Pub Date : 2017-03-25DOI: 10.25258/IJPCR.V9I3.8324
V. Suganya, V. Anuradha
Encapsulation is a process of enclosing the substances within an inert material which protects from environment as well as control drug release. Recently, two type of encapsulation has been performed in several research. Nanoencapsulation is the coating of various substances within another material at sizes on the nano scale. Microencapsulation is similar to nanoencapsulation aside from it involving larger particles and having been done for a greater period of time than nanoencapsulation. Encapsulation is a new technology that has wide applications in pharmaceutical industries, agrochemical, food industries and cosmetics. In this review, the difference between micro and nano encapsulation has been explained. This article gives an overview of different methods and reason for encapsulation. The advantages and disadvantages of micro and nano encapsulation technology were also clearly mentioned in this paper.
{"title":"Microencapsulation and Nanoencapsulation: A Review","authors":"V. Suganya, V. Anuradha","doi":"10.25258/IJPCR.V9I3.8324","DOIUrl":"https://doi.org/10.25258/IJPCR.V9I3.8324","url":null,"abstract":"Encapsulation is a process of enclosing the substances within an inert material which protects from environment as well as\u0000control drug release. Recently, two type of encapsulation has been performed in several research. Nanoencapsulation is\u0000the coating of various substances within another material at sizes on the nano scale. Microencapsulation is similar to\u0000nanoencapsulation aside from it involving larger particles and having been done for a greater period of time than\u0000nanoencapsulation. Encapsulation is a new technology that has wide applications in pharmaceutical industries,\u0000agrochemical, food industries and cosmetics. In this review, the difference between micro and nano encapsulation has been\u0000explained. This article gives an overview of different methods and reason for encapsulation. The advantages and\u0000disadvantages of micro and nano encapsulation technology were also clearly mentioned in this paper.","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77293864","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 : 2017-03-25DOI: 10.25258/IJPCR.V9I3.8322
P. Apostol, Mark Anthony G. Fran, Chien-Chang Shen, C. Ragasa
Chemical investigation of the dichloromethane extract of Premna nauseosa Blanco afforded squalene (1) and a mixture of ?-sitosterol (2) and stigmasterol (3) in about 6:1 ratio. The structures of 1-3 were identified by comparison of their NMR data with literature data
{"title":"Triterpene and Sterols from Premna nauseosa Blanco","authors":"P. Apostol, Mark Anthony G. Fran, Chien-Chang Shen, C. Ragasa","doi":"10.25258/IJPCR.V9I3.8322","DOIUrl":"https://doi.org/10.25258/IJPCR.V9I3.8322","url":null,"abstract":"Chemical investigation of the dichloromethane extract of Premna nauseosa Blanco afforded squalene (1) and a mixture of\u0000?-sitosterol (2) and stigmasterol (3) in about 6:1 ratio. The structures of 1-3 were identified by comparison of their NMR\u0000data with literature data","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"105 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84421136","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}
The anthelmintic resistance has limited the control of gastrointestinal nematodes of small ruminants and thus has awakened interest in the study of plants extract as a source of anthelmintics. These experiments were carried out to evaluate the in vitro efficacy of Jatrophacurcas latex extract against Haemonchuscontortus larval motility. To evaluate the larvicidal activity, H.contortus L3 were incubated with the extracts with varying concentration of 5 mg/mL, 10 mg/mL, 15 mg/mL and 20 mg/mL at 27°C for 48, 72 and 96 hrs. The results were subjected to the Kruskal-Wallis test (P<0.05). The extracts showed dose-dependent larvicidal effects. These results suggest that J.curcas can be used to control gastrointestinal nematodes of small ruminants.
{"title":"Effect of Jatropha curcas Latex on L3 Haemonchus contortus Larval Motility","authors":"Noorzaid Muhamad, Syahirah Sazeli, Resni Mona, Jannathul Firdous","doi":"10.25258/IJPCR.V9I3.8317","DOIUrl":"https://doi.org/10.25258/IJPCR.V9I3.8317","url":null,"abstract":"The anthelmintic resistance has limited the control of gastrointestinal nematodes of small ruminants and thus has awakened interest in the study of plants extract as a source of anthelmintics. These experiments were carried out to evaluate the in vitro efficacy of Jatrophacurcas latex extract against Haemonchuscontortus larval motility. To evaluate the larvicidal activity, H.contortus L3 were incubated with the extracts with varying concentration of 5 mg/mL, 10 mg/mL, 15 mg/mL and 20 mg/mL at 27°C for 48, 72 and 96 hrs. The results were subjected to the Kruskal-Wallis test (P<0.05). The extracts showed dose-dependent larvicidal effects. These results suggest that J.curcas can be used to control gastrointestinal nematodes of small ruminants.","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"64 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76701267","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 : 2017-03-25DOI: 10.25258/IJPCR.V9I3.8326
Lurwan Muazu, Y. Abdullahi, Z. Umar
A prospective study was carried out to determine the prevalence of human intestinal parasitic nematodes among outpatients attending Wudil General Hospital, Wudil Local Government Area of Kano State, Nigeria. A total of 56 stool samples were randomly collected from the outpatients; processed and examined (macroscopic and microscopic) by formal ether sedimentation techniques. The prevalence of human intestinal parasitic nematode among the patient in the study area was 46.4%. The Males had the highest (48.98%) infection rate, while females had the least (28.6%) prevalence rate, however, this is not statistically significant (p>0.05). The 36-40years age groups had the highest prevalence of 75%, while 21-25years age groups had the least prevalence rate of 25%, the difference in prevalence among the ages was found to be statistically not significant (p>0.05). Strongyloides stercoralis had the highest prevalence of 30.36% while Trichuris trichiura had the least prevalence rate of 3.57%, the differences among the species of human intestinal parasitic nematode was found to be statistically not significant (p>0.05). The control of human intestinal parasitic nematode should be done by adopting drug treatment for those already infected similar to the national immunization program, improve standard sanitation and health services in Wudil L.G.A, particularly the rural area.
{"title":"Prevalence of Human Intestinal Parasitic Nematode Among OutPatients Attending Wudil General Hospital, Kano State, Nigeria","authors":"Lurwan Muazu, Y. Abdullahi, Z. Umar","doi":"10.25258/IJPCR.V9I3.8326","DOIUrl":"https://doi.org/10.25258/IJPCR.V9I3.8326","url":null,"abstract":"A prospective study was carried out to determine the prevalence of human intestinal parasitic nematodes among outpatients\u0000attending Wudil General Hospital, Wudil Local Government Area of Kano State, Nigeria. A total of 56 stool\u0000samples were randomly collected from the outpatients; processed and examined (macroscopic and microscopic) by formal\u0000ether sedimentation techniques. The prevalence of human intestinal parasitic nematode among the patient in the study area\u0000was 46.4%. The Males had the highest (48.98%) infection rate, while females had the least (28.6%) prevalence rate,\u0000however, this is not statistically significant (p>0.05). The 36-40years age groups had the highest prevalence of 75%, while\u000021-25years age groups had the least prevalence rate of 25%, the difference in prevalence among the ages was found to be\u0000statistically not significant (p>0.05). Strongyloides stercoralis had the highest prevalence of 30.36% while Trichuris\u0000trichiura had the least prevalence rate of 3.57%, the differences among the species of human intestinal parasitic nematode\u0000was found to be statistically not significant (p>0.05). The control of human intestinal parasitic nematode should be done\u0000by adopting drug treatment for those already infected similar to the national immunization program, improve standard\u0000sanitation and health services in Wudil L.G.A, particularly the rural area.","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91098428","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 : 2017-03-25DOI: 10.25258/IJPCR.V9I3.8329
S. S, R. Samson, C. Amalraj, S. Sundaresan
Neglected pain in neonates leads to various ill effects and it can be prevented by using simple and safe non-pharmacological pain relieving measures. Pharmacologic agents are not recommended in neonates for acute pain due toinvasive procedures however, administration of 24% oralsucrose solutionis found to be effective. The objective of this study was to assess the efficacy of 24%oral sucrose in combination with Facilitated tucking during BCG Vaccination through intradermalroute in term neonates which is not done elsewhere. Fifty five healthy term neonates who fulfilled the inclusion criteria such as gestational age above 37 weeks, within 24 hoursof birth age, and neonates delivered only through spontaneous vaginal delivery were included in the study. The study intervention consists of administration of 2 ml of oral 24% sucrose 2 minutes before BCG Vaccination through intradermal route and Facilitated tuckingat the time of vaccination. The primary outcome measure of cumulative NIPS score at 0, 3,5 minuteswas not significant in both the study groups. Whereas there was significant reduction in the level of pain and mean cry time in the neonates of sucrose group. Heart rateand oxygen saturation after intradermal injection also showed significant (p less than 0.001) differenceamong the neonates, who received 24% of oral sucroseand Facilitated tucking than for neonates of control group. Thus oral (24%)sucrose solution given 2 minutes before injection was effective in reducing level of neonatal pain following Intradermal Vaccination. It is a simple, safe and fast acting analgesic and should be considered for minor invasive procedures in term neonates which last for 5-7minutes.
{"title":"Sucrose and Facilitated Tucking for Pain Among Neonates Receiving Vaccination, in Puducherry","authors":"S. S, R. Samson, C. Amalraj, S. Sundaresan","doi":"10.25258/IJPCR.V9I3.8329","DOIUrl":"https://doi.org/10.25258/IJPCR.V9I3.8329","url":null,"abstract":"Neglected pain in neonates leads to various ill effects and it can be prevented by using simple and safe non-pharmacological\u0000pain relieving measures. Pharmacologic agents are not recommended in neonates for acute pain due toinvasive procedures\u0000however, administration of 24% oralsucrose solutionis found to be effective. The objective of this study was to assess the\u0000efficacy of 24%oral sucrose in combination with Facilitated tucking during BCG Vaccination through intradermalroute in\u0000term neonates which is not done elsewhere. Fifty five healthy term neonates who fulfilled the inclusion criteria such as\u0000gestational age above 37 weeks, within 24 hoursof birth age, and neonates delivered only through spontaneous vaginal\u0000delivery were included in the study. The study intervention consists of administration of 2 ml of oral 24% sucrose 2 minutes\u0000before BCG Vaccination through intradermal route and Facilitated tuckingat the time of vaccination. The primary outcome\u0000measure of cumulative NIPS score at 0, 3,5 minuteswas not significant in both the study groups. Whereas there was\u0000significant reduction in the level of pain and mean cry time in the neonates of sucrose group. Heart rateand oxygen\u0000saturation after intradermal injection also showed significant (p less than 0.001) differenceamong the neonates, who received 24%\u0000of oral sucroseand Facilitated tucking than for neonates of control group. Thus oral (24%)sucrose solution given 2 minutes\u0000before injection was effective in reducing level of neonatal pain following Intradermal Vaccination. It is a simple, safe and\u0000fast acting analgesic and should be considered for minor invasive procedures in term neonates which last for 5-7minutes.","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"36 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87044973","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 : 2017-03-25DOI: 10.25258/ijpcr.v9i3.8323
N. RaviKiranS, M. Gowrav, H. Gangadharappa, G. Ravi
Background of the study: Difficult lies at the core of drug producer successful operation. Laboratory testing, which is compulsory by the CGMP regulations are required to check that components, containers and closures, in-process materials, and finished products conform to specifications, including stability specifications. Objective of the study: The objective of the investigation procedure should clearly state when the investigation is required, and define OOS, OOT, and aberrant results. OOS results are most often generated due to laboratory or manufacturing-related errors, the setting of inappropriate specifications, or poor method development. Materials and Methods: The current work is an effort to deliberate several aspects of finding the root cause for the OOS during the finished product analysis by using HPLC. Results and Discussion: Product’s individual unknown impurity was not in specification limit and, hence study carried out to find the root cause. Conclusion: After conducting detail investigation it was proved that an analyst conducted the analysis of the product after the due date to expiry.
{"title":"Management of Out of Specification (OOS) for Finished Product","authors":"N. RaviKiranS, M. Gowrav, H. Gangadharappa, G. Ravi","doi":"10.25258/ijpcr.v9i3.8323","DOIUrl":"https://doi.org/10.25258/ijpcr.v9i3.8323","url":null,"abstract":"Background of the study: Difficult lies at the core of drug producer successful operation. Laboratory testing, which is compulsory by the CGMP regulations are required to check that components, containers and closures, in-process materials, and finished products conform to specifications, including stability specifications. Objective of the study: The objective of the investigation procedure should clearly state when the investigation is required, and define OOS, OOT, and aberrant results. OOS results are most often generated due to laboratory or manufacturing-related errors, the setting of inappropriate specifications, or poor method development. Materials and Methods: The current work is an effort to deliberate several aspects of finding the root cause for the OOS during the finished product analysis by using HPLC. Results and Discussion: Product’s individual unknown impurity was not in specification limit and, hence study carried out to find the root cause. Conclusion: After conducting detail investigation it was proved that an analyst conducted the analysis of the product after the due date to expiry.","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86405772","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 : 2017-03-25DOI: 10.25258/ijpcr.v9i3.8325
S. Mahfouz, Z. Ikawati, D. Wahyono
COPD therapy aims to prevent and overcome acute exacerbation on COPD which could be fatal and even lead to death. Thus, it must be prevented with optimum medication during stable condition. Bronchodilator in the form of inhalation are preferred in COPD medication because systemic bronchodilator has many side effects compared to that of topical bronchodilator (inhalation). DPI (dry-powder inhaler) has been developed and introduced to the market since 1967 as a solution or choice concerning MDI (metered-dose inhaler) setbacks where patients felt difficult in coordinating hands and lungs. Evidences suggested that multi-unit dose DPI such as Diskus® offered most reliable and consistent performance and it is preferred by patients. The improper using of inhaler is one of the main causes holding up asthma control since it can affect patients dosage intake which is not optimal. This research aimed to know the efficacy of Diskus® preparation usage education given to COPD patients. Method used in this research was one study group pre-test dan post test. The number of respondents involved in this research was 55 respondents. The result of t-test suggested that t-count is fewer than p-value (0.05) suggesting that there was difference between pre and post test score as a result of oral or motor evaluation. It is then concluded that Diskus® usage education affected the patients in the improvement of inhaler usage accuracy based on oral and motor evaluation. This research only reviewed COPD patients skill in using Diskus®, thus it is required to conduct further research to dig the understanding in the usage of Diskus® like drug indications, interval, how to notice side effects and how to overcome them. Also, this research only reviewed knowledge increase, but yet described outcome improvement from the using of COPD therapy itself.
{"title":"The Effectiveness of Video Education How to Use Diskus® DryPowder inhaler on Out-Patients Copd In Mojokerto, Indonesia","authors":"S. Mahfouz, Z. Ikawati, D. Wahyono","doi":"10.25258/ijpcr.v9i3.8325","DOIUrl":"https://doi.org/10.25258/ijpcr.v9i3.8325","url":null,"abstract":"COPD therapy aims to prevent and overcome acute exacerbation on COPD which could be fatal and even lead to death. Thus, it must be prevented with optimum medication during stable condition. Bronchodilator in the form of inhalation are preferred in COPD medication because systemic bronchodilator has many side effects compared to that of topical bronchodilator (inhalation). DPI (dry-powder inhaler) has been developed and introduced to the market since 1967 as a solution or choice concerning MDI (metered-dose inhaler) setbacks where patients felt difficult in coordinating hands and lungs. Evidences suggested that multi-unit dose DPI such as Diskus® offered most reliable and consistent performance and it is preferred by patients. The improper using of inhaler is one of the main causes holding up asthma control since it can affect patients dosage intake which is not optimal. This research aimed to know the efficacy of Diskus® preparation usage education given to COPD patients. Method used in this research was one study group pre-test dan post test. The number of respondents involved in this research was 55 respondents. The result of t-test suggested that t-count is fewer than p-value (0.05) suggesting that there was difference between pre and post test score as a result of oral or motor evaluation. It is then concluded that Diskus® usage education affected the patients in the improvement of inhaler usage accuracy based on oral and motor evaluation. This research only reviewed COPD patients skill in using Diskus®, thus it is required to conduct further research to dig the understanding in the usage of Diskus® like drug indications, interval, how to notice side effects and how to overcome them. Also, this research only reviewed knowledge increase, but yet described outcome improvement from the using of COPD therapy itself.","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"60 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84882375","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 : 2017-03-25DOI: 10.25258/IJPCR.V9I3.8327
S. Srividya, G. Sridevi, A. Manimegalai
The ethanolic extract of the leaves of Cassia occidentalis (Co) were subjected to phytochemical analysis by standard qualitative analysis and the invitro antioxidant activity was evaluated by determination of total antioxidant capacity, 1.1- diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, hydrogen peroxide (H2O2) radical scavenging activity, superoxide scavenging activity and Ferric reducing anti oxidant potential (FRAP). The analyses revealed that the ethanolic extract of Co was able to efficiently scavenge the free radicals in a dose dependant manner. The results were compared with the standard antioxidant ascorbic acid. The results have shown that crude ethanolic extract of the leaves of Co showed excellent antioxidant activity due to the presence of bioactive compounds namely alkaloids, betacyanin, cardiac glycosides, coumarins, flavonoids, phenols, steroids, saponins, tannins, terpenoids, anthraquinones and emodins.
{"title":"Phytochemical Screening and In Vitro Antioxidant Activity of Ethanolic Extract of Cassia occidentalis","authors":"S. Srividya, G. Sridevi, A. Manimegalai","doi":"10.25258/IJPCR.V9I3.8327","DOIUrl":"https://doi.org/10.25258/IJPCR.V9I3.8327","url":null,"abstract":"The ethanolic extract of the leaves of Cassia occidentalis (Co) were subjected to phytochemical analysis by standard\u0000qualitative analysis and the invitro antioxidant activity was evaluated by determination of total antioxidant capacity, 1.1-\u0000diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, hydrogen peroxide (H2O2) radical scavenging activity,\u0000superoxide scavenging activity and Ferric reducing anti oxidant potential (FRAP). The analyses revealed that the ethanolic\u0000extract of Co was able to efficiently scavenge the free radicals in a dose dependant manner. The results were compared\u0000with the standard antioxidant ascorbic acid. The results have shown that crude ethanolic extract of the leaves of Co showed\u0000excellent antioxidant activity due to the presence of bioactive compounds namely alkaloids, betacyanin, cardiac glycosides,\u0000coumarins, flavonoids, phenols, steroids, saponins, tannins, terpenoids, anthraquinones and emodins.","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"104 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87710569","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 : 2017-02-25DOI: 10.25258/IJPCR.V9I2.8298
Mayson H. Alkhatib, Dalal A. Al-Saedi, W. S. Backer
The combination of anticancer drugs in nanoparticles has great potential as a promising strategy to maximize efficacies by eradicating resistant, reduce the dosage of the drug and minimize toxicities on the normal cells. Gemcitabine (GEM), a nucleoside analogue, and atorvastatin (ATV), a cholesterol lowering agent, have shown anticancer effect with some limitations. The objective of this in vitro study was to evaluate the antitumor activity of the combination therapy of GEM and ATVencapsulated in a microemulsion (ME) formulation in the HCT116 colon cancer cells. The cytotoxicity and efficacy of the formulation were assessed by the 3- (4,5dimethylthiazole-2-yl)-2,5-diphyneltetrazolium bromide (MTT) assay. The mechanism of cell death was examined by observing the morphological changes of treated cells under light microscope, identifying apoptosis by using the ApopNexin apoptosis detection kit, and viewing the morphological changes in the chromatin structure stained with 4?,6-diamidino-2-phenylindole (DAPI) under the inverted fluorescence microscope. It has been found that reducing the concentration of GEM loaded on ME (GEM-ME) from 5?M to 1.67?M by combining it with 3.33?M of ATV in a ME formulation (GEM/2ATV-ME) has preserved the strong cytotoxicity of GEM-ME against HCT116 cells. The current study proved that formulating GEM with ATV in ME has improved the therapeutic potential of GEM and ATV as anticancer drugs.
{"title":"Cytotoxic Effect of the Combination of Gemcitabine and Atorvastatin Loaded in Microemulsion on the HCT116 Colon Cancer Cells","authors":"Mayson H. Alkhatib, Dalal A. Al-Saedi, W. S. Backer","doi":"10.25258/IJPCR.V9I2.8298","DOIUrl":"https://doi.org/10.25258/IJPCR.V9I2.8298","url":null,"abstract":"The combination of anticancer drugs in nanoparticles has great potential as a promising strategy to maximize efficacies by eradicating resistant, reduce the dosage of the drug and minimize toxicities on the normal cells. Gemcitabine (GEM), a nucleoside analogue, and atorvastatin (ATV), a cholesterol lowering agent, have shown anticancer effect with some limitations. The objective of this in vitro study was to evaluate the antitumor activity of the combination therapy of GEM and ATVencapsulated in a microemulsion (ME) formulation in the HCT116 colon cancer cells. The cytotoxicity and efficacy of the formulation were assessed by the 3- (4,5dimethylthiazole-2-yl)-2,5-diphyneltetrazolium bromide (MTT) assay. The mechanism of cell death was examined by observing the morphological changes of treated cells under light microscope, identifying apoptosis by using the ApopNexin apoptosis detection kit, and viewing the morphological changes in the chromatin structure stained with 4?,6-diamidino-2-phenylindole (DAPI) under the inverted fluorescence microscope. It has been found that reducing the concentration of GEM loaded on ME (GEM-ME) from 5?M to 1.67?M by combining it with 3.33?M of ATV in a ME formulation (GEM/2ATV-ME) has preserved the strong cytotoxicity of GEM-ME against HCT116 cells. The current study proved that formulating GEM with ATV in ME has improved the therapeutic potential of GEM and ATV as anticancer drugs.","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"33 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-02-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88314981","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 : 2017-02-25DOI: 10.25258/IJPCR.V9I2.8294
A. Puspaningtyas
A new compound of Mefenamic Acid derivate, 4-nitrobenzoyl-mefenamic acid has been synthesized by benzoylation reaction between mefenamic acid and 4-nitrobenzoyl chloride after prediction by in silico study/molecular approach. A derivative of mefenamic acid (4-NO2-benzoyl-mefenamic acid) has been synthesized for increase its activity as candidate of analgesic drug/inhibitor COX-2 (Cyclooxigenase-2). This compound has been purified by Column Chromatography and analyzed using TLC-Densitometry to determine purity with Rf value 0,8. The spot has good purity and then it was identified this structure using H-NMR 400 MHz and FTIR-KBr. The result showed that this compound is 4-nitrobenzoyl-mefenamic acid (4NBMA). 4NBMA gives white yellow color with melting point 198-199C. Finally, 4NBMA was tested analgetic activity by hot plate method and it showed that 4-nitrobenzoyl-mefenamic acid has been higher activity than mefenamic acid. Keyword: 4-nitrobenzoyl-mefenamic acid, analgesic, benzoylation, molecular approach. INTRODUCTION Pain is a multidimentional sensory experience. International Association for the Study of Pain (IASP) defines that pain is a sensory and unpleasant emotional experience associated with tissue damage, both actual and potential. Chronic pain becomes a serious problem if it increases rate of pain and gives chronic prevalence. Pain is one of the most frequently reported symptom occurs in one from six people in the population and it is estimated to occur in 2-40% of adult population. Some studies estimate that the prevalence of chronic pain in Europe is up to 55.2%. In Indonesia, the population of the elderly, reported that 25-50% of them experienced pain. Chronic pain causes increasing health care costs. The research in the United States showed that the cost yearly for chronic pain is estimated around 100 billion dollars. Mefenamic acid is a drug in the market as NSAIDs (Non-steroidal AntiInflammatory Drugs) which has long been used as an analgesic-inflammatory COX and widely used in the world for treatment of diseases to relieve pain/pain and inflammation such as rheumatoid arthritis, toothache, gout and peripheral muscle pain. In the effort to design and develop new drugs, the first step is modification of commercial drug that has been known its molecular structure and biological activity and was become guidance based on a systematic and rational research to reduce trial and error. Further guidance from lead compounds were developed and modified that become new compounds/derivatives and then was tested this biological activity. Because of extensive use of mefenamic acid so we effort to develop new drugs and created derivatives. Based on previous research, mefenamic acid was substituted benzenesulfonic, bromo anthranilic, paracetamol, phenoxybenzoic, cyclocarboimide the coupling reaction, cyclourea, esters and amides, hydrazine and hidramin can enhance the analgesic effect of anti-inflammatory and reduce the side effects (ulcers). In thi
经硅研究/分子方法预测，甲氧胺酸与4-硝基苯甲酰氯发生苯甲酰化反应，合成了甲氧胺酸衍生物4-硝基苯甲酰甲氧胺酸。合成了甲氧胺酸的衍生物(4- no2 -苯甲酰甲氧胺酸)，以提高其作为镇痛药物/抑制剂COX-2(环氧化酶-2)的候选活性。该化合物经柱层析纯化，并用tlc -密度测定法测定纯度，Rf值为0,8。该斑点具有良好的纯度，然后用400 MHz的H-NMR和FTIR-KBr对该结构进行了鉴定。结果表明，该化合物为4-硝基苯甲酰甲胺酸(4NBMA)。nbma呈白色黄色，熔点198-199C。最后用热板法测定了4-硝基苯甲酰甲胺酸的活性，结果表明4-硝基苯甲酰甲胺酸的活性高于甲胺酸。关键词:硝基苯甲酰甲胺酸，镇痛药，苯甲酰化，分子途径。疼痛是一种多维度的感官体验。国际疼痛研究协会(IASP)将疼痛定义为一种与组织损伤相关的感官和不愉快的情绪体验，包括实际的和潜在的。慢性疼痛是一个严重的问题，如果它增加了疼痛率和慢性患病率。疼痛是最常见的症状之一，在人群中每六个人中就有一个发生疼痛，估计在2-40%的成年人中发生疼痛。一些研究估计，欧洲慢性疼痛的患病率高达55.2%。在印度尼西亚，老年人中有25-50%的人经历过疼痛。慢性疼痛会增加医疗保健费用。美国的研究表明，每年用于慢性疼痛的费用估计在1000亿美元左右。甲氧胺酸作为非甾体抗炎药(NSAIDs, non - steroids AntiInflammatory Drugs，非甾体抗炎药)在市场上早已被用作止痛-炎症的COX，在国际上广泛用于治疗诸如类风湿关节炎、牙痛、痛风、外周肌痛等疾病，以缓解疼痛/疼痛和炎症。在设计和开发新药的过程中，第一步是对已经了解其分子结构和生物活性的商品药物进行修饰，并在系统、合理的研究基础上成为指导，以减少试验和错误。从先导化合物中进一步开发和修饰成新的化合物/衍生物，然后测试其生物活性。由于甲氧胺酸的广泛使用，所以我们努力开发新药和创造衍生物。基于前人的研究，甲氧胺酸被取代苯磺酸、溴苯甲酸、对乙酰氨基酚、苯氧苯甲酸、环碳酰亚胺的偶联反应，环脲、酯类和酰胺类、肼和水牛明可增强抗炎镇痛作用，减少副作用(溃疡)。本研究采用toppliss理论对苯甲酰衍生物进行取代，并用分子方法进行预测。基于Jayaselli等和Susilowati的研究，通过苯甲酰化反应对扑热息痛和吡罗西康衍生物等非甾体抗炎药进行了苯甲酰取代，其生物活性比先导化合物更强。我们使用了几个取代基，苯甲酰衍生物是基于Topliss理论，通过亲脂性，电子和空间参数预测作为取代基。与生物膜渗透速率相关的亲脂性参数。电子参数通过电离和极化过程参与药物与受体相互作用的过程，从而总体上提高了药物的生物有效性。立体参数与化合物与细胞内受体相互作用的相容性有关，它影响最大的结合方向，从而增加活性。亲脂性的提高可以通过插入非极性基团如芳香环来实现，而电子性能的提高可以通过插入电负性取代基如空间卤素来实现。立体位阻特性可以通过创造一个更大的结构来实现，作为一个屏障，促进药物和受体活性位点之间的相互作用。而我们通过增加亲脂性、电子性和立体参数的官能团修饰甲苯胺酸，影响DOI号:10.25258/ ijppr .v9i1.8294 Puspaningtyasm等/ Drug Development of…IJPCR，第9卷，第2期:2017年2月124页生物活性。甲苯甲酰衍生物与甲苯胺酸通过亲核加成反应合成甲苯胺酸衍生物。该机制如图1所示。通过与Molegro虚拟Docker (MVD)对接的分子方法，可以在合成前预测甲苯胺酸衍生物的活性。
{"title":"Drug Development of Mefenamic Acid Derivatives as Analgesic by Molecular Approach","authors":"A. Puspaningtyas","doi":"10.25258/IJPCR.V9I2.8294","DOIUrl":"https://doi.org/10.25258/IJPCR.V9I2.8294","url":null,"abstract":"A new compound of Mefenamic Acid derivate, 4-nitrobenzoyl-mefenamic acid has been synthesized by benzoylation reaction between mefenamic acid and 4-nitrobenzoyl chloride after prediction by in silico study/molecular approach. A derivative of mefenamic acid (4-NO2-benzoyl-mefenamic acid) has been synthesized for increase its activity as candidate of analgesic drug/inhibitor COX-2 (Cyclooxigenase-2). This compound has been purified by Column Chromatography and analyzed using TLC-Densitometry to determine purity with Rf value 0,8. The spot has good purity and then it was identified this structure using H-NMR 400 MHz and FTIR-KBr. The result showed that this compound is 4-nitrobenzoyl-mefenamic acid (4NBMA). 4NBMA gives white yellow color with melting point 198-199C. Finally, 4NBMA was tested analgetic activity by hot plate method and it showed that 4-nitrobenzoyl-mefenamic acid has been higher activity than mefenamic acid. Keyword: 4-nitrobenzoyl-mefenamic acid, analgesic, benzoylation, molecular approach. INTRODUCTION Pain is a multidimentional sensory experience. International Association for the Study of Pain (IASP) defines that pain is a sensory and unpleasant emotional experience associated with tissue damage, both actual and potential. Chronic pain becomes a serious problem if it increases rate of pain and gives chronic prevalence. Pain is one of the most frequently reported symptom occurs in one from six people in the population and it is estimated to occur in 2-40% of adult population. Some studies estimate that the prevalence of chronic pain in Europe is up to 55.2%. In Indonesia, the population of the elderly, reported that 25-50% of them experienced pain. Chronic pain causes increasing health care costs. The research in the United States showed that the cost yearly for chronic pain is estimated around 100 billion dollars. Mefenamic acid is a drug in the market as NSAIDs (Non-steroidal AntiInflammatory Drugs) which has long been used as an analgesic-inflammatory COX and widely used in the world for treatment of diseases to relieve pain/pain and inflammation such as rheumatoid arthritis, toothache, gout and peripheral muscle pain. In the effort to design and develop new drugs, the first step is modification of commercial drug that has been known its molecular structure and biological activity and was become guidance based on a systematic and rational research to reduce trial and error. Further guidance from lead compounds were developed and modified that become new compounds/derivatives and then was tested this biological activity. Because of extensive use of mefenamic acid so we effort to develop new drugs and created derivatives. Based on previous research, mefenamic acid was substituted benzenesulfonic, bromo anthranilic, paracetamol, phenoxybenzoic, cyclocarboimide the coupling reaction, cyclourea, esters and amides, hydrazine and hidramin can enhance the analgesic effect of anti-inflammatory and reduce the side effects (ulcers). In thi","PeriodicalId":19889,"journal":{"name":"Pharmaceutical and Clinical Research","volume":"67 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-02-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87947989","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}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：