Influence of monoolein on progesterone transdermal delivery

Abstract

This work aimed to investigate in vitro the influence of monoolein (MO) on progesterone (PG) transdermal delivery and skin retention. Information about the role of MO as an absorption enhancer for lipophilic molecules can help on innovative product development capable of delivering the hormone through the skin in a consistent manner, improving transdermal therapy of hormonal replacement. MO was dispersed in propylene glycol under heat at concentrations of 0% (control), 5% w/w, 10% w/w and 20% w/w. Then, 0.6% of PG (w/w) was added to each formulation. Permeation profile of the hormone was determined in vitro for 48 h using porcine skin in Franz diffusion cells. PG permeation doubled when 5% (w/w) of MO was present in formulation in comparison to both the control and higher MO concentrations (10% and 20% w/w). An equal trend was observed for PG retention in stratum corneum (SC) and reminiscent skin (E+D). PG release rates from the MO formulations, investigated using cellulose membranes, revealed that concentrations of MO higher than 5% (w/w) hindered PG release, which indeed negatively reflected on the hormone permeation through the skin. In conclusion, this work demonstrated the feasibility of MO addition (at 5% w/w) in formulations as a simple method to increase transdermal PG delivery for therapies of hormonal replacement. In contrast, higher MO concentrations (from 10% to 20% w/w) can control active release, and this approach could be extrapolated to other lipophilic, low-molecular-weight molecules.Uniterms: Monoolein/influence/transdermal therapy. Progesterone/transdermal delivery. Progesterone/ skin retention. Hormonal replacement/transdermal therapy. Skin permeation.Este trabalho teve como objetivo investigar in vitro a influência de monooleína (MO) na permeação transdérmica de progesterona (PG), bem como sobre a retenção cutânea desse hormônio a fim de (i) liberar de maneira mais consistente hormônio através da pele para melhorar a terapia transdérmica de reposição hormonal e (ii) trazer mais informações sobre o papel da MO como promotor da absorção cutânea de moléculas lipofílicas, tema ainda pouco explorado na literatura. MO foi dispersa em propilenoglicol, a concentrações de 0% (controle), 5%, 10% e 20% (p/p). Adicionou-se, em seguida, 0,6% (p/p) de PG a cada uma das formulações. O perfil de permeação do hormônio foi então determinado in vitro durante 48 h, utilizando pele de porco em células de difusão do tipo Franz. MO a 5% (p/p) foi capaz de duplicar a permeação de PG em comparação ao controle e às concentrações mais elevadas de MO, assim como a retenção de PG no estrato córneo (SC) e epiderme e derme remanescentes (E+D). A velocidade de liberação de PG a partir das formulações foi investigada usando membranas de celulose e este estudo revelou que concentrações de MO superiores a 5% (p/p) impediram a liberacão de PG, o que de fato refletiu de forma negativa na permeação cutânea do hormônio. Concluindo, este trabalho demonstrou a viabilidade da adição de MO a uma formulação como um método simples para...

Monoolein Assisted Oil-Based Transdermal Delivery of Powder Vaccine

“…Furthermore, the amount of cyclosporin A in the receptor phase increased up to an MO concentration of 10% w / w , while it decreased at MO concentrations above 10% w / w . Another group reported that the steroid hormone progesterone was delivered into the skin by MO, and the permeability of progesterone decreased when the concentration of MO was higher than 5% w / w [ 11 ]. In our patch system, MO enhanced the skin permeation of OVA linearly up to 6% w / w .…”

“…Daily use causes no skin irritation when small amounts are applied. However, because of the high lipophilicity of MO, it has been used in combination with polyhydric alcohols such as propylene glycol [ 9 , 10 , 11 ], or in liquid crystal systems [ 12 , 13 ], and aqueous dispersions of liquid crystals [ 14 , 15 ]. Recently, an oil-based transdermal peptide vaccine delivery system has been reported, using a reverse micelle system composed of water, MO, isopropyl alcohol, and isopropyl myristate (IPM) (2/18/20/60, w / w ) [ 16 ].…”