Influence of nanocarrier type and size on skin delivery of hydrophilic agents

Küchler, Sarah; Abdel-Mottaleb, Mona M.A.; Lamprecht, Alf; Radowski, Michał R.; Haag, Rainer; Schäfer‐Korting, Monika

doi:10.1016/j.ijpharm.2009.04.046

Cited by 103 publications

(73 citation statements)

References 11 publications

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“…In these conditions, an increase of caffeine thermodynamic activity is observed so facilitating the delivery. Küchler et al (2009) are in agreement with this explanation and pointed out the main role of the lipid matrix of SLN to promote the skin penetration of hydrophilic drugs. Besides, the author stated that both size of nanocarriers and surfactant used for SLN stabilization appeared of subsidiary relevance for the enhancement of drug skin permeation.…”

Section: In Vitro Studysupporting

confidence: 89%

Design of solid lipid nanoparticles for caffeine topical administration

et al. 2014

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Caffeine is an interesting compound showing anticancer and protective effects upon topical administration, although its penetration through the skin is compromised by its hydrophilicity. Materials and methods: SLN-CAF were formulated by using a modification of the quasi-emulsion solvent diffusion technique (QESD) and characterized by PCS and DSC analyses. In vitro percutaneous absorption studies were effected using excised human skin membranes (i.e. Stratum Corneum Epidermis or SCE).Results: SLN-CAF were in a nanometric range (182.6 ± 8.4 nm) and showed an interesting payload value (75% ± 1.1). DSC studies suggest the presence of a well-defined system and the successful drug incorporation. Furthermore, SLN-CAF generated a significantly faster permeation than a control formulation over 24 h of monitoring. Discussion and conclusions: SLN-CAF were characterized by valid dimensions and a good encapsulation efficiency, although the active to incorporate showed a hydrophilic character. This result confirms the suitability of the formulation strategy employed in the present work. Furthermore, the in vitro evidence outline the key role of lipid nanoparticles in enhancing caffeine permeation through the skin.

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Section: In Vitro Studysupporting

confidence: 89%

Design of solid lipid nanoparticles for caffeine topical administration

et al. 2014

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“…Generally, it was concluded that smaller PS did not correspond to higher permeation and particles below 200 nm were sufficient for delivery to deeper layers. 11,34,35 In a recent study, it was shown that liposomes were shown to not penetrate below 5 μm in the SC; rather, they fused with the lipid layer inside the skin and released their cargo. 36 Moreover, extrusion method in liposome preparation is known to produce monodisperse particles, and PS is adjustable depending on the membrane pore size.…”

Section: Optimization Studymentioning

confidence: 99%

Design, optimization and characterization of coenzyme Q10- and D-panthenyl triacetate-loaded liposomes

Çelik¹,

Sagiroglu²,

Özdemir³

2017

IJN

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Coenzyme Q10 (CoQ10) is a lipid-soluble molecule found naturally in many eukaryotic cells and is essential for electron transport chain and energy generation in mitochondria. D-Panthenyl triacetate (PTA) is an oil-soluble derivative of D-panthenol, which is essential for coenzyme A synthesis in the epithelium. Liposomal formulations that encapsulate both ingredients were prepared and optimized by applying response surface methodology for increased stability and skin penetration. The optimum formulation comprised 4.17 mg CoQ10, 4.22 mg PTA and 13.95 mg cholesterol per 100 mg of soy phosphatidylcholine. The encapsulation efficiency of the optimized formulation for CoQ10 and PTA was found to be 90.89%±3.61% and 87.84%±4.61%, respectively. Narrow size distribution was achieved with an average size of 161.6±3.6 nm, while a spherical and uniform shape was confirmed via scanning electron microscopy and transmission electron microscopy images. Cumulative release of 90.93% for PTA and 24.41% for CoQ10 was achieved after 24 hours of in vitro release study in sink conditions. Physical stability tests indicated that the optimized liposomes were suitable for storage at 4°C for at least 60 days. The results suggest that the optimized liposomal formulation would be a promising delivery system for both ingredients in various topical applications.

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“…3) but overall at 46 h, ~26 % cumulative amount of ART (Fig. 4) had permeated irrespective of dose [43][44][45]. A control experiment employing only ART in solution was impossible due to insolubility of ART in water.…”

Section: Ex Vivo Skin Permeation Experimentsmentioning

confidence: 99%

Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application

Nnamani

Hansen

Windbergs

et al. 2014

International Journal of Pharmaceutics

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NLC topical formulation as an alternative to oral and parenteral (IM) delivery of artemether (ART), a poorly water-soluble drug was designed. A Phospholipon 85G-modified Gelucire 43/01 based NLC formulation containing 75 % Transcutol was chosen from DSC studies and loaded with gradient concentration of ART (100-750 mg). ART-loaded NLCs were stable (-22 to -40 mV), polydispersed (0.4 to 0.7) with d90 size distribution range of 247 to 530 nm without microparticles up to one month of storage. The encapsulation efficiency (EE %) for ART in the NLC was concentration independent as 250 mg of ART loading achieved ~61%. DSC confirmed molecular dispersion of ART due to low matrix crystallinity (0.028 J/g). Ex vivo study showed detectable ART amounts after 20 h which gradually increased over 48 h achieving ~26 % cumulative amount permeated irrespective of the applied dose. This proves that ART permeates excised human epidermis, where the current formulation served as a reservoir to gradually control drug release over an extended period of time. Full thickness skin study therefore may confirm if this is a positive signal to hope for a topical delivery system of ART.

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Influence of nanocarrier type and size on skin delivery of hydrophilic agents

Cited by 103 publications

References 11 publications

Design of solid lipid nanoparticles for caffeine topical administration

Design of solid lipid nanoparticles for caffeine topical administration

Design, optimization and characterization of coenzyme Q10- and D-panthenyl triacetate-loaded liposomes

Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application

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