Enhancement of stability and skin permeation by sucrose stearate and cyclodextrins in progesterone nanoemulsions

Lecithin-based nanoemulsions are colloidal drug delivery systems which offer fundamental advantages in topical therapy, such as excellent skin permeation of lipophilic drugs; however, their physicochemical long-term stability is usually rather poor without the use of additional synthetic surfactants...

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Vydáno v:	International journal of pharmaceutics Ročník 393; číslo 1; s. 153 - 161
Hlavní autoři:	Klang, Victoria, Matsko, Nadejda, Zimmermann, Anna-Maria, Vojnikovic, Emina, Valenta, Claudia
Médium:	Journal Article
Jazyk:	angličtina
Vydáno:	Amsterdam Elsevier B.V 30.06.2010 Elsevier
Témata:	alpha-Cyclodextrins - pharmacology Animals beta-Cyclodextrins - pharmacology Biological and medical sciences Calorimetry, Differential Scanning Chemistry, Pharmaceutical Cryoelectron Microscopy Cyclodextrin Cyclodextrins - chemistry Cyclodextrins - pharmacology Drug Compounding Drug Stability Emulsions Excipients - chemistry Excipients - pharmacology gamma-Cyclodextrins - pharmacology General pharmacology Medical sciences Microscopy, Electron, Transmission Nanoemulsion Nanoparticles Permeability Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Progesterone Progesterone - chemistry Progesterone - metabolism Skin - drug effects Skin - metabolism Skin Absorption - drug effects Sphingosine - analogs & derivatives Sphingosine - chemistry Submicron emulsion Sucrose - analogs & derivatives Sucrose - chemistry Sucrose - pharmacology Sucrose stearate Surface Properties Swine Technology, Pharmaceutical - methods Time Factors Submicron emulsion Cyclodextrin Progesterone Nanoemulsion Sucrose stearate Stability Pharmaceutical technology Sucrose Permeation Stearate Progestagen Emulsion Oside polymer Skin Inclusion compound Sex steroid hormone Physicochemical properties
ISSN:	0378-5173, 1873-3476, 1873-3476
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Popis
Shrnutí:	Lecithin-based nanoemulsions are colloidal drug delivery systems which offer fundamental advantages in topical therapy, such as excellent skin permeation of lipophilic drugs; however, their physicochemical long-term stability is usually rather poor without the use of additional synthetic surfactants such as polysorbates. In a novel approach negatively and positively charged formulations were developed without the use of conventional synthetic surfactants. Natural substances such as sucrose esters and different cyclodextrins were additionally used as stabilising agents. Emphasis was laid on optimisation of the homogenisation process and formulation properties. The optimised formulations were tested for their potential as drug delivery systems for progesterone. Furthermore, crucial formulation parameters such as particle size and zeta potential were monitored for more than a year. In this context, the effect of the natural excipients sucrose stearate and cyclodextrins α, β and γ on in vitro skin permeation was investigated; the influence of the positive particle surface charge induced by incorporation of the cationic phytosphingosine was evaluated as well. The results showed that in particular the cyclodextrins seemed to induce fundamental changes in formulation microstructure as confirmed by cryo TEM, thus leading to remarkably increased skin permeation rates of progesterone compared to the control.
Bibliografie:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0378-5173 1873-3476 1873-3476
DOI:	10.1016/j.ijpharm.2010.04.029