Zinc Oxide Nanoparticles: Therapeutic Benefits and Toxicological Hazards

Despite the widespread application of zinc oxide nanoparticles in biomedicine, their use is still a controversial issue. Zinc oxide nanoparticles were reported to have therapeutic benefits. However, they were reported to have toxicological hazards as well. Several studies reported the antibacterial, anticancer, antioxidant, and immunomodulatory effects of zinc oxide nanoparticles. Additionally, zinc oxide nanoparticles were used in sunscreens. Furthermore, the ability to use zinc oxide nanoparticles as an adjuvant treatment to alleviate the toxic effects of chemotherapeutic drugs has been reported. However, zinc oxide nanoparticles were shown to induce toxic effects in different body organs and systems. The affected organs included liver, spleen, kidney, stomach, pancreas, heart and lung. In addition, zinc oxide nanoparticles were reported to adversely affect the neurological system, lymphatic system, hematological indices, sex hormones levels, and fetal development. The toxic effects of zinc oxide nanoparticles were based on their concentration, their dose, the route of their administration, and the time of exposure to those particles. Thus, it is crucial to assess their efficacy and safety to determine their toxicological risks and therapeutic benefits.

Development, Characterization and Transdermal Delivery of Dapsone and an Antibiotic Entrapped in Ethanolic Liposomal Gel for the Treatment of Lapromatous Leprosy

Background and Objective: Applying Ethosomal Gels (EGs) in transdermal drug delivery systems has evoked considerable interest because of their good water-solubility and biocompatibility. The aim of present study was to prepare and characterize ethosomes of antileprotic drug Dapsone (DAP) together with an antibiotic Cloxacillin Sodium (CLXS) which may deliver these drugs to targeted site more efficiently than marketed gel preparation of DAP and also overcome the problems related with oral administration of CLXS. Methodology: Ethosomes were prepared by cold method then characterized for particle size, Entrapment Efficiency (EE), zeta potential and permeation studies. Vesicular size was determined by Scanning Electron Microscopy (SEM) and found to be varied from 127±9.01 to 215±7.23 nm depending on the concentrations of soya lecithin and ethanol. Results: The average percent drug entrapment efficiency of formulations ranged between 52.31% to 73.51% and 49.07% to 71.91% for DAP and CLXS respectively. The high ethanol concentration in ethosomes has shifted the vesicular charge from positive to negative. It was observed that F1 and F2 formulations were having zeta potential of -25.08±1.03 mV and -50.11±1.97 mV respectively and do not aggregate rapidly. The drug release of ethosomes ranged from 84.68% to 96.58% and 64.89% to 84.21% for DAP and CLXS respectively. Ethosomal gel was prepared with optimized ethosome and studied for its release and physicochemical characteristics. Conclusion: Finally, G5 demonstrated better (p < 0.05) antileprotic effect to improve effectiveness, stability and to reduce side effects and toxicity associated with the chosen drugs in order to treat Leprosy.

Development of Dry Powder Inhaler Containing Prothionamide-PLGA Nanoparticles Optimized Through Statistical Design: In-vivo Study

Objective:The objective of the present work was to formulate Prothionamide (PTH) nanoparticles using Poly lactic co-glycolic acid (PLGA), optimized by Box-Behnken Design and further modification to dry powder inhaler followed byin-vivostudy.Methods:Poly-lactic co-gycolic acid (PLGA), a biodegradable polymer was used to coat Prothionamide by solvent evaporation technique. Formulation was optimized using Box-Behnken Design. Response surface curve and desirability factors helped in the selection of optimum formulation of PTH nanoparticles. Dry powder inhaler was prepared by adding inhalable grade lactose to optimize PTH nanoparticles. Mass median aerodynamic diameter (MMAD) was carried out using Andersen Cascade Impactor (ACI) to demonstrate its suitability in the pulmonary administration.In-vitrodrug release of dry powder inhaler was carried out in simulated lungs fluid. Correlationin-vitrotoin-vivowas established after performing animal experiment.Results:FTIR study reveals no chemical interaction between PTH, lactose and PLGA as the principle peaks was retained with same intensity in the physical mixture. Scanning electron microscope showed the spherical shape and aerodynamic particle size was found to be 1.69µm. Drug release study showed initial burst release followed by zero order release.In-vivomodel confirmed the presence of PTH after 24h. Aerodynamic particle size and the release profile revealed the suitability of PTH loaded nanoparticles containing dry powder inhaler for the pulmonary administration.Conclusion:Prepared DPI containing PTH nanoparticles can improve in the management of tuberculosis by increasing PTH residency in the lungs tissue for prolong period of time.

Formulation and In-Vitro Evaluation of Solid Lipid Nanoparticles Containing Levosulpiride

Objectives: The present study aims on preparing Levosulpiride loaded solid lipid nanoparticles (SLNs) to reduce the dose, frequency of dosing, reduce side effects and to increase the bioavailable fraction of drug (<30% orally in general). Methods: Levosulpiride was characterized by preformulation studies like physical appearance, melting point, assay, calibration curve, FTIR analysis and DSC analysis. The calibration curve of the drug was prepared in pH 6.8 phosphate buffer. Two lipids (Stearic acid and Palmitic acid) were used as lipid phase to prepare SLNs. Factorial design (23) was applied to formulate 16 formulations (8 for each lipid i.e. SF1-SF8 and PF1-PF8). Levosulpiride SLNs were prepared by solvent evaporation method followed by homogenization. Results: The optimized formulations were characterized by particle size analysis, zeta potential analysis, in vitro drug release and drug release kinetics. Drug-excipient interaction in optimized formulation was characterized by FTIR, DSC and TEM analysis. Conclusion: On the basis of evaluation parameters, the formulation SF1 (containing Stearic acid) and PF1 (containing Palimitic acid) found to be better formulations amongst their groups with a controlled drug release after a period of 24 hrs.

Biofabricated Silver Nanoparticles Synergistically Activate Amphotericin B Against Mature Biofilm Forms of Candida Albicans

Background: Biofilm formation by Candida albicans is a significant clinical challenge. Fungal biofilms are resistant to most of the currently available antifungal agents. Amphotericin-B (AmB) is an antifungal agent used for the treatment of systematic fungal infections but it is well known for its toxicities and side-effects. Novel approaches are needed to treat these infections that can reduce its toxicities. Objectives: Current study aims to evaluate the efficacy of silver nanoparticles (SNPs) alone and in combination with AmB against growth and biofilm formation in C. albicans. Methods: Combinations of SNP-AmB were tested against planktonic growth and biofilm formation in vitro. Micro broth dilution method was used to study planktonic growth and biofilm formation. The fractional inhibitory concentration indices (FICI) were calculated by using a checkerboard format. Biofilm formation was analyzed by using XTT-metabolic assay. Results: MIC of AmB for developing biofilm was lowered by 16 fold in combination with SNPs. The calculated fractional inhibitory concentration indices were 0.1875 suggesting that this interaction is synergistic. Similarly, the mature biofilms were significantly prevented by SNPs-AmB combination. This interaction was synergistic. Furthermore, interaction between SNPs and AmB against planktonic growth was additive. Hemolytic activity assay was carried out on these drugs and combinations. Drug required for inhibition alone as well as in combination did not exhibit hemolytic activity. Conclusion: The combinations with SNPs lead to decreases in the dosage of AmB required for anti-Candida activity. SNPs-AmB combination could be an effective strategy against biofilm formed by C. albicans.