ABSTRACT
In this study, we carried out extensive in vitro studies on various concentrations of tioxolone along with benzoxonium chloride and their niosomal forms against Leishmania tropica. Niosomes were prepared by the hydration method and were evaluated for morphology, size, release study, and encapsulation efficiency. This study measured leishmanicidal activity against promastigote and amastigote, apoptosis and gene expression levels of free solution and niosomal-encapsulated tioxolone along with benzoxonium chloride. Span/Tween 60 niosome had good physical stability and high encapsulation efficiency (more than 97%). The release profile of the entrapped compound showed that a gradual release rate. The combination of niosomal forms on promastigote and amastigote were more effective than glucantime. Also, the niosomal form of this compound was significantly less toxic than glucantime (P≤0.05). The flowcytometric analysis on niosomal form of drugs showed that higher number of early apoptotic event as the principal mode of action (89.13% in 200 μg/ml). Also, the niosomal compound increased the expression level of IL-12 and metacaspase genes and decreased the expression level of the IL-10 gene, which further confirming the immunomodulatory role as the mechanism of action. We observed the synergistic effects of these 2 drugs that induced the apoptotic pathways and also up regulation of an immunomodulatory role against as the main mode of action. Also, niosomal form of this combination was safe and demonstrated strong anti-leishmaniasis effects highlights further therapeutic approaches against anthroponotic cutaneous leishmaniasis in future planning.
Subject(s)
Apoptosis , Gene Expression , In Vitro Techniques , Interleukin-10 , Interleukin-12 , Leishmania tropica , Leishmania , Leishmaniasis, Cutaneous , Liposomes , Methods , Up-RegulationABSTRACT
Objective: To explore the antileishmanial effect of tioxolone and its niosomal form against Leishmania tropica. Methods: Tioxolone niosomes were prepared by the hydration method and were evaluated for morphology, size, release study, and encapsulation efficiency. The cytotoxicity of tioxolone and its niosomal form was measured by MTT assay, leishmanicidal activity against promastigote and amastigote by MTT assay, apoptosis by flow cytometry, IL-12, IL-10 and metacaspase gene expression levels by q-PCR. Results: Span/Tween 40 and Span/Tween 60 niosomes had good physical stability as depicted in their size distribution curves and high encapsulation efficiency (>99%). The release profile of the entrapped compounds showed Fickian's model of tioxolone delivery based on diffusion through lipid bilayers. With the IC
ABSTRACT
Statement of the Problem: A significant proportion of patients undergoing chemotherapy or radiotherapy suffer from mucositis. The first symptom of oral mucositis is pain. Severe pain, burning sensation, and discomfort in the oral cavity make it difficult to continue treatment and even continue living in these patients
Purpose: The aim of this study was to evaluate and compare the effect of amitriptyline mouthwash [in two forms of simple and niosomal] as a local anesthetic agent with benzydamine HCl mouthwash in oral mucositis after radiotherapy or chemotherapy
Materials and Method: This double-blind study was performed on 60 patients with oral mucositis caused by radiotherapy and chemotherapy. The severity of mucositis was determined based on patient judgment; then dental examination was performed and recorded in a checklist. Three groups were assigned based on using either benzydamine HCL, amitriptyline, or niosomal form of amitriptyline. Pain and burning sensation were evaluated with VAS at different time intervals: before use and one, five, ten, and thirty minutes and one hour after using mouthwash. T-test was used to compare the intensity of pain between the two groups. ANOVA and Tukey test were used to compare the intensity of pain between groups
Results: Statistical analyses showed the maximum reduction in pain intensity at two different time intervals [p= 0.04]. Ten minutes after the use of niosomal form of amitriptyline, a 95% decrease in pain was observed. A 99% reduction in pain occurred after the use of simple form of amitriptyline [p= 0.04]
Conclusion: Use of amitriptyline mouthwash had local anesthetic effects in oral mucositis without systemic side effects. Decrease in the severity of pain with the use of amitriptyline mouthwash was more than that of benzydamine HCL mouthwash
ABSTRACT
Niosomes, non-ionic surfactant vesicles [NSVs], are the hydrated lipids composed mainly of different classes of non-ionic surfactants, introduced in the seventies as a cosmetic vehicle. Nowadays, niosomes are used as important new drug delivery systems by many research groups and also they are effective immunoadjuvants which some commercial forms are available in the market. These vesicles recently used as gene transfer vectors too. This review article presents a brief explain about the achievements in the field of nano-science related to NSVs. Different polar head groups from a vast list of various surfactant with one, two or three lipophilic alkyl, perfluoroalkyl and steroidal chemical moieties may be utilized to form the proper vesicular structures for encapsulating both hydrophilic and hydrophobic compounds. The methods of niosome preparation, the vesicle stability related aspects and many examples about pharmaceutical applications of NSVs will be presented. The routes of administration of these amphiphilic assemblies are also discussed