Recent Patents on Anti-Infective Drug Discovery - Volume 15, Issue 1, 2020

Background: Acne vulgaris a chronic disease which is caused by blockage of the sebaceous gland is commonly seen in almost every human being at some point in their lives. There are 20-25% chances of progression of acne to severe cases, which leads to permanent scarring that results in psychological problems like depression, social isolation, lowered self-esteem, and lowered self-confidence. Objective: Though several conventional treatments are available in the market but still there are various adverse effects associated with topical anti-acne agents due to which it lacks patient compatibility. The present study is undertaken to find out the major shortcoming; why the current therapies do not give the desired therapeutic results. Conclusion: Novel drug delivery strategies can play a crucial role in the enhancement of topical delivery of anti-acne agents by escalating their dermal localization and reducing their adverse effects. Consumption of medicinal plants like Aloe vera, Withania somniferia etc. have clinical evidence regarding the effective management of acne. The current inclination towards nanotechnology is considerable due to several changes in the pharmaceutical research area. To secure the research work in different pharmaceutical fields, patents are filed against various agents like Galderma Research & Development have filed patents for adapalene and benzoyl peroxide for the management of acne vulgaris. The current review highlights the potential of various novel drug delivery approaches like liposomes, niosomes, ethosomes, transfersomes etc. in enhancing the topical delivery of anti-acne agents.

Introduction: Antibiotic resistance and extensive use of antibiotics are amongst the major causes of failure in antibiotic treatment. The purpose of this study was to investigate antibiotic resistance patterns and to identify resistance genes of quinolones and colistin in Escherichia coli. There are a very few patents on E. coli isolated from colorectal cancer. So, this study demonstrates that some bacteria resistant to ciprofloxacin have not resistance genes.Moreover, new patterns for E. coli are presented for isolates of patients with colorectal cancer. Materials and Methods: Of the three healthy people, inflammatory bowel diseases (IBD) patients and colorectal cancer patients, 40 E. coli strains isolated after confirmation by biochemical and molecular methods. The susceptibility of isolates to antibiotics was investigated using disk diffusion test. After deoxyribonucleic acid (DNA) extraction, polymerase chain reaction (PCR) was used to identify genes encoding resistance to ciprofloxacin (qnr A, qnr B) and colistin (mcr-1). Results: The results showed that E. coli isolates from colorectal cancer patients had the highest resistance to piperacillin (67.5%), ceftazidime (47.5%), and cefepime (42.5%). Also, E. coli strains isolated from IBD patients showed resistance to antibiotic ceftazidime 13%. More than 95% of E. coli strains isolated from healthy people were susceptible to antibiotics. Based on the results, 18 (15%) E. coli strains showed resistance to ciprofloxacin. The qnr A gene was detected in 61.11% isolates; however, qnr B was detected in 9 (50%) isolates. Isolates resistant to colistin were not observed. Conclusion: These findings indicate increased resistance of E. coli to ciprofloxacin in comparison with prior studies. Further research in this field will increase our knowledge and more effective exposure to the antibiotic resistance of the pathogenic microorganisms.

Introduction: The main purpose of the research was to develop, optimize and characterize tobramycin sulphate loaded chitosan nanoparticles based gel in order to ameliorate its therapeutic efficacy, precorneal residence time, stability, targeting and to provide controlled release of the drug. Methods: Box-Behnken design was used to optimize formulation by 3-factors (chitosan, STPP and tween 80) and 3-levels. Developed formulation was subjected for characterizations such as shape and surface morphology, zeta potential, particle size, in vitro drug release studies, entrapment efficiency of drug, visual inspection, pH, viscosity, spreadability, drug content, ex vivo transcorneal permeation studies, ocular tolerance test, antimicrobial studies, isotonicity evaluation and histopathology studies. Results: Based on the evaluation parameters, the optimized formulation showed a particle size of 43.85 ± 0.86 nm and entrapment efficiency 91.56% ± 1.04, PDI 0.254. Cumulative in vitro drug release was up to 92.21% ± 1.71 for 12 hours and drug content was found between 95.36% ± 1.25 to 98.8% ± 1.34. TEM analysis unfolded spherical shape of nanoparticles. TS loaded nanoparticulate gel exhibited significantly higher transcorneal permeation as well as bioadhesion when compared with marketed formulation. Ocular tolerance was evaluated by HET-CAM test and formulation was non-irritant and well-tolerated. Histopathology studies revealed that there was no evidence of damage to the normal structure of the goat cornea. As per ICH guidelines, stability studies were conducted and were subjected for 6 months. Conclusion: Results revealed that the developed formulation could be an ideal substitute for conventional eye drops for the treatment of bacterial keratitis.

Background: Microbial resistance to antibiotics and their adverse effects related to these antibiotics are a matter of global public health in the 21th century. The emergence of drug-resistant strains, has gained the interest of the scientists to discover new antimicrobial agents from the essential oil of medicinal plants. Methods: Anti-mycobacterial effects of Trachyspermum copticum and Pelargonium graveolens essential oils were determined against multi-drug resistant clinical strains of Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium fortuitum and standard strain of Mycobacterium tuberculosis H37Rv by a Broth micro-dilution method. Pelargonium graveolens plant named Narmada was discovered by Kulkarni R.N et al. (Patent ID, USPP12425P2) and a formulation comprising thymol obtained from Trachyspermum is useful in the treatment of drug-resistant bacterial infections (Patent ID, US6824795B2). The chemical composition of hydro-distilled essential oils was determined by GC and GC-MS. Results: Minimum Inhibitory Concentration (MIC) values for T. copticum essential oil against tested isolates were ranged from 19.5 μg/mL to 78 μg/mL. The least minimum inhibitory concentration of P. graveolens extract against M. Kansasii and MDR-TB was 78 μg/ml. Conclusion: The results of the present research introduced T. copticum and P. graveolens essential oils as a remarkable natural anti-mycobacterial agent, but more pharmacological studies are required to evaluate their efficacy in animal models.

Background: Studies showed that biogenic selenium nanoparticles (SeNPs) have a number of pharmacological properties, such as antimicrobial ones. Objective: The present investigation assesses the efficacy of biogenic selenium nanoparticles (SeNPs) as a new patent against latent toxoplasmosis in a mice model. Methods: Male BALB/c mice were orally treated with SeNPs at the doses of 2.5, 5, 10 mg/kg once a day for 14 days. On the 15th day, the mice were infected with the intraperitoneal inoculation of 20-25 tissue cysts from the Tehran strain of Toxoplasma gondii. The mean numbers of brain tissue cysts and the mRNA levels of TNF-α, IL-12, IL-10, IFN-γ, and inducible nitric oxide synthase (iNOS) in mice of each tested group were measured. Moreover, serum clinical chemistry factors in treated mice were examined to determine the safety of SeNPs. Results: The mean number of the brain tissue cysts was significantly (P<0.001) decreased in mice treated with SeNPs at doses 2.5 (n=37), 5 (n=11), and 10 mg/kg (n=3) based on a dose dependent manner compared with the control group (n=587). The mRNA levels of IFN-γ, TNF-α, IL-12, and iNO were significantly increased in mice treated with SeNPs at the doses 10 mg/kg compared with control subgroups (p<0.05). No significant variation (p>0.05) was observed in the clinical chemistry parameters among the mice in the control subgroups compared with groups treated with SeNPs. Conclusion: The results of the present study showed a new patent in the treatment of toxoplasmosis; so that taking the biogenic selenium nanoparticles in concentrations of 2.5-10 mg/kg for 2 weeks was able to prevent severe symptoms of the toxoplasmosis in a mice model. This indicated the prophylactic effects of SeNPs with no considerable toxicity against latent toxoplasmosis. However, more studies are required to elucidate the correct anti-Toxoplasma mechanisms of SeNPs.