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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Bibliographic Details
Published in:International journal of pharmaceutics Vol. 393; no. 1; pp. 153 - 161
Main Authors: Klang, Victoria, Matsko, Nadejda, Zimmermann, Anna-Maria, Vojnikovic, Emina, Valenta, Claudia
Format: Journal Article
Language:English
Published: Amsterdam Elsevier B.V 30.06.2010
Elsevier
Subjects:
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
Online Access:Get full text
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Summary: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.
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ISSN:0378-5173
1873-3476
1873-3476
DOI:10.1016/j.ijpharm.2010.04.029