In Vitro Skin Permeation and Retention of Paromomycin from Liposomes for Topical Treatment of the Cutaneous Leishmaniasis

Ferreira, Lisiane Seguti; Ramaldes, Gilson Andrade; Nunan, E. A.; Ferreira, Lucas Antônio Miranda

doi:10.1081/ddc-120030423

Cited by 66 publications

(38 citation statements)

References 18 publications

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“…Moreover, they are also able to increase the amount of drug deposited into the upper layers of the skin and have been demonstrated to lower systemic drug levels, as compared with conventional formulations containing the same drug (Elsayed et al, 2007). This makes them highly promising for improved drug delivery to the skin (Ferreira et al, 2004, Chen et al, 2013.…”

Section: Resultsmentioning

confidence: 99%

Development and optimization of a new processing approach for manufacturing topical liposomes-in-hydrogel drug formulations by dual asymmetric centrifugation

Ingebrigtsen

Škalko‐Basnet

Holsæter

2016

Drug Development and Industrial Pharmacy

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Objectives: The objective of the present study was to utilize dual asymmetric centrifugation (DAC) as a novel processing approach for the production of liposomes-in-hydrogel formulations. Materials and Methods:Lipid films of phosphatidylcholine, with and without chloramphenicol (CAM), were hydrated and homogenized by DAC to produce liposomes in the form of vesicular phospholipid gels with a diameter in the size range of 200-300 nm suitable for drug delivery to the skin. Different homogenization processing parameters were investigated along with the effect of adding propylene glycol (PG) to the formulations prior to homogenization. The produced liposomes were incorporated into a hydrogel made of 2.5 % (v/v) soluble β-1,3/1,6-glucan (SBG) and mixed by DAC to achieve a homogenous liposomes-inhydrogel-formulation suitable for topical application.Results and Discussion: CAM-containing liposomes with a vesicle diameter of 282 ± 30 nm and polydispersity index (PI) of 0.13 ± 0.02 were successfully produced by DAC after 50 minutes centrifugation at 3500 rpm, and homogenously (< 4 % content variation) incorporated into the SBG hydrogel. Addition of PG decreased the necessary centrifugation time to 2 minutes and 55 seconds, producing liposomes of 230 ± 51 nm and PI of 0.25 ± 0.04. All formulations had an entrapment efficiency of approximately 50%. Conclusions:We managed to develop a relatively fast and reproducible new method for the production of liposomes-in-hydrogel formulation by DAC.

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Section: Resultsmentioning

confidence: 99%

Development and optimization of a new processing approach for manufacturing topical liposomes-in-hydrogel drug formulations by dual asymmetric centrifugation

Ingebrigtsen

Škalko‐Basnet

Holsæter

2016

Drug Development and Industrial Pharmacy

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“…PM formulations have some disadvantages, including a short half-life in plasma and rapid renal excretion (being a hydrophilic molecule with high molecular weight). All these factors decrease the concentration of PM at the sites of action, e.g., the reduction of PM oral absorption, thus making the oral administration of PM inefficient (8,9,12,14). According to the data obtained from clinical trials, the effect of the topical form of PM for the treatment of cutaneous leishmaniasis has been promising, but due to the powerful barrier nature of the skin, it is not effective (16)(17)(18).…”

Section: Discussionmentioning

confidence: 99%

“…The lack of an effective drug against CL has recently prioritized the creation of new, alternative therapeutic drugs. To this end, various pharmaceutical formulations have been assessed for the treatment of CL (9,(13)(14)(15). The effects of the topical form of PM in clinical trials for the treatment of CL have been promising, but due to the powerful barrier nature of the skin, this form of PM is not always effective (16)(17)(18).…”

Section: Introductionmentioning

confidence: 99%

“…The effects of the topical form of PM in clinical trials for the treatment of CL have been promising, but due to the powerful barrier nature of the skin, this form of PM is not always effective (16)(17)(18). Lipid-based formulation of PM, i.e., liposomal PM, was prepared and its topical effects on the treatment of leishmaniasis evaluated (9,14). Recently, solid lipid nanoparticles (SLN) have received much attention due to advantages, such as low cost and safety, compared to other colloidal nanoparticles (19).…”

Section: Introductionmentioning

confidence: 99%

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Drug Targeting to Macrophages With Solid Lipid Nanoparticles Harboring Paromomycin: an In Vitro Evaluation Against L. major and L. tropica

et al. 2015

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Abstract. Leishmaniasis is a worldwide disease that leads to high mortality and morbidity in human populations. Today, leishmaniasis is managed via drug therapy. The drugs that are already in clinical use are limited to a number of toxic chemical compounds and their parasite drug resistance is increasing. It is therefore essential, in order to circumvent the current difficulties, to design a new anti-leishmanial drug treatment strategy. Besides producing new, active anti-leishmanial entities, another promising strategy could be developing novel delivery systems and formulations of the existing pharmaceutical ingredients to improve drug efficacy. In the present study, paromomycin sulfate (PM), as one of the promising antileishmanial drugs, was formulated in solid lipid nanoparticles (SLN), and its in vitro efficacy was investigated against different strains of Leishmania using a MTT test, Parasite-Rescue-Transformation-Assay, SYTO Green staining, and fluorescent microscope imaging. The results show that PM-loaded SLN is significantly more effective than PM in inhibiting parasite propagation (P<0.05) and that cytotoxicity of PM-SLN formulations is size dependent. According to our results, delivery of the drugs to the macrophages via nanoparticle utilization seems to be an accessible and practical approach.KEY WORDS: cutaneous leishmaniasis; drug delivery system; paromomycin sulfate; solid lipid nanoparticle.

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“…The use of colloidal systems, such as liposomes, can allow increased drug accumulation into the skin, depending on the type of drug, as well as on the characteristics of the nanocarrier. [13][14][15][16][17][18] The aim of this study was to develop a new aqueous formulation containing VK1 suitable to be administered by aerosol (with a portable device) on the skin. In particular, we investigated if a formulation based on liposomes could be used to overcome the low water solubility of VK1.…”

mentioning

confidence: 99%

Development of a liposome-based formulation for vitamin K1 nebulization on the skin

Campani

Marchese

Pitaro³

et al. 2014

IJN

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Vitamin K1 (VK1) is a very lipophilic and photosensitive molecule contained in some vegetables. Recently, the use of VK1 on the skin has been proposed for different pharmaceutical or cosmeceutical applications. In this study, an innovative strategy for the administration of VK1 on the skin was proposed. In particular, to overcome the drawbacks associated with a VK1-containing fatty ointment available on the market, an aqueous formulation suitable to be administered by nebulization was developed. The use of liposomes encapsulating VK1 enabled issues due to the lipophilicity of VK1 to be overcome. Thus, different liposomal formulations, with different VK1 concentrations, were prepared and characterized in terms of size, zeta potential, VK1 encapsulation into liposomes, and stability of the formulations during storage. After a first phase of screening, the selected formulation was tested by a portable device for nebulization. No alteration of the vesicle characteristics following the liposome supply through the nebulizer was found. Finally, permeation studies were carried out on pig-excised skin in Franz cells and the newly developed formulation was compared to a marketed VK1-containing ointment. In this test, an enhanced VK1 accumulation into the skin was found when using nebulized liposomes. In conclusion, in order to administer VK1 on the skin, the newly developed formulation could be a valid alternative to the products available on the market today. In particular, the use of liposomes could facilitate the multiple administrations per day by aerosol, but also increase, compared to a semi-solid preparation, the accumulation of VK1 into the epidermis and dermis

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In Vitro Skin Permeation and Retention of Paromomycin from Liposomes for Topical Treatment of the Cutaneous Leishmaniasis

Cited by 66 publications

References 18 publications

Development and optimization of a new processing approach for manufacturing topical liposomes-in-hydrogel drug formulations by dual asymmetric centrifugation

Development and optimization of a new processing approach for manufacturing topical liposomes-in-hydrogel drug formulations by dual asymmetric centrifugation

Drug Targeting to Macrophages With Solid Lipid Nanoparticles Harboring Paromomycin: an In Vitro Evaluation Against L. major and L. tropica

Development of a liposome-based formulation for vitamin K1 nebulization on the skin

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