Interaction of a lecithin microemulsion gel with human stratum corneum and its effect on transdermal transport

Dreher, Frank; Walde, Peter; Walther, Paul; Wehrli, E.

doi:10.1016/s0168-3659(96)01559-3

Cited by 176 publications

(98 citation statements)

References 28 publications

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“…Although the physicochemical properties of 5-FU, a BCS class III drug, highly water soluble, possessing a log P value of −0.78 are not suitable for dermal partitioning, the results indicate that a more effective skin penetration of 5-FU can be achieved using ME carrier. Different mechanisms can be stated to explain the enhanced transdermal drug delivery which include the penetration-enhancing effect of the ME components (42). Firstly, in the present study, IPM which was used as the oil phase for the ME is a penetration enhancer and it penetrates within lipid bilayers of the stratum corneum by disrupting their order and arrangement and results in drug permeation through it (43).…”

Section: Microemulsion Stability Studiesmentioning

confidence: 84%

Development of Novel Ionic Liquid-Based Microemulsion Formulation for Dermal Delivery of 5-Fluorouracil

et al. 2014

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Abstract. The present study was aimed at synthesizing an imidazole-based ionic liquid 1-butyl-3-methylimidazolium bromide (BMIMBr) and subsequent development of a novel ionic liquid-in-oil (IL/o) microemulsion (ME) system for dermal delivery of a poorly permeating drug 5-fluorouracil (5-FU). A significant enhancement in the solubility of 5-FU was observed in BMIMBr. IL/o MEs of 5-FU were prepared using isopropyl myristate, Tween 80/Span 20, and BMIMBr. Results of ex vivo skin permeation studies through mice skin indicated that the selected IL/o ME exhibited 4-fold enhancement in percent drug permeation as compared to aqueous solution, 2.3-fold as compared to hydrophilic ointment, and 1.6-fold greater permeation than water in oil (w/o) ME. The results of in vivo studies against dimethylbenz(a)anthracene (DMBA)/12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mice skin carcinogenesis demonstrated that the IL/o ME could effectively treat skin cancer in 4 weeks. In addition, the side effects such as erythema and irritation associated with the conventional formulations were not observed. Histopathological studies showed that the use of IL/o ME caused no anatomic and pathological changes in the skin structure of mice. These studies suggest that the use of IL-based ME system can efficiently enhance the solubility and permeability of 5-FU and hence its therapeutic efficacy.KEY WORDS: 5-fluorouracil; dermal delivery; ionic liquids; ionic liquid in oil (IL/o) microemulsion; skin cancer.

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Section: Microemulsion Stability Studiesmentioning

confidence: 84%

Development of Novel Ionic Liquid-Based Microemulsion Formulation for Dermal Delivery of 5-Fluorouracil

et al. 2014

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“…In the last decade, studies suggested that phospholipid microemulsions produce enhanced transdermal flux for oilsoluble drugs (Dreher et al, 1997;Paolino et al, 2002;Peltola et al, 2003). However, the potential of phospholipidbased microemulsion have never been explored in cutaneous delivery of local anesthetics.…”

Section: Introductionmentioning

confidence: 99%

Phospholipid microemulsion-based hydrogel for enhanced topical delivery of lidocaine and prilocaine: QbD-based development and evaluation

et al. 2014

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Topical delivery of local anesthetics has been an area of interest for researchers considering the barrier properties of skin and unfavorable physicochemical properties of drugs. In the present study, efforts have been made to modify the in vivo efficacy of eutectic mixture of lidocaine and prilocaine by exploiting the phospholipid modified microemulsion based delivery systems. The strategic QbD (D-optimal mixture design) enabled systematic optimization approach, after having obtained the isotropic area of interest by ternary phase diagram, has resulted into the system with most desirable attributes. Latter include nano-scale, globular structures with an average size of 40.6 nm, as characterized by TEM and DLS. The optimized microemulsion systems in gel dosage forms revealed the better permeability over commercial cream (CC) through abdominal rat skin. Enhancement in the flux from M OPT-NMP gel was 3.22-folds for prilocaine and 4.94-folds for lidocaine, in comparison to that of CC. This enhanced skin permeability is very well reflected in the in vivo studies, wherein intensity and duration of action was augmented significantly. The skin compliance of the optimized formulation was revealed in histopathological studies. The overall benefit relating to efficacy and safety-compliance could be correlated to the uniqueness of the carriers, composed of phospholipids and other components. Hence, the developed phospholipid-microemulsion based gel formulation has been proposed as more useful alternative for the topical delivery of lidocaine and prilocaine.

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“…For FLs, the peak observed at 2924 cm −1 was attributed to methylene C−H antisymmetric stretching, and the peak at 1087 cm −1 was due to the P−O of SPC. 31,32 The FT-IR spectra of SLs showed vibrational absorption bands centered around 1080 cm …”

Section: Results and Discussion Preparation And Characterization Of Cmentioning

confidence: 99%

Silica-coated flexible liposomes as a nanohybrid delivery system for enhanced oral bioavailability of curcumin

Li¹,

Zhang²,

Su³

et al. 2012

IJN

105

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Abstract:We investigated flexible liposomes as a potential oral drug delivery system. However, enhanced membrane fluidity and structural deformability may necessitate liposomal surface modification when facing the harsh environment of the gastrointestinal tract. In the present study, silica-coated flexible liposomes loaded with curcumin (CUR-SLs) having poor water solubility as a model drug were prepared by a thin-film method with homogenization, followed by the formation of a silica shell by the sol-gel process. We systematically investigated the physical properties, drug release behavior, pharmacodynamics, and bioavailability of CUR-SLs. CURSLs had a mean diameter of 157 nm and a polydispersity index of 0.14, while the apparent entrapment efficiency was 90.62%. Compared with curcumin-loaded flexible liposomes (CURFLs) without silica-coatings, CUR-SLs had significantly higher stability against artificial gastric fluid and showed more sustained drug release in artificial intestinal fluid as determined by in vitro release assays. The bioavailability of CUR-SLs and CUR-FLs was 7.76-and 2.35-fold higher, respectively, than that of curcumin suspensions. Silica coating markedly improved the stability of flexible liposomes, and CUR-SLs exhibited a 3.31-fold increase in bioavailability compared with CUR-FLs, indicating that silica-coated flexible liposomes may be employed as a potential carrier to deliver drugs with poor water solubility via the oral route with improved bioavailability.

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Interaction of a lecithin microemulsion gel with human stratum corneum and its effect on transdermal transport

Cited by 176 publications

References 28 publications

Development of Novel Ionic Liquid-Based Microemulsion Formulation for Dermal Delivery of 5-Fluorouracil

Development of Novel Ionic Liquid-Based Microemulsion Formulation for Dermal Delivery of 5-Fluorouracil

Phospholipid microemulsion-based hydrogel for enhanced topical delivery of lidocaine and prilocaine: QbD-based development and evaluation

Silica-coated flexible liposomes as a nanohybrid delivery system for enhanced oral bioavailability of curcumin

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