or maltodextrin) as spray-drying adjuvants furnished redispersible powders (redispersibility index approximately 1.0) suitable for incorporation into hydrogels. All formulations showed a better controlled in vitro release of melatonin compared with the melatonin solution. The best controlled release results were achieved with hydrogels prepared with dried nanocapsules (hydrogels > redispersed dried nanocapsules > nanocapsule suspension > melatonin solution). The skin permeation studies demonstrated a significant modulation of the transdermal melatonin permeation for hydrogels prepared with redispersible nanocapsules. In this way, the additive effect of the different approaches used in this study (nanoencapsulation, spray-drying, and preparation of semisolid dosage forms) allows not only the control of melatonin release, but also transdermal permeation. Keywords: Hydrogels, Maltodextrin, Melatonin, Nanocapsules, Spray-drying, Lactose, Skin permeation, Transdermal delivery
Background Melatonin (N-acetyl-5-methoxytryptamine) is a hormone secreted by the pineal gland of mammals at nighttime, and it is involved in the regulation of the sleep-wake cycle as well as in several biological functions, including the regulation of mood, the control of seasonal reproduction, and the circadian rhythm, in animals and humans. The administration of dosage forms containing exogenous melatonin has been used to treat circadian rhythm disorders such as jet lag and insomnia [1]. Besides being a potent antioxidant, melatonin is a free scavenger [1,2]; it protects against lipid peroxidation in several models [3] and against oxidative stress in * Correspondence: [email protected] 1 Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Av. 2752, Porto Alegre, CEP 90610-000, Brazil Full list of author information is available at the end of the article
some neurodegenerative diseases such as Alzheimer's disease [1,4]. Furthermore, it protects against ischemia/ reperfusion injury [5] and has antitumor activity [6]. Melatonin has a very short half-life and low and variable oral bioav
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