Pub Date : 2021-09-01DOI: 10.37285/ijpsn.2021.14.5.5
Anuradha P. Prajapati, Jalpa H Kanzaria, Shailesh V Luhar, Sachin B. Narkhede
The objective of the present work is to formulate, develop and evaluate nasal in situ gel of Pregabalin to provide better therapy for Epilepsy. Pregabalin is BCS class I drug. It is 3rd generation anticonvulsant used in epilepsy in which faster action is required. Nasal route has faster action than oral route, also convenient to unconscious patient. Pregabalin loaded in situ gel, for the treatment of epilepsy to avoid side effects and first pass metabolism associated with conventional treatment and increase bioavailability. Pregabalin was loaded into different polymeric solutions of Polycarbophil and HPMC K4M. The drug was characterized for various parameters like UV-Spectroscopy, FTIR Spectroscopy and DSC study. Excipients were screened for selection of mucoadhesive and gelling polymer. Then the drug was formulated as in situ gel. The experiment was subjected to 32 full factorial design, the concentration of Polycarbophil (X1) and HPMC K4M (X2) were selected as independent variables with % drug release and muco-adhesive strength as dependent variables. The kinetic study was carried out for 30 days. Polycarbophil was selected as mucoadhesive and gelling polymer. The values for X1 and X2 were 0.3922% and 0.5263% relating the % drug release and mucoadhesive strength values were 78.20% CDR at 240 min. and 960 dynes/cm2 respectively for checkpoint batch following zero order and Higuchi kinetic. The formulation was found to be stable for 30 days. The present research will be helpful in order to improve the efficacy and tolerability of the antiepileptic drug therapy. So alternative administration strategy has been investigated which deliver nasally administered medication directly to brain effectively. The intranasal in situ gelling system is a promising novel drug delivery system for an antiepileptic drug Pregabalin which could enhance nasal residence time with increased viscosity and mucoadhesive character and provided better release profile of drug for treating epileptic conditions.
{"title":"Formulation, Development and Evaluation of Nasal In situ Gel of Pregabalin","authors":"Anuradha P. Prajapati, Jalpa H Kanzaria, Shailesh V Luhar, Sachin B. Narkhede","doi":"10.37285/ijpsn.2021.14.5.5","DOIUrl":"https://doi.org/10.37285/ijpsn.2021.14.5.5","url":null,"abstract":"\u0000The objective of the present work is to formulate, develop and evaluate nasal in situ gel of Pregabalin to provide better therapy for Epilepsy. Pregabalin is BCS class I drug. It is 3rd generation anticonvulsant used in epilepsy in which faster action is required. Nasal route has faster action than oral route, also convenient to unconscious patient. Pregabalin loaded in situ gel, for the treatment of epilepsy to avoid side effects and first pass metabolism associated with conventional treatment and increase bioavailability. Pregabalin was loaded into different polymeric solutions of Polycarbophil and HPMC K4M. The drug was characterized for various parameters like UV-Spectroscopy, FTIR Spectroscopy and DSC study. Excipients were screened for selection of mucoadhesive and gelling polymer. Then the drug was formulated as in situ gel. The experiment was subjected to 32 full factorial design, the concentration of Polycarbophil (X1) and HPMC K4M (X2) were selected as independent variables with % drug release and muco-adhesive strength as dependent variables. The kinetic study was carried out for 30 days. Polycarbophil was selected as mucoadhesive and gelling polymer. The values for X1 and X2 were 0.3922% and 0.5263% relating the % drug release and mucoadhesive strength values were 78.20% CDR at 240 min. and 960 dynes/cm2 respectively for checkpoint batch following zero order and Higuchi kinetic. The formulation was found to be stable for 30 days. The present research will be helpful in order to improve the efficacy and tolerability of the antiepileptic drug therapy. So alternative administration strategy has been investigated which deliver nasally administered medication directly to brain effectively. The intranasal in situ gelling system is a promising novel drug delivery system for an antiepileptic drug Pregabalin which could enhance nasal residence time with increased viscosity and mucoadhesive character and provided better release profile of drug for treating epileptic conditions. ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79989804","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-07-01DOI: 10.37285/ijpsn.2021.14.4.7
Y. Kumar, K. M., H. S, M. M
Salbutamol is a short acting, selective beta2-adrenergic receptor agonist used in the treatment of astama and COPD. The aim of this study is to formulate oral disintegrating tablets of salbutamol sulphate to achieve rapid dissolution, absorption and further improving the bioavailability of the drug. Oral disintegrating tablets of salbutamol sulphate were designed with a view to enhance the patient compliance and provide a quick onset of action. The oral disintegrating tablets were prepared by using different synthetic polymers by direct compression method. Development of the formulation in the present study was based on the concentration of superdisintegrants and the properties of the drug. Nine batches of tablets were formulated and evaluated for various parameters: drug content, weight variation, water absorption ratio, wetting time, in vitro disintegration, hardness, friability, thickness uniformity, and in vitro dissolution. A fourier-transform infrared spectroscopy (FTIR) study showed that there were no significant interactions between the drug and the excipients. The prepared tablets were good in appearance and showed acceptable results for hardness and friability. The in vitro disintegrating time of the formulated tablets was found to be 14.39-32.41 sec and the drug content of tablets in all formulations was found to be between 87.48-99.96 %, which complied within the limits established in the Indian pharmacopeia. The study concluded that taste of the drug was masked with the help of sodium saccarhin, flavor and the concentration of super disintegrating agent increases the disintegration time of tablets get decreases. The formulation (F9) had a minimum disintegration time of 14.39 sec and 99.96 % of the drug was released within 20 min.
{"title":"Formulation and Evaluation of Salbutamol Sulphate Taste Masked Oral Disintegrating Tablets","authors":"Y. Kumar, K. M., H. S, M. M","doi":"10.37285/ijpsn.2021.14.4.7","DOIUrl":"https://doi.org/10.37285/ijpsn.2021.14.4.7","url":null,"abstract":"Salbutamol is a short acting, selective beta2-adrenergic receptor agonist used in the treatment of astama and COPD. The aim of this study is to formulate oral disintegrating tablets of salbutamol sulphate to achieve rapid dissolution, absorption and further improving the bioavailability of the drug. Oral disintegrating tablets of salbutamol sulphate were designed with a view to enhance the patient compliance and provide a quick onset of action. The oral disintegrating tablets were prepared by using different synthetic polymers by direct compression method. Development of the formulation in the present study was based on the concentration of superdisintegrants and the properties of the drug. Nine batches of tablets were formulated and evaluated for various parameters: drug content, weight variation, water absorption ratio, wetting time, in vitro disintegration, hardness, friability, thickness uniformity, and in vitro dissolution. A fourier-transform infrared spectroscopy (FTIR) study showed that there were no significant interactions between the drug and the excipients. The prepared tablets were good in appearance and showed acceptable results for hardness and friability. The in vitro disintegrating time of the formulated tablets was found to be 14.39-32.41 sec and the drug content of tablets in all formulations was found to be between 87.48-99.96 %, which complied within the limits established in the Indian pharmacopeia. The study concluded that taste of the drug was masked with the help of sodium saccarhin, flavor and the concentration of super disintegrating agent increases the disintegration time of tablets get decreases. The formulation (F9) had a minimum disintegration time of 14.39 sec and 99.96 % of the drug was released within 20 min.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80653138","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-07-01DOI: 10.37285/ijpsn.2021.14.4.2
Sakhare Sfurti Shamling, S. Chavan, G. Chandrakant, Rutuja Tanaji Kharat, A. Kulkarni
Oral disintegrating tablets are solid dosage form containing medical substances which disintegrate rapidly, usually within few seconds when placed upon tongue requiring no additional water to facilitate swallowing. Solid dosage forms that can be disintegrated, dissolved, or suspended by saliva in the mouth resulting in easy swallowing can provide significant benefits to the pediatric and geriatric population, as well as other patients who prefer the convenience of easily swallowable dosage forms Superdisintegrants are currently approached and utilized in the formulation of the orally disintegrating tablets. The present work includes isolation of starch from Echinochloa Colona and further characterizing it for various physicochemical and phytochemical analysis. The isolated starch has been modified chemically and its disintegrating efficiency has been tested in tablet formulation; the present work also explores the optimization of concentration of starch in formulation of Ibuprofen tablets in comparison with synthetic and natural superdisintegrants. Phytochemical analysis confirmed the presence of starches and carbohydrates. Results indicated that the Echinochloa Colona starch samples could be potential superdisintegrants in orally disintegrating tablets of Ibuprofen. Tablet performance was found to influence by the way of addition of starch, its concentration and the method of tablet preparation. From these results it is possible to conclude that Echinochloa Colona starch could be used as a superdisintegrant.
{"title":"Isolation, Characterization, Chemical Modification and Application of Echinochloa Colona Starch as Tablet Disintegrant","authors":"Sakhare Sfurti Shamling, S. Chavan, G. Chandrakant, Rutuja Tanaji Kharat, A. Kulkarni","doi":"10.37285/ijpsn.2021.14.4.2","DOIUrl":"https://doi.org/10.37285/ijpsn.2021.14.4.2","url":null,"abstract":"Oral disintegrating tablets are solid dosage form containing medical substances which disintegrate rapidly, usually within few seconds when placed upon tongue requiring no additional water to facilitate swallowing. Solid dosage forms that can be disintegrated, dissolved, or suspended by saliva in the mouth resulting in easy swallowing can provide significant benefits to the pediatric and geriatric population, as well as other patients who prefer the convenience of easily swallowable dosage forms Superdisintegrants are currently approached and utilized in the formulation of the orally disintegrating tablets. The present work includes isolation of starch from Echinochloa Colona and further characterizing it for various physicochemical and phytochemical analysis. The isolated starch has been modified chemically and its disintegrating efficiency has been tested in tablet formulation; the present work also explores the optimization of concentration of starch in formulation of Ibuprofen tablets in comparison with synthetic and natural superdisintegrants. Phytochemical analysis confirmed the presence of starches and carbohydrates. Results indicated that the Echinochloa Colona starch samples could be potential superdisintegrants in orally disintegrating tablets of Ibuprofen. Tablet performance was found to influence by the way of addition of starch, its concentration and the method of tablet preparation. From these results it is possible to conclude that Echinochloa Colona starch could be used as a superdisintegrant.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"139 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88545133","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-07-01DOI: 10.37285/ijpsn.2021.14.4.3
Aliasgar J. Kundawala, Khushbu S Chauhan, H. Patel, Swati K. Kurtkoti
Budesonide is an anti-asthmatic agent which is used to control the symptoms of asthma like bronchospasm, oedema. Drug delivered to lung through inhalation will provide systemic and local drug delivery at lower dose in chronic and acute diseases. Dry powder inhalers are the best choice for targeting the anti-asthmatic drugs through pulmonary route. The objective of the present study is to prepare inhalable lipid coated budesonide microparticles by spray drying method so effective delivery of budesonide to the lungs can be achieved. The microparticles in the form of dry powder were obtained by either spray drying liposomal drug suspension or lipid drug suspension. The liposomes were initially prepared by solvent evaporation method using Hydrogenated Soyabean Phosphatidylcholine and Cholesterol (1:1, 1:2, 2:1) as lipid carrier and then spray dried later with mannitol as bulking agent at different lipid to diluent ratio (1:1.25, 1:2.5 & 1:5). The liposomes and liposomal dry powder were evaluated for vesicle size, % entrapment efficiency, in vitro drug release studies, powder characteristics, aerosol performance and stability studies. The liposomes prepared showed vesicle size (2-8 µm), Entrapment efficiency (92.22%) at lipid: drug ratio of (2.5:1) and observed 80.41 % drug release in 24 hrs. Pro-liposomes prepared by spray drying of liposomal drug suspension (LSD1) showed emitted dose, mean mass aerodynamic diameter, geometric standard deviation and fine particle fraction of 99.01%, 3.12 µm, 1.78 and 43.5% along with good powder properties. The spray dried powder was found to be stable at 4 ± 2 °C & 65% ± 5 % RH. The inhalable microparticles containing Budesonide containing lipid dry powder was successfully prepared by spray drying method that showed good aerodynamic properties and stability with mannitol as diluent. The microparticles produced with this novel approach could deliver drug on target via inhalation route and also ease manufacture process at large scale in fewer production steps.
{"title":"Inhalable Spray Dried Pro-Liposome Powder Containing Budesonide for Pulmonary Delivery","authors":"Aliasgar J. Kundawala, Khushbu S Chauhan, H. Patel, Swati K. Kurtkoti","doi":"10.37285/ijpsn.2021.14.4.3","DOIUrl":"https://doi.org/10.37285/ijpsn.2021.14.4.3","url":null,"abstract":"Budesonide is an anti-asthmatic agent which is used to control the symptoms of asthma like bronchospasm, oedema. Drug delivered to lung through inhalation will provide systemic and local drug delivery at lower dose in chronic and acute diseases. Dry powder inhalers are the best choice for targeting the anti-asthmatic drugs through pulmonary route. The objective of the present study is to prepare inhalable lipid coated budesonide microparticles by spray drying method so effective delivery of budesonide to the lungs can be achieved. The microparticles in the form of dry powder were obtained by either spray drying liposomal drug suspension or lipid drug suspension. The liposomes were initially prepared by solvent evaporation method using Hydrogenated Soyabean Phosphatidylcholine and Cholesterol (1:1, 1:2, 2:1) as lipid carrier and then spray dried later with mannitol as bulking agent at different lipid to diluent ratio (1:1.25, 1:2.5 & 1:5). The liposomes and liposomal dry powder were evaluated for vesicle size, % entrapment efficiency, in vitro drug release studies, powder characteristics, aerosol performance and stability studies. The liposomes prepared showed vesicle size (2-8 µm), Entrapment efficiency (92.22%) at lipid: drug ratio of (2.5:1) and observed 80.41 % drug release in 24 hrs. Pro-liposomes prepared by spray drying of liposomal drug suspension (LSD1) showed emitted dose, mean mass aerodynamic diameter, geometric standard deviation and fine particle fraction of 99.01%, 3.12 µm, 1.78 and 43.5% along with good powder properties. The spray dried powder was found to be stable at 4 ± 2 °C & 65% ± 5 % RH. The inhalable microparticles containing Budesonide containing lipid dry powder was successfully prepared by spray drying method that showed good aerodynamic properties and stability with mannitol as diluent. The microparticles produced with this novel approach could deliver drug on target via inhalation route and also ease manufacture process at large scale in fewer production steps.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90872430","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-07-01DOI: 10.37285/ijpsn.2021.14.4.6
B. Yadav, Y. Trilochana, K. Kumari, Saurabh N Singh, A. Sachan
In today’s scenario, fungal and bacterial infections are one of the most challenging pestilential diseases for the health-care professional which is increasing with a very high rate in the growing population, especially among the immune compromised people.The present work involved the study to extract active principles of Moringa concanensis and perform antibacterial and antifungal activity for various extracts. The leaves were dried powdered unexpected using solvents petroleum ether, chloroform, ethanol and water. Chemical tests were performed to ascertain presence of various classes of phyto-constituents like alkaloids, glycosides, saponins, carbohydrates, proteins, amino acids tannins, flavonoids and phenolic substances. All four extracts showed the presence of various phytochemicals responsible for multiple pharmacological activities. The extracts were reconstituted using 1% aqueous solution of carboxy methyl cellulose and were tested for antibacterial and antifungal activity against six microorganisms, namely Bacillus subtilis, Enterobacter aerogenes, Bacillus cereus, Aspergillus Flavus, Aspergillus Niger and Helminthosporium, using well diffusion method. The results of the activity are promising with chloroform extract showing highest inhibitory activity against most of the organisms. All the extracts were able to demonstrate significant activity compared to control inhibition of microorganisms tested and hold key to discover lead molecules after further scientific investigation.
{"title":"Evaluation of Antibacterial and Antifungal Activity of Moringa Concanensis","authors":"B. Yadav, Y. Trilochana, K. Kumari, Saurabh N Singh, A. Sachan","doi":"10.37285/ijpsn.2021.14.4.6","DOIUrl":"https://doi.org/10.37285/ijpsn.2021.14.4.6","url":null,"abstract":"In today’s scenario, fungal and bacterial infections are one of the most challenging pestilential diseases for the health-care professional which is increasing with a very high rate in the growing population, especially among the immune compromised people.The present work involved the study to extract active principles of Moringa concanensis and perform antibacterial and antifungal activity for various extracts. The leaves were dried powdered unexpected using solvents petroleum ether, chloroform, ethanol and water. Chemical tests were performed to ascertain presence of various classes of phyto-constituents like alkaloids, glycosides, saponins, carbohydrates, proteins, amino acids tannins, flavonoids and phenolic substances. All four extracts showed the presence of various phytochemicals responsible for multiple pharmacological activities. The extracts were reconstituted using 1% aqueous solution of carboxy methyl cellulose and were tested for antibacterial and antifungal activity against six microorganisms, namely Bacillus subtilis, Enterobacter aerogenes, Bacillus cereus, Aspergillus Flavus, Aspergillus Niger and Helminthosporium, using well diffusion method. The results of the activity are promising with chloroform extract showing highest inhibitory activity against most of the organisms. All the extracts were able to demonstrate significant activity compared to control inhibition of microorganisms tested and hold key to discover lead molecules after further scientific investigation.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"73 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77398122","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-07-01DOI: 10.37285/ijpsn.2021.14.4.4
Praveen Praveen, G. Jeyabalan
Stem Bark, Root and fruit of Ziziphus oenoplia (Rhamnaceae) has been used in traditional health systems to treat diabetes and many more disorders in southern Asia as India, Sri Lanka and Burma. However hypoglycemic and hypo-lipidemic potential of fruit of this valuable plant is not scientifically validated till date. The aim of present study is to evaluate hypoglycemic and hypo-lipidemic effect of ethanol extracts and solvent fractions of Ziziphus oenoplia fruit. The ethanol extracts and solvent fractions in different dose concentration 100, 200, 400 mg/kg of Ziziphus oenoplia fruit were evaluated for hypo-glycemic effect in single dose and multiple dose study for 21 days as well as for hypo-lipidemic potential in streptozotocin induced diabetic rats. The outcome of present study indicates, crude extract and solvent fractions significantly reduce blood glucose level on normoglycemic and diabetic rats.The acute oral toxicity study of Z. oenoplia fruit extract did not show mortality in the animals at the limit dose of 2g/kg. In STZ induced diabetic rat, maximum BGL lowering effect produced by EEZO400 followed by CF400 after 21 days of treatment. Total cholesterol, triglycerides and low-density lipoprotein was also significantly decreased. The observed result may be due to active principles present in extract and fractions. The result showed the potential effects of Z.oenoplia fruit extract and fractions as hypoglycemic and anti hyper-lipidemic in dose dependant manner compare to glibenclemide as standard drug. The claimed traditional use as anti-diabetic has scientific back ground.
{"title":"Hypoglycemic and anti-lipidemic Evaluation of Fruit Extract and Solvent Fractions of Ziziphus oenoplia in Streptozotocin-Induced Diabetic Rats","authors":"Praveen Praveen, G. Jeyabalan","doi":"10.37285/ijpsn.2021.14.4.4","DOIUrl":"https://doi.org/10.37285/ijpsn.2021.14.4.4","url":null,"abstract":"Stem Bark, Root and fruit of Ziziphus oenoplia (Rhamnaceae) has been used in traditional health systems to treat diabetes and many more disorders in southern Asia as India, Sri Lanka and Burma. However hypoglycemic and hypo-lipidemic potential of fruit of this valuable plant is not scientifically validated till date. The aim of present study is to evaluate hypoglycemic and hypo-lipidemic effect of ethanol extracts and solvent fractions of Ziziphus oenoplia fruit. The ethanol extracts and solvent fractions in different dose concentration 100, 200, 400 mg/kg of Ziziphus oenoplia fruit were evaluated for hypo-glycemic effect in single dose and multiple dose study for 21 days as well as for hypo-lipidemic potential in streptozotocin induced diabetic rats. The outcome of present study indicates, crude extract and solvent fractions significantly reduce blood glucose level on normoglycemic and diabetic rats.The acute oral toxicity study of Z. oenoplia fruit extract did not show mortality in the animals at the limit dose of 2g/kg. In STZ induced diabetic rat, maximum BGL lowering effect produced by EEZO400 followed by CF400 after 21 days of treatment. Total cholesterol, triglycerides and low-density lipoprotein was also significantly decreased. The observed result may be due to active principles present in extract and fractions. The result showed the potential effects of Z.oenoplia fruit extract and fractions as hypoglycemic and anti hyper-lipidemic in dose dependant manner compare to glibenclemide as standard drug. The claimed traditional use as anti-diabetic has scientific back ground. \u0000 ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"11 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87506905","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-07-01DOI: 10.37285/ijpsn.2021.14.4.5
Srinivas Podeti, Suresh Lapaka, R. Chouhan, Nagraj Alpula
Identification of proper microbial sources and optimizing the enzyme production conditions are essential for industrial-scale enzyme production. The present study was done to identify and enhance the production of protease enzyme from an important microbial source Rummeliibacillus stabekisii (TWSS-P-2). Ultra-violet radiation physical method and ethyl methanesulfonate and ethidium bromide dependent chemical methods were considered for mutagenesis. Enzyme assay-dependent screening resulted in identifying Rummeliibacillus stabekisii (TWSS-P-2) as the best strain with optimum protease production that was improved through the chemical treatment mentioned. The strains were tested under various physical and chemical factors including carbon source, nitrogen source, inoculum sizes, pH, temperature to optimize the production of the protein. Submerged fermentation (SmF) was used to assess enzyme production. We were successful in deriving the optimum condition for the protease enzyme production for Rummeliibacillus stabekisii (TWSS-P-2) and the mutagenic effect yielded 2-4 fold better enzyme production.
{"title":"Enhanced Protease Production from Rummeliibacillus Stabekisii (TWSS-P-2) Strain through Mutagenesis and Optimized Culture Conditions","authors":"Srinivas Podeti, Suresh Lapaka, R. Chouhan, Nagraj Alpula","doi":"10.37285/ijpsn.2021.14.4.5","DOIUrl":"https://doi.org/10.37285/ijpsn.2021.14.4.5","url":null,"abstract":"Identification of proper microbial sources and optimizing the enzyme production conditions are essential for industrial-scale enzyme production. The present study was done to identify and enhance the production of protease enzyme from an important microbial source Rummeliibacillus stabekisii (TWSS-P-2). Ultra-violet radiation physical method and ethyl methanesulfonate and ethidium bromide dependent chemical methods were considered for mutagenesis. Enzyme assay-dependent screening resulted in identifying Rummeliibacillus stabekisii (TWSS-P-2) as the best strain with optimum protease production that was improved through the chemical treatment mentioned. The strains were tested under various physical and chemical factors including carbon source, nitrogen source, inoculum sizes, pH, temperature to optimize the production of the protein. Submerged fermentation (SmF) was used to assess enzyme production. We were successful in deriving the optimum condition for the protease enzyme production for Rummeliibacillus stabekisii (TWSS-P-2) and the mutagenic effect yielded 2-4 fold better enzyme production.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"89 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81601623","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-01DOI: 10.37285/ijpsn.2021.14.4.1
Sunitha M. Reddy, Sravani Baskarla
This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.
{"title":"A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems","authors":"Sunitha M. Reddy, Sravani Baskarla","doi":"10.37285/ijpsn.2021.14.4.1","DOIUrl":"https://doi.org/10.37285/ijpsn.2021.14.4.1","url":null,"abstract":"This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis. \u0000 ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"8 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88023542","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-09-15DOI: 10.37285/IJPSN.2020.13.5.6
Jimish R. Patel, Laxman M. Prajapati, H. Joshi, Ujashkumar A. Shah
COVID-19 disease has spread quickly across the globe after its first detection in late December 2019 in Wuhan, China. The disease is considered as a potential global health threat by world health organization due to its high emerging deaths. Coronaviruses are transmitted by respiratory aerosols producing mild upper respiratory infections. Currently, no vaccine or specific COVID-19 inhibitors are available for treatment except repurposed drugs. The COVID-19 virus genome has ~30,000 nucleotides. Its replicase gene encodes overlapping polyproteins necessary for viral replication and transcription. Recently COVID-19 main protease was successfully crystallized and made available in Protein Data Bank for public use. Several studies report medicinal plants to have antiviral bioactivities. Application of in silico computer‐based docking studies involving small molecules could be time saving for irrelevant in vivo models. In the present study, we have investigated 500 natural compounds from different plants having antiviral properties. We have also screened several protease inhibitors and other repurposed drugs claimed to be active against COVID-19. The docking was performed on Autodock vina, using grid size 22, 22, 24 along the X, Y, and Z axes with 1.000 A˚ spacing. The docked positions in binding pockets were visualized using Discovery studio 3.5 software. Most of the repurposed protease inhibitors were having good binding energy, saquinavir being the most potent. Among natural compounds, jervine and isoacteoside were found to be having good binding with protease protein. It was observed that flavonoid was the commonest chemical group amongst most potent natural compounds. The amino acids Thr26, Asn142, Gly143, Ser144, Cys145, His163, and Glu166 showed strong H-bond interactions with docked compounds. The conclusion of the recent study will help researchers to identify the better drug to battle COVID-19. To be brief, our findings emphasize a promising pharmaceutical perspective for targeting main protease of novel coronavirus. However further preclinical and clinical trials should be carried out to validate these potential compounds.
2019年12月下旬在中国武汉首次发现COVID-19后，该疾病迅速在全球传播。由于该病的高新发死亡率，世界卫生组织将其视为潜在的全球健康威胁。冠状病毒通过呼吸道气溶胶传播，产生轻度上呼吸道感染。目前，除了重新利用的药物外，没有疫苗或特定的COVID-19抑制剂可用于治疗。COVID-19病毒基因组有大约3万个核苷酸。它的复制酶基因编码病毒复制和转录所必需的重叠多蛋白。最近，新冠病毒主蛋白酶结晶成功，并在蛋白质数据库中开放使用。一些研究报道药用植物具有抗病毒生物活性。应用基于硅计算机的小分子对接研究可以为不相关的体内模型节省时间。在本研究中，我们研究了来自不同植物的500种具有抗病毒特性的天然化合物。我们还筛选了几种蛋白酶抑制剂和其他据称对COVID-19有活性的重新用途药物。对接在Autodock vina上进行，沿X、Y和Z轴使用网格尺寸为22、22、24，间距为1.000 A˚。使用Discovery studio 3.5软件可视化捆扎袋中的对接位置。大多数重组蛋白酶抑制剂具有良好的结合能，沙奎那韦是最有效的。在天然化合物中，菊苣和异牛油果苷与蛋白酶蛋白结合良好。结果表明，黄酮类化合物是最有效的天然化合物中最常见的化学基团。氨基酸Thr26、Asn142、Gly143、Ser144、Cys145、His163和Glu166与停靠物表现出强烈的氢键相互作用。这项最新研究的结论将有助于研究人员找到更好的药物来对抗COVID-19。简而言之，我们的研究结果强调了针对新型冠状病毒主要蛋白酶的有希望的制药前景。然而，需要进行进一步的临床前和临床试验来验证这些潜在的化合物。
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Pub Date : 2020-06-10DOI: 10.37285/ijpsn.2010.3.3.15
S. Debnath, Malla Reddy V, Manjunath S Y, Francis Saleshier M
Ethyl2-amino-4-(4-chlorophenyl)-6-(4-methylphenyl)-4H-pyran-3-carboxylate and 2-amino-4-(4-chlorophenyl)-6-(4-methylphenyl)-4H-pyran-3-carbonitrile and their respective Schiffs bases were prepared by conventional and microwave methods. The required α, β - unsaturated ketone (chalcone) were prepared by the Claisen-Schmidt reaction using appropriate aromatic aldehyde and me
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