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      Design and evaluation of lidocaine- and prilocaine-coloaded nanoparticulate drug delivery systems for topical anesthetic analgesic therapy: a comparison between solid lipid nanoparticles and nanostructured lipid carriers

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          Topical anesthesia analgesic therapy has diverse applicability in solving the barrier properties of skin and unfavorable physicochemical properties of drugs. Lidocaine (LID) combined with prilocaine (PRI) has been used as a topical preparation for dermal anesthesia for treatment of conditions such as paresthesia.

          Materials and methods

          In this study, for combination anesthesia and overcoming the drawbacks of LID and PRI, respectively, LID- and PRI-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were prepared and characterized by determination of their particle size, drug loading capacity, stability, in vitro drug release behavior and in vitro cellular viability. Ex vivo skin permeation and in vivo anesthesia analgesic efficiency of these two systems were also evaluated and compared.


          Results revealed that combination delivery of the dual drugs exhibited more remarkable efficiency than signal drug-loaded systems. SLN systems have better ex vivo skin permeation ability than NLCs. NLC systems revealed a stronger in vivo anesthesia analgesic effect than SLN systems.


          It can be concluded that SLNs and NLCs have different advantages, and that both carriers are promising dual drug delivery systems for topical anesthetic analgesic therapy.

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          Most cited references 40

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          Particle size of liposomes influences dermal delivery of substances into skin.

           D. Verma (2003)
          In the present study, the influence of vesicle size on the penetration of two fluorescently labeled substances into the human skin was investigated. For the measurements either a hydrophilic fluorescent compound [carboxyfluorescein (CF)] or a lipophilic one [1,1'-dioctadecyl-3,3,3',3'-tertramethylindocarbo-cyanine perchlorate (DiI)] were encapsulated into vesicles. Liposomal formulations were prepared by extruding the vesicles through polycarbonate membrane filters with pores of different sizes. In vitro penetration studies into human abdominal skin were performed by using the Franz diffusion cell and a standardized skin stripping technique in attempt to find an optimum size for topical drug delivery by liposomes. Confocal laser scanning microscopy (CLSM) was used to visualize the effect of penetration ability of liposomal DiI. The maximum DiI fluorescence in the skin was observed with smaller liposomes of 71 nm diameter. The liposomes with a size of 120 nm diameter showed statistically enhanced penetration of CF into the skin as compared to larger ones. The results indicated that the CF penetration was inversely related to the size of the liposomes, which was confirmed by the data of the confocal laser scanning microscopy studies.
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            Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) for pulmonary application: a review of the state of the art.

            Drug delivery by inhalation is a noninvasive means of administration that has following advantages for local treatment for airway diseases: reaching the epithelium directly, circumventing first pass metabolism and avoiding systemic toxicity. Moreover, from the physiological point of view, the lung provides advantages for systemic delivery of drugs including its large surface area, a thin alveolar epithelium and extensive vasculature which allow rapid and effective drug absorption. Therefore, pulmonary application is considered frequently for both, the local and the systemic delivery of drugs. Lipid nanoparticles - Solid Lipid Nanoparticles and Nanostructured Lipid Carriers - are nanosized carrier systems in which solid particles consisting of a lipid matrix are stabilized by surfactants in an aqueous phase. Advantages of lipid nanoparticles for the pulmonary application are the possibility of a deep lung deposition as they can be incorporated into respirables carriers due to their small size, prolonged release and low toxicity. This paper will give an overview of the existing literature about lipid nanoparticles for pulmonary application. Moreover, it will provide the reader with some background information for pulmonary drug delivery, i.e., anatomy and physiology of the respiratory system, formulation requirements, application forms, clearance from the lung, pharmacological benefits and nanotoxicity.
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              Influence of curcumin-loaded cationic liposome on anticancer activity for cervical cancer therapy.

              The delivery of curcumin has been explored in the form of liposomal nanoparticles to treat various cancer cells. Since curcumin is water insoluble and an effective delivery route is through encapsulation in liposomes, which were modified with three components of DDAB, cholesterol and non-ionic surfactant. The purpose of this study was to establish a critical role of DDAB in liposomes containing curcumin at cellular response against two types of cell lines (HeLa and SiHa). Here, we demonstrate that DDAB is a potent inducer of cell uptake and cell death in both cell lines. The enhanced cell uptake was found on DDAB-containing liposome, but not on DDAB-free liposome. However, the cytotoxicity of DDAB-containing liposomes was high and needs to be optimized. The cytotoxicity of liposomal curcumin was more pronounced than free curcumin in both cells, suggesting the benefits of using nanocarrier. In addition, the anticancer efficiency and apoptosis effect of the liposomal curcumin formulations with DDAB was higher than those of DDAB-free liposomes. Therefore curcumin loaded liposomes indicate significant potential as delivery vehicles for the treatment of cervical cancers. Copyright © 2013 Elsevier B.V. All rights reserved.

                Author and article information

                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                18 September 2017
                : 11
                : 2743-2752
                [1 ]Department of Anesthesiology, Shandong Jining No 1 People’s Hospital, Shandong, People’s Republic of China
                [2 ]Department of Anesthesiology, Affiliated Hospital of Jining Medical College, Jining, Shandong, People’s Republic of China
                Author notes
                Correspondence: Chuanyu Chen, Department of Anesthesiology, Shandong Jining No 1 People’s Hospital, No 6 Jiankang Road, Jining, 272011, Shandong, People’s Republic of China. Email chencyjnph@ 123456163.com
                © 2017 You et al. This work is published and licensed by Dove Medical Press Limited

                The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

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