Investigation of the factors influencing the incorporation of clotrimazole in SLN and NLC prepared by hot high-pressure homogenization.
Clotrimazole, a fungicidal effective for the local treatment of cutaneous and mucosal infections, was incorporated into solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). The aim was to increase its dermal bioavailability and to control drug release, thereby potentially reducing its side effects. Prior to the release studies, the carrier was optimized and characterized by using different techniques. Laser diffractometry (LD), photon correlation spectroscopy (PCS) and scanning electron microscopy (SEM) indicated that SLN were spherical in shape with a mean size of approximately 400 nm. Some aggregation phenomena occurred during preparation of SEM samples due to the lipid character of the carriers. No physico-chemical instability of the drug-loaded lipid nanoparticles was detected during 2 years of storage at different temperatures. X-ray and DSC results suggested that during storage time the drug remained molecularly dispersed in the lipid matrix. Drug associated to SLN and NLC in its crystal form could be excluded.
Souto
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EB
Department of Pharmaceutical Technology, Biotechnology & Quality Management, The Free University of Berlin, Berlin, Germany.
Müller
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RH
D000935:Antifungal Agents / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D003022:Clotrimazole / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods*; D004356:Drug Storage; D008055:Lipids / Q000737:chemistry; D053758:Nanoparticles; D049329:Nanostructures / Q000737:chemistry; D011312:Pressure; D013696:Temperature; D014961:X-Ray Diffraction
D000935:Antifungal Agents; D004337:Drug Carriers; D008055:Lipids; D003022:Clotrimazole