Effects of Phomopsidione on the Viability, Virulence, and Metabolites Profile of Methicillin-Resistant Staphylococcus aureus (MRSA).

Methicillin-resistant Staphylococcus aureus (MRSA) infections have become one of the most threatening multidrug-resistant pathogens. Thus, an ongoing search for anti-MRSA compounds remains an urgent need to effectively treating MRSA infections. Phomopsidione, a novel antibiotic isolated from Diaporthe fraxini, has previously demonstrated potent anti-candidal activity. The present study aimed to investigate the effects of phomopsidione on the viability, virulence, and metabolites profile of MRSA. MRSA was sensitive to phomopsidione in a concentration-dependent manner. Phomopsidione exhibited minimum inhibitory concentration and minimum bactericidal concentration of 62.5 and 500.00 µg/mL against MRSA on broth microdilution assay. The compound showed significant reduction in virulence factors production including extracellular polymeric substances quantification, catalase, and lipase. An untargeted metabolomics analysis using liquid chromatography-high resolution mass spectrometry revealed a significant difference in the metabolites profile of MRSA with 13 putatively identified discriminant metabolites. The present study suggested the potential of phomopsidione as a promising anti-MRSA agent.

Chitosan-Based Nanoencapsulated Essential Oils: Potential Leads against Breast Cancer Cells in Preclinical Studies.

Since ancient times, essential oils (EOs) derived from aromatic plants have played a significant role in promoting human health. EOs are widely used in biomedical applications due to their medicinal properties. EOs and their constituents have been extensively studied for treating various health-related disorders, including cancer. Nonetheless, their biomedical applications are limited due to several drawbacks. Recent advances in nanotechnology offer the potential for utilising EO-loaded nanoparticles in the treatment of various diseases. In this aspect, chitosan (CS) appears as an exceptional encapsulating agent owing to its beneficial attributes. This review highlights the use of bioactive EOs and their constituents against breast cancer cells. Challenges associated with the use of EOs in biomedical applications are addressed. Essential information on the benefits of CS as an encapsulant, the advantages of nanoencapsulated EOs, and the cytotoxic actions of CS-based nanoencapsulated EOs against breast cancer cells is emphasised. Overall, the nanodelivery of bioactive EOs employing polymeric CS represents a promising avenue against breast cancer cells in preclinical studies.

Thymol-Loaded Polymeric Nanoparticles Improve the Postharvest Microbiological Safety of Blueberries.

Research background: The presence of Yersinia enterocolitica on raw food products raises the concern of yersiniosis as most of the berries are consumed raw. This is a challenging issue from the food safety aspect since it could increase the occurrence of foodborne diseases among humans. Thus, it is crucial to implement an effective sanitation before the packaging. Experimental approach: This study aims to synthesize and characterize thymol-loaded polyvinyl alcohol (Thy/PVA) nanoparticles as a sanitizer for postharvest treatment of blueberries. Thy/PVA nanoparticles were characterized by spectroscopic and microscopic approaches, prior to the analyses of antimicrobial properties. Results and conclusions: The diameter size of the nanoparticles was on average 84.7 nm, with a surface charge of -11.73 mV. Based on Fourier transform infrared (FTIR) measurement, the Thy/PVA nanoparticles notably shifted to the frequency of 3275.70, 2869.66, 1651.02 and 1090.52 cm-1. A rapid burst was observed in the first hour of release study, and 74.9 % thymol was released from the PVA nanoparticles. The largest inhibition zone was displayed by methicillin-resistant Staphylococcus aureus (MRSA), followed by Y. enterocolitica and Salmonella typhi. However, amongst these bacteria, the inhibition and killing of Y. enterocolitica required a lower concentration of Thy/PVA nanoparticles. The treatment successfully reduced the bacterial load of Y. enterocolitica on blueberries by 100 %. Novelty and scientific contribution: Thymol is a plant-based chemical without reported adverse effects to humans. In this study, by using the nanotechnology method of encapsulation with PVA, we improved the stability and physicochemical properties of thymol. This nanoparticle-based sanitizer could potentially promote the postharvest microbiological safety of raw berries, which may become an alternative practice of food safety.

Nanoparticle-laden contact lens for controlled release of vancomycin with enhanced antibiotic efficacy.

Vancomycin is the last resort antibiotic for the treatment of severe bacterial keratitis. Its clinical application is limited due to its hydrophilicity and high molecular weight. To overcome this, this study aims to develop nanoparticles-laden contact lens for controlled ocular delivery of vancomycin. Polyvinyl alcohol (PVA) was used as encapsulant material. The nanoparticles had a negative surface charge and an average size of 147.6 nm. A satisfactory encapsulation efficiency (61.24%) was obtained. The release profile was observed to be slow and sustained, with a release rate of 1.29 µL mg-1 h-1 for 48 h. Five out of 6 test bacteria were suppressed by vancomycin nanoparticles-laden contact lens. Vancomycin is generally ineffective against Gram-negative bacteria and unable to pass through the outer membrane barrier. In this study, vancomycin inhibited Proteus mirabilis and Pseudomonas aeruginosa. Nano-encapsulation enables vancomycin to penetrate the Gram-negative cell wall and further destroy the bacterial cells. On Hohenstein challenge test, all test bacteria exhibited significant reduction in growth when exposed to vancomycin nanoparticles-laden contact lens. This study created an effective and long-lasting vancomycin delivery system via silicone hydrogel contact lenses, by using PVA as encapsulant. The antibiotic efficacy and vancomycin release should be further studied using ocular in vivo models.

Development of sodium alginate-pectin biodegradable active food packaging film containing cinnamic acid.

Plastics are still the most popular food packaging material and many of them end up in the environment for a long period. Due to packaging material's inability to inhibit microbial growth, beef often contains microorganisms that affect its aroma, colour and texture. Cinnamic acid is categorized as generally recognised as safe and is permitted for use in food. The development of biodegradable food packaging film with cinnamic acid has never been conducted before. This present study was aimed to develop a biodegradable active packaging material for fresh beef using sodium alginate and pectin. The film was successfully developed with solution casting method. The films' thickness, colour, moisture level, dissolution, water vapour permeability, bending strength and elongation at break were comparable to those of polyethylene plastic film in terms of these attributes. The developed film also showed the degradability in soil of 43.26% in a duration of 15 days. Fourier Transform Infrared (FTIR) spectra showed that cinnamic acid was successfully incorporated with the film. The developed film showed significant inhibitory activity on all test foodborne bacteria. On Hohenstein challenge test, a 51.28-70.45% reduction on bacterial growth was also observed. The antibacterial efficacy of the established film by using fresh beef as food model. The meats wrapped with the film showed significant reduction in bacterial load throughout the experimental period by 84.09%. The colour of the beef also showed significant different between control film and edible film during 5 days test. Beef with control film turned into dark brownish and beef with cinnamic acid turn into light brownish. Sodium alginate and pectin film with cinnamic acid showed good biodegradability and antibacterial activity. Further studies can be conducted to investigate the scalability and commercial viability of this environmental-friendly food packaging materials.

Metabolites characterisation of endophytic Phyllosticta fallopiae L67 isolated from Aloe vera with antimicrobial activity on diabetic wound microorganisms.

This study aimed to assess the antimicrobial activity of endophytic Phyllosticta fallopiae L67 isolated from Aloe vera against diabetic wound microorganisms and characterise their active fraction for biologically important metabolites. The dichloromethane (DCM) extract exhibited the most significant activity with inhibition zones ranging from 11.33 to 38.33 mm. The minimal inhibitory and lethality concentrations of DCM extract ranged from 78.13 to 2500.00 µg/ml and 625.00 to 5000.00 µg/ml, respectively. The extract showed teratogenicity and lethality in the zebrafish model, where peritoneal and hepatic oedema occurred at 62.50 µg/ml, and no abnormality appeared at 31.25 µg/ml. The extract also inhibited more than 82% biofilm formation. Bioassay-guided fractionation on DCM extract yielded 18 fractions and the most active fraction was subjected to UPLC-QTOF-MS/MS analysis. Flavones, stilbenes, flavanonols, isoflavonoids, phenolic glycosides and phenol derivatives were detected. In conclusion, endophytic P. fallopiae possessed bioactive metabolites with significant antimicrobial activity against diabetic wound microorganisms.

Cynometra cauliflora essential oils loaded-chitosan nanoparticles: Evaluations of their antioxidant, antimicrobial and cytotoxic activities.

Nanoencapsulation has appeared as an alternative approach to protect the bioactive constituents of essential oils (EOs) and to improve their properties. In this study, Cynometra cauliflora essential oils (CCEOs) were nanoencapsulated in chitosan nanoparticles (CSNPs) using an emulsion-ionic gelation technique. Transmission electron microscopy (TEM) images illustrated a well dispersion and spherical shape of C. cauliflora EOs-loaded chitosan nanoparticles (CCEOs-CSNPs) with an average size of less than 100 nm. In addition to that, Fourier transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS) and X-ray diffraction (XRD) analyses revealed the success of CCEOs nanoencapsulation. The encapsulation efficiency (EE) was in the range of 38.83% to 44.16% while the loading capacity (LC) reached 32.55% to 33.73%. The antioxidant activity (IC50) of CCEOs-CSNPs was ranged from 21.65 to 259.13 µg/mL when assessed using DPPH radical scavenging assay. CCEOs-CSNPs showed an appreciable antimicrobial effects on diabetic wound microorganisms. Notably, cytotoxic effects against human breast cancer MCF-7 and MDA-MB-231 cells recorded IC50 of 3.72-17.81 µg/mL and 16.24-17.65 µg/mL, respectively, after 72 h treatment. Interestingly, no cytotoxicity against human breast normal MCF-10A cells was observed. Thus, nanoencapsulation using CSNPs could improve the properties of CCEOs in biomedical related applications.

Metabolomics Analysis and Antioxidant Potential of Endophytic Diaporthe fraxini ED2 Grown in Different Culture Media.

Endophytic fungi are a promising source of bioactive metabolites with a wide range of pharmacological activities. In the present study, MS-based metabolomics was conducted to study the metabolomes variations of endophytic Diaporthe fraxini ED2 grown in different culture media. Total phenolic content (TPC), total flavonoid content (TFC), 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), and ferric reducing antioxidant power (FRAP) assays were conducted to assess the antioxidant potential of the fungal extracts. Multivariate data analysis (MVDA) was employed in data analysis and interpretation to elucidate the complex metabolite profile. The supplemented culture medium of D. fraxini fungal extract stimulated the production of metabolites not occurring in the normal culture medium. Antioxidant activity studies revealed the potential of supplemented cultured fungal extract of D. fraxini as a source of antioxidants. The present findings highlight that fungal culture medium supplementation is an effective approach to unravelling the hidden metabolome in plant-associated fungal diversity.

Cholic acid: a novel steroidal uncompetitive inhibitor against ß-lactamase produced by multidrug-resistant isolates.

ß-lactam antibiotics are the most frequently prescribed class of drugs worldwide, due to its efficacy and good safety profile. However, the emergence of ß-lactamase producing bacterial strains eliminated the use of ß-lactam antibiotics as a chemotherapeutic choice. To restore their usability, a non-antibiotic adjuvant in conjunction with ß-lactam antibiotics is now being utilised. Cholic acid potentially acts as an adjuvant since it can blunt the pro-inflammatory activity in human. Our main objective is to scrutinise the inhibition of ß-lactamase-producing bacteria by adjuvant cholic acid, synergism of the test drugs and the primary mechanism of enzymatic reaction. Antibacterial effect of the cholic acid-ampicillin (CA-AMP) on 7 ß-lactamase positive isolates were evaluated accordingly to disc diffusion assay, antibiotic susceptibility test, as well as checkerboard analysis. Then, all activities were compared with ampicillin alone, penicillin alone, cholic acid alone and cholic acid-penicillin combination. The CA-AMP displayed notable antibiotic activity on all test bacteria and depicted synergistic influence by representing low fractional inhibitory concentration index (FIC ≤ 0.5). According to kinetic analyses, CA-AMP behaved as an uncompetitive inhibitor against beta lactamase, with reducing values of Michaelis constant (Km) and maximal velocity (Vmax) recorded. The inhibitor constant (Ki) of CA-AMP was equal to 4.98 ± 0.3 µM, which slightly lower than ampicillin (5.00 ± 0.1 µM).

Recent Developments in Metabolomics Studies of Endophytic Fungi.

Endophytic fungi are microorganisms that colonize living plants' tissues without causing any harm. They are known as a natural source of bioactive metabolites with diverse pharmacological functions. Many structurally different chemical metabolites were isolated from endophytic fungi. Recently, the increasing trends in human health problems and diseases have escalated the search for bioactive metabolites from endophytic fungi. The conventional bioassay-guided study is known as laborious due to chemical complexity. Thus, metabolomics studies have attracted extensive research interest owing to their potential in dealing with a vast number of metabolites. Metabolomics coupled with advanced analytical tools provides a comprehensive insight into systems biology. Despite its wide scientific attention, endophytic fungi metabolomics are relatively unexploited. This review highlights the recent developments in metabolomics studies of endophytic fungi in obtaining the global metabolites picture.

Gelatine Film Incorporated with Clitoria ternatea-Derived Anthocyanin Microcapsules, A Food Packaging Material Effective Against Foodborne Pathogens.

RESEARCH BACKGROUND: Microbial contamination of food products is one of the significant causes of food spoilage and foodborne illnesses. The use of active packaging films incorporated with antimicrobial agents can be a measure to improve food quality and extend shelf life. Nevertheless, antimicrobial agents such as silver, copper, titanium and zinc in the packaging films have raised concerns among consumers due to toxicity issues. EXPERIMENTAL APPROACH: The current study aims to develop biodegradable gelatine-based edible films incorporated with microcapsules of Clitoria ternatea-derived anthocyanins as a natural antimicrobial agent. The impact of incorporation of microcapsules with anthocyanins on the morphology, thermal, mechanical, water vapour barrier and physicochemical properties of the gelatine films was evaluated in this study. The effectiveness of the developed films against foodborne pathogens and their application for perishable food protection were also investigated. RESULTS AND CONCLUSIONS: The results show that incorporating anthocyanin microcapsules enhances the gelatine film physical and mechanical properties by increasing the thickness, tensile strength, Young's modulus and elongation at break of the films. Scanning electronic microscopy analysis revealed that the film surface morphology with anthocyanin microcapsules had a homogeneous and smooth surface texture compared to the control. The thermogravimetric analysis also showed a slight improvement in the thermal properties of the developed films. Agar well diffusion assay revealed that the developed films exhibit significant inhibition against a broad-spectrum of bacteria. Furthermore, the films composed of gelatine with anthocyanin microcapsules significantly reduced the total viable count of microorganisms in the bean curd during storage for 12 days compared with the control films. NOVELTY AND SCIENTIFIC CONTRIBUTION: Increasing global awareness of healthy and safe food with minimal synthetic ingredients as preservatives has sparked the search for the use of antimicrobial agents of natural origins in active food packaging material. In this study, a safe and effective active packaging film was developed using an environmentally friendly biopolymer, gelatine film incorporated with microcapsules of Clitoria ternatea-derived anthocyanins as a natural antimicrobial agent. This study demonstrated that such a method is not only able to improve the film physical properties but can also significantly prolong the shelf life of food products by protecting them from microbial spoilage.

Potential of Endophytic Diaporthe sp. as a New Source of Bioactive Compounds.

Endophytic fungi are symbiotically related to plants and spend most of their life cycle within them. In nature, they have a crucial role in plant micro-ecosystem. They are harnessed for their bioactive compounds to counter human health problems and diseases. Endophytic Diaporthe sp. is a widely distributed fungal genus that has garnered much interest within the scientific community. A substantial number of secondary metabolites have been detected from Diaporthe sp. inhabited in various plants. As such, this minireview highlights the potential of Diaporthe sp. as a rich source of bioactive compounds by emphasizing on their diverse chemical entities and potent biological properties. The bioactive compounds produced are of significant importance to act as new lead compounds for drug discovery and development.

Homalomena pineodora essential oil nanoparticle inhibits diabetic wound pathogens.

Essential oil of Homalomena pineodora inhibits diabetic pathogens; however, the activity was not sustainable when applied as wound dressing. This study aims to synthesise the essential oil nanoparticle using chitosan. The nanoparticles were synthesised with ion gelation method, confirmed by spectroscopic analysis. The spherical nanoparticles display a size of 70 nm, with strong surface charge of +24.10 mV. The nanoparticles showed an initial burst release followed by a slow release pattern for 72 h, following the first order of kinetic. The release behaviour was ideal for wound dressing. The antimicrobial activity was broad spectrum. The formation of nanoparticle enhanced the antimicrobial efficacy of the essential oil. The nanoparticle also showed a concentration-dependent killing behaviour on time-kill assay. In the 3D collagen wound models, the nanoparticles reduced the microbial growth by 60-80%. In conclusion, H. pineodora nanoparticles showed pharmaceutical potential in inhibiting microbial growth on diabetic ulcers.

Sesquiterpenes rich essential oil from Garcinia celebica L. and its cytotoxic and antimicrobial activities.

Garcinia celebica L., locally known as "manggis hutan" in Malaysia is widely used in folkloric medicine to treat various diseases. The present study was aimed to examine the chemical composition of the essential oil from the leaves of G. celebica L. (EO-GC) and its cytotoxic and antimicrobial potential. EO-GC obtained by hydrodistillation was analysed using capillary GC and GC-MS. Twenty-two compounds were identified, dominated by α-copaene (61.25%), germacrene D (6.72%) and ß-caryophyllene (5.85%). In the in vitro MTT assay, EO-GC exhibited significant anti-proliferative effects towards MCF-7 human breast cancer cells with IC50 value of 45.2 µg/mL. Regarding the antimicrobial activity, it showed better inhibitory effects on Gram-positive bacteria than Gram-negative bacteria and none on the fungi and yeasts tested.

Antimicrobial activities of endophytic fungi residing in Aloe vera against diabetic wound pathogens

Aims@#Endophytic fungi are organisms that colonize living plant tissues without causing significant symptoms of diseases. They are known as the repository of bioactive compounds. This study was aimed to isolate endophytic fungi associated with Aloe vera and to assess their antimicrobial activity against the diabetic wound pathogens that result to lower limb amputations. @*Methodology and results@#In this study, 84 endophytic fungi were isolated from A. vera by using 5% sodium hypochlorite and 70% ethanol as surface sterilants. On preliminary antimicrobial screening by agar plug assay, 12 (14.3%) isolates showed significant antagonistic activity on the test microorganisms. Two of the endophytes were identified as Aspergillus flavus and Colletotrichum gloeosporioides through morphological and molecular techniques. The fungal cultures fermented in shake flask were extracted subsequently with hexane, dichloromethane, ethyl acetate, and n-butanol. Ethyl acetate and dichloromethane extracts of A. flavus and C. gloeosporioides inhibited all test bacteria. The compounds in the extracts were seemed to be semi-polar in nature. On broth microdilution assay, minimal inhibitory and minimal lethality concentration of ethyl acetate extracts of the fungi were found in the range of 0.63−2.50 and 1.25−5.00 mg/mL, respectively. @*Conclusion, significance and impact of study@#This study reveals that A. vera harbours a wide diversity of endophytic fungi. A. flavus and C. gloeosporioides showing broad spectrum antimicrobial activity on wound pathogens may be potential sources of bioactive compounds. Further investigations should be conducted to isolate and identify the antimicrobial compound produced by these fungal isolates.

Potential Antimicrobial Applications of Chitosan Nanoparticles (ChNP).

Polymeric nanoparticles are widely used for drug delivery due to their biodegradability property. Among the wide array of polymers, chitosan has received growing interest among researchers. It was widely used as a vehicle in polymeric nanoparticles for drug targeting. This review explored the current research on the antimicrobial activity of chitosan nanoparticles (ChNP) and the impact on the clinical applications. The antimicrobial activities of ChNP were widely reported against bacteria, fungi, yeasts and algae, in both in vivo and in vitro studies. For pharmaceutical applications, ChNP were used as antimicrobial coating for promoting wound healing, preventing infections and combating the rise of infectious disease. Besides, ChNP also exhibited significant inhibitory on foodborne microorganisms, particularly on fruits and vegetables. It is noteworthy that ChNP can be also applied to deliver antimicrobial drugs, which further enhance the efficiency and stability of the antimicrobial agent. The present review addresses the potential antimicrobial applications of ChNP from these few aspects.

Phomopsidione nanoparticles coated contact lenses reduce microbial keratitis causing pathogens.

Microbial keratitis is the infection caused by pathogenic microorganisms that commonly occurs among the contact lens users. Various antimicrobial compounds were coated on contact lenses to kill keratitis causing microorganisms, however these compounds caused several adverse side effects. Hence, the aim of this study is to develop a silicone hydrogel contact lens coated with phomopsidione nanoparticle that inhibit keratitis causing clinical isolates. Phomopsidione nanoparticles were synthesized using polyvinyl alcohol as encapsulant. The nanoparticles showed an average size of 77.45 nm, with neutral surface charge. Two drug release patterns were observed in the drug release profile, which are the initial slow release phase with extended drug release (release rate 46.65 µg/h), and the burst release phase observed on Day 2 (release rate 2224.49 µg/h). This well-regulated drug delivery system enables the control of drug release to meet the therapeutic requirements. On agar diffusion assay, 3 out of 5 test microorganisms were inhibited by phomopsidione nanoparticle coated contact lenses, including two Gram negative bacteria. Besides, all test microorganisms showed at least 99% of growth reduction, with the treatment of the contact lens model. The drug loaded onto the nanoparticles is sufficient to prevent the bacterial growth. In conclusion, this study provides an effective alternative to combat keratitis-causing microorganisms among contact wearers.

Antimicrobial wound dressing film utilizing nano-cellulose and gelatin as drug delivery system for Garcinia mangostana L extract

Aims@#Diabetic patients with foot ulcer showed 150-fold increased risk of amputation, which is primarily caused by microbial infection. Silver ions are commonly incorporated into wound dressing to enhance the antimicrobial property. However, concerns have been expressed about the development of bacterial resistance to heavy metals. In this study, we extracted the nano-cellulose from medical cotton and reinforced with gelatin to develop a film for wound dressing. @*Methodology and results@#Garcinia mangostana L pericarp extract was incorporated into the nano-cellulose film as antimicrobial finishing. The efficacy of the developed nano-cellulose film was evaluated on diabetic wound microorganisms. We observed cellulose nano crystals with an average length of 133.71 nm under transmission electron microscope. The developed film showed gradual release of the extract over a period of 48 h and no burst effect was observed. The film exhibited significant inhibitory activity on three Gram positive bacteria, three Gram negative and all filamentous fungi tested. On Hohenstein challenge test, all test microorganisms showed significant growth reduction, with the treatment of the film. We also noticed that the antimicrobial activity of the film sustained even after 20 washes. @*Conclusion, significance and impact of study@#Our results indicate that the G. mangostana L pericarp extract loaded nano-cellulose films exhibited significant inhibitory activity on diabetic wound microorganisms. The developed film can be potentially used to prevent foot ulcer infection among diabetic patients.

Chemical Composition and Antimicrobial Efficiency of Swietenia macrophylla Seed Extract on Clinical Wound Pathogens

Microbial wound infection prolonged the hospitalization and increase the cost for wound management. Silver is commonly used as antimicrobial wound dressing. However, it causes several adverse side effects. Hence, this study was aimed to evaluate the antimicrobial efficiency of Swietenia macrophylla seed extract on clinical wound pathogens. Besides, the bioactive constituents of the seed extract were also determined. S. macrophylla seeds were extracted with methanol by maceration method. The seed extract inhibited 5 test bacteria and 1 yeast on disc diffusion assay. The antibacterial activity was broad spectrum, as the extract inhibited both Gram positive and Gram negative bacteria. On kill curve analysis, the antibacterial activity of the seed extract was concentration-dependent, the increase of extract concentration resulted in more reduction of bacterial growth. The extract also caused 99.9% growth reduction of Bacillus subtilis relative to control. A total of 21 compounds were detected in gas chromatography-mass spectrometry analysis. The predominant compounds present in the extract were oleic acid (18.56%) and linoleic acid (17.72%). In conclusion, the methanolic extract of S. macrophylla seeds exhibited significant antimicrobial activity on clinical wound pathogens. Further investigations should be conducted to purify other bioactive compounds from the seeds of S. macrophylla.

The potential to treat lung cancer via inhalation of repurposed drugs.

Lung cancer is a highly invasive and prevalent disease with ineffective first-line treatment and remains the leading cause of cancer death in men and women. Despite the improvements in diagnosis and therapy, the prognosis and outcome of lung cancer patients is still poor. This could be associated with the lack of effective first-line oncology drugs, formation of resistant tumors and non-optimal administration route. Therefore, the repurposing of existing drugs currently used for different indications and the introduction of a different method of drug administration could be investigated as an alternative to improve lung cancer therapy. This review describes the rationale and development of repositioning of drugs for lung cancer treatment with emphasis on inhalation. The review includes the current progress of repurposing non-cancer drugs, as well as current chemotherapeutics for lung malignancies via inhalation. Several potential non-cancer drugs such as statins, itraconazole and clarithromycin, that have demonstrated preclinical anti-cancer activity, are also presented. Furthermore, the potential challenges and limitations that might hamper the clinical translation of repurposed oncology drugs are described.