scholarly journals NICLOSAMIDE-EXFOLIATED ANIONIC CLAY NANOHYBRID REPURPOSED AS AN ANTIVIRAL DRUG FOR TACKLING COVID-19; ORAL FORMULATION WITH TWEEN 60/EUDRAGIT S100

Author(s):  
N. Sanoj Rejinold ◽  
Huiyan Piao ◽  
Goeun Choi ◽  
Geun-Woo Jin ◽  
Jin-Ho Choy
2021 ◽  
Vol 14 (5) ◽  
pp. 486
Author(s):  
Goeun Choi ◽  
Huiyan Piao ◽  
N. Sanoj Rejinold ◽  
Seungjin Yu ◽  
Ki yeok Kim ◽  
...  

COVID-19 has been affecting millions of individuals worldwide and, thus far, there is no accurate therapeutic strategy. This critical situation necessitates novel formulations for already existing, FDA approved, but poorly absorbable drug candidates, such as niclosamide (NIC), which is of great relevance. In this context, we have rationally designed NIC-loaded hydrotalcite composite nanohybrids, which were further coated with Tween 60 or hydroxypropyl methyl cellulose (HPMC), and characterized them in vitro. The optimized nanohybrids showed particle sizes <300 nm and were orally administrated to rats to determine whether they could retain an optimum plasma therapeutic concentration of NIC that would be effective for treating COVID-19. The pharmacokinetic (PK) results clearly indicated that hydrotalcite-based NIC formulations could be highly potential options for treating the ongoing pandemic and we are on our way to understanding the in vivo anti-viral efficacy sooner. It is worth mentioning that hydrotalcite–NIC nanohybrids maintained a therapeutic NIC level, even above the required IC50 value, after just a single administration in 8–12 h. In conclusion, we were very successfully able to develop a NIC oral formulation by immobilizing with hydrotalcite nanoparticles, which were further coated with Tween 60 or HPMC, in order to enhance their emulsification in the gastrointestinal tract.


2020 ◽  
Vol 11 (3) ◽  
pp. 3309-3315
Author(s):  
Manahil B Elamin ◽  
Amani Abd Elrazig Salman Abd Elaziz ◽  
Emad Mohamed Abdallah

Heterocyclic chemistry has provided an inexhaustible source of pharmaceutical molecules. Heterocyclic compounds such as benzothiazole moieties and its derivatives area substantial class of compounds in pharmaceutical chemistry and exhibited therapeutic capabilities, such as antitumor, anticancer, antioxidant, antidiabetic, antiviral, antimicrobial, antimalarial, anthelmintic and other activities. Besides, some antibiotics such as penicillin and cephalosporin have heterocyclic moiety. The growing prevalence of multi-drug resistant pathogens represents serious global concern,which requires the development of new antimicrobial drugs. Moreover, the emergence of pandemic SARSCoV-2 causing Covid-19 disease and all these health dilemmas urge the scientific community to examine the possible antimicrobial and antiviral capacities of some bioactive benzothiazole derivatives against these severe causative agents.This mini-review highlights some recent scientific literature on different benzothiazole molecules and their derivatives. It turns out that, there are numerous synthesized benzothiazole derivatives which exhibited different mode of actions against microorganisms or viruses and accordingly suggested them as an active candidate in the discovery of new antimicrobial or antiviral agents for clinical development. The recommended bioactive benzothiazole derivatives mentioned in the current study are mainly Schiff bases, azo dyes and metal complexes benzothiazole derivatives; the starting material for most of these derivatives are 2-aminobenzothiazole although careful pharmaceutical studies should be conducted to ensure the safety and efficacy of these bioactive synthesized molecules as an antimicrobial or antiviral drug in the future.


2020 ◽  
Vol 11 (SPL1) ◽  
pp. 475-481
Author(s):  
Jotheeswari P ◽  
Yuvaraj M ◽  
Balaji K ◽  
Gunapriya Raghunath ◽  
Kumaresan M

COVID-19 is a current sensational and dangerous threat that affects millions of people across the world. As the day progresses the rate of growth of COVID-19 drastically increases. No vaccine or specific antiviral drug are active against corona, therefore, preventing the exposure to the virus is the base of support against its spread across the world. Despite the implementation of preventive measures, the rate of virus-infected cases progressively increases which stimulates our thought process to raise a question, whether the preventive measures that we follow are effective against the spread of COVID-19 infection. Evidence from previous literature obtained from various online tools implies multiple preventive measures that should be followed and also illustrates their mechanism of action against the active spread of COVID-19 infection. According to the results from the evidence, we can identify the gold standard preventive measure among the described preventive measures. The precautionary measure encompasses both pharmaceutical interventions and non- pharmaceutical interventions among which non-pharmaceutical measures are superior in the prevention of the developing pandemic. Among the non-pharmaceutical interventions, social distancing is the paramount to other measures in the mitigation of the spread of viral infection.


Author(s):  
T. A. Borovskaya ◽  
M. E. Poluektova ◽  
A. V. Vychuzhanina ◽  
V. A. Mashanova ◽  
Yu. A. Shchemerova

In experimental studies on rats (males, females) at their infantile stage starting from 10 days, a potential delayed toxic effect of the antiviral drug Kagocel on the reproductive system was studied. The drug was administered for 12 days in a therapeutic dose and at a dose 10-fold higher than the therapeutic one. Reproductive safety was estimated after animals reached the reproductive age (2.5 months). It was found out that the drug, when administered in both doses, does not decrease the fertility of animals, does not induce morphological and pathological changes in the sex glands, and does not have toxic effect on the offspring. Obtained data characterize Kagocel as a preparation with a wide reproductive safety profile and show that it can be used in pediatric practice for infants.


Author(s):  
Prakash Goudanavar ◽  
Ankit Acharya ◽  
Vinay C.H

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. 


Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.


Sign in / Sign up

Export Citation Format

Share Document