Elastic liposomes bearing meloxicam-beta-cyclodextrin for transdermal delivery.
Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar [M. P.] 470003, India.Current Drug Delivery (Impact Factor: 1.48). 07/2008; 5(3):207-14.
The ultra-flexible lipid vesicles, the elastic liposomes bearing meloxicam-beta-cyclodextrin complex were prepared for its topical administration with the aim of simultaneously exploiting the favorable properties of both the carriers. The prepared meloxicam-beta-cyclodextrin complex was evaluated using DSC, XRD and FT-IR, which indicates the formation of inclusion complex in a molar ratio of 1:2 of meloxicam and beta-cyclodextrin (beta-CD). The elastic liposomes were prepared by conventional rotary evaporation method and characterized for various parameters such as vesicle shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, stability and in-vitro release pattern. Permeability studies of meloxicam and meloxicam-beta-cyclodextrin complex, as such or incorporated in elastic liposomes performed both across artificial membranes and rat skin highlighted a favorable effect of cyclodextrin on drug permeation rate, due to its solubilizing action. Moreover skin-permeation enhancer property of elastic liposomes has been evidenced. Skin permeation potential of the developed formulation was assessed using confocal laser scanning microscopy (CLSM), which revealed an enhanced permeation of the formulation to the deeper layers of the skin (up to 160 microm) following channel like pathways. Skin permeation profile of elastic liposomal formulation bearing meloxicam-beta-cyclodextrin complex was observed and the investigations revealed an enhanced transdermal flux (12.48+/-0.9 microg/cm(2)/h) and decreased lag time (0.7 h) for meloxicam. The obtained flux was nearly 1.4 and 9.1 times higher than elastic liposomal formulation bearing meloxicam and plain drug solution, respectively (P<0.005). The results indicate that the elastic liposomes may be promising vehicles for the transdermal delivery of meloxicam.
Article: Intradermal microdialysis[Show abstract] [Hide abstract]
ABSTRACT: Intradermal microdialysis permits us to measure the concentration in dermis of drugs applied to the skin. Microdialysis is especially efficient in sampling water-soluble molecules. Consequently, it appears particularly suitable to study current based delivery systems like iontophoresis that deliver ions or highly polar molecules. The purpose of this work was to evaluate the adequacy of a skin microdialysis technique to characterize and quantify the dermatopharmacokinetics of iontophoretically delivered propranolol in the dermis of healthy human volunteers. Linear microdialysis probes were inserted in the subject’s forearm skin and an iontophoresis device was installed above them. Constant current was applied for two periods of 1 h each separated by a 1-h interval. Dialysate samples were collected every 6 min for 4.4 h and analyzed by HPLC. Probes were always placed in the dermis as measured by ultrasonography. Propranolol was detectable in the dialysate. It was possible to build detailed concentration vs. midtime profiles that mirrored the current applied. Elimination rate from the dermis had first-order kinetics and was similar in all subjects. Quantification of the absorption process, indexed by lag-time and area under the concentration curve showed a high inter- and intrasubject variability that did not correlate with probe depth.
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ABSTRACT: This work was focused on the loading of benzophenone-3 in elastic liposomes composed of egg phosphatidylcholine and cholesterol, prepared by the Bangham method. Samples were characterized in terms of particle size, polydispersity index (PI), zeta potential, encapsulation efficiency and in vitro photoprotection properties. The extrusion of liposomes loading benzophenone-3 produced reduced-size (100 nm) elastic liposomes with a PI of 0.2. The active was loaded with a concentration of 20.34% (m/m) revealing changes in the ultraviolet properties after loading. On the basis of these results, it can be anticipated that liposomes are able to improve sun protector factor in vitro compared the free active.
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ABSTRACT: Introduction: With the incorporation of edge activators into the lipid bilayer structure, elasticity properties are given to liposomes. Regardless of the debate over the precise permeation mechanism of elastic liposomes, these vesicles have been proven to enhance drug permeation into or through skin in most cases. Areas covered: This article provides an overview of the formulation ingredients of elastic liposomes and their relationship with skin permeation behavior. The ingredients are divided into two categories of basic and optional ingredients. The effect of stability on permeation behavior of the vesicles is highlighted. Expert opinion: More attention should be paid to the stability of elastic liposomes. The different stability properties of the elastic liposomes following administration can induce different skin permeation behaviors of the vesicles. It is necessary to select the optimum composition of the elastic liposomes in order to control the stability and permeation behavior of the vesicles into or through the skin. Moreover, for the development of elastic liposomes, particular attention should also be paid to the drug leakage from the vesicles during long-term storage. The application of optional ingredients to improve the stability and/or elasticity of the elastic liposomes is becoming a new trend.
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