Pub Date : 2023-08-25DOI: 10.25004/ijpsdr.2023.150413
Rajavenkata P Patha, Karunakar Dasa, R. Bhoomireddy, Srinivas R Thumu
A sensitive and selective liquid chromatography-mass spectrometry (LC-MS/MS) method using multiple reaction monitoring (MRM) mode was developed and validated for trace analysis of 4-(chloromethyl)-1, 2-dimethoxybenzene (Veratryl chloride) a potential genotoxic impurity in Ivabradine hydrochloride (IVB). Chromatographic separation was performed on a Poroshell 120EC C18 (50 × 3.0 mm, 2.7 μm) column using a mixture of 10 mM ammonium formate and acetonitrile in isocratic elution mode at a 0.25 mL/min flow rate. A simple pre-column derivatization with di-ethylamine was employed for the derivatization of the veratryl chloride. The developed LC-MS/MS method was linear and accurate in the 1.5–10.0 ppm concentration range with r2 ˃ 0.999 and percent recoveries greater than 90%. The developed method was precise with RSD (%) of not more than 4.5%. In-silico genotoxicity and carcinogenicity potential of veratryl chloride was assessed using ICH M7 principles found to be positive. The developed method can identify and quantify veratryl chloride in IVB, hence can be applied by quality control labs of pharmaceutical industries for trace quantification.
{"title":"In-silico Toxicity Assessment and Trace Level Quantification of Veratryl Chloride a Potential Genotoxic Impurity in Ivabradine Hydrochloride using LC-MS/MS","authors":"Rajavenkata P Patha, Karunakar Dasa, R. Bhoomireddy, Srinivas R Thumu","doi":"10.25004/ijpsdr.2023.150413","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150413","url":null,"abstract":"A sensitive and selective liquid chromatography-mass spectrometry (LC-MS/MS) method using multiple reaction monitoring (MRM) mode was developed and validated for trace analysis of 4-(chloromethyl)-1, 2-dimethoxybenzene (Veratryl chloride) a potential genotoxic impurity in Ivabradine hydrochloride (IVB). Chromatographic separation was performed on a Poroshell 120EC C18 (50 × 3.0 mm, 2.7 μm) column using a mixture of 10 mM ammonium formate and acetonitrile in isocratic elution mode at a 0.25 mL/min flow rate. A simple pre-column derivatization with di-ethylamine was employed for the derivatization of the veratryl chloride. The developed LC-MS/MS method was linear and accurate in the 1.5–10.0 ppm concentration range with r2 ˃ 0.999 and percent recoveries greater than 90%. The developed method was precise with RSD (%) of not more than 4.5%. In-silico genotoxicity and carcinogenicity potential of veratryl chloride was assessed using ICH M7 principles found to be positive. The developed method can identify and quantify veratryl chloride in IVB, hence can be applied by quality control labs of pharmaceutical industries for trace quantification.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139349254","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 : 2023-08-25DOI: 10.25004/ijpsdr.2023.150406
A. Naveena, J. Jeyasundari, P.V Priya, A. Athithan
Bimetallic nanoparticles (BNPs) have gained significant attention in the field of biomedical and pharmaceutical because of its tunable size, shape, high surface to volume and enhanced biological properties. In this study, we report the ecofriendly route to produce the noble (Ag-Au) bimetallic nanoparticles using aqueous flower extract of Clitoria ternatea as a reducing and capping agent. The synthesized C.T-Ag-Au BNPs were characterized by using physicochemical techniques such as UV-visible, FTIR, XRD and SEM-EDX analysis. The UV-visible spectra reveal the formation of homogeneous bimetallic nanoparticles by the single blue-shifted peak at 541 nm of C.T-Ag-Au BNPs. The phyto fabrication of synthesized C.T-Ag-Au BNPs was analyzed using FTIR spectroscopy. XRD confirms the formation of phase pure cubic Ag-Au alloy bimetallic nanoparticles with crystallite size is 14.5 nm. The surface morphology and elemental analysis of C.T-Ag-Au BNPs were examined by using SEM-EDX analysis. The synthesized C.TAg- Au BNPs were evaluated for their cytotoxicity against A549 human lung cancer cells through standard MTT assay. From this assay, green synthesized bimetallic nanoparticles induced cell apoptosis, suggesting that the synthesized C.T-Ag-Au BNPs gave best anticancer properties against lung cancer A549 cell lines.
{"title":"IN VITRO ANTICANCER POTENTIAL OF PHYTOGENIC AG-AU BIMETALLIC NANOPARTICLES USING CLITORIA TERNATEA FLOWER EXTRACT","authors":"A. Naveena, J. Jeyasundari, P.V Priya, A. Athithan","doi":"10.25004/ijpsdr.2023.150406","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150406","url":null,"abstract":"Bimetallic nanoparticles (BNPs) have gained significant attention in the field of biomedical and pharmaceutical because of its tunable size, shape, high surface to volume and enhanced biological properties. In this study, we report the ecofriendly route to produce the noble (Ag-Au) bimetallic nanoparticles using aqueous flower extract of Clitoria ternatea as a reducing and capping agent. The synthesized C.T-Ag-Au BNPs were characterized by using physicochemical techniques such as UV-visible, FTIR, XRD and SEM-EDX analysis. The UV-visible spectra reveal the formation of homogeneous bimetallic nanoparticles by the single blue-shifted peak at 541 nm of C.T-Ag-Au BNPs. The phyto fabrication of synthesized C.T-Ag-Au BNPs was analyzed using FTIR spectroscopy. XRD confirms the formation of phase pure cubic Ag-Au alloy bimetallic nanoparticles with crystallite size is 14.5 nm. The surface morphology and elemental analysis of C.T-Ag-Au BNPs were examined by using SEM-EDX analysis. The synthesized C.TAg- Au BNPs were evaluated for their cytotoxicity against A549 human lung cancer cells through standard MTT assay. From this assay, green synthesized bimetallic nanoparticles induced cell apoptosis, suggesting that the synthesized C.T-Ag-Au BNPs gave best anticancer properties against lung cancer A549 cell lines.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139348975","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 : 2023-08-25DOI: 10.25004/ijpsdr.2023.150402
Kishorkumar Sorathi̇a, A. Lumbhani, Santosh Chauhan, Mehul Patel, Tejal Soni̇, B. Suhagia
Fluvastatin sodium is a hypolipidemic agent that reduces cholesterol synthesis by inhibiting HMG-COA reductase. The drug has a comparatively short biological half-life (1.2 hours) and low bioavailability (24– 29%), making it an appropriate candidate for a sustained-release drug delivery system. This study aimed to formulate biodegradable microspheres of fluvastatin sodium by optimization through an experimental design approach. Microspheres containing fluvastatin sodium were prepared by o/w emulsification solvent evaporation method using poly (lactic-co-glycolic acid) (PLGA 50:50) as a biodegradable polymer. 32 full factorial design was applied to study the effect of drug to polymer ratio and stirring speed on dependent variables, i.e. particle size, entrapment efficiency, Q1h, t80%. Prepared formulations were subjected to evaluate physicochemical properties and release characteristics. DSC and FTIR proved no interaction between the drug and excipients. Microspheres possessed size in the range of 193 to 344 μm and entrapment efficiency varied from 63.1 to 85.6%. Formulations showed drug release up to 23% within 1-hour. while t80% was found in between 3–9 hours. Regression analysis and ANOVA results suggested a significant effect (p<0.05) of variables on responses. The results of the present study suggested that biodegradable microspheres of fluvastatin sodium prepared using poly (lactic-co-glycolic acid) can be a promising alternative for conventional delivery and suitable for sustained drug release.
{"title":"Development and Optimization of Fluvastatin Sodium Loaded Biodegradable Microspheres","authors":"Kishorkumar Sorathi̇a, A. Lumbhani, Santosh Chauhan, Mehul Patel, Tejal Soni̇, B. Suhagia","doi":"10.25004/ijpsdr.2023.150402","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150402","url":null,"abstract":"Fluvastatin sodium is a hypolipidemic agent that reduces cholesterol synthesis by inhibiting HMG-COA reductase. The drug has a comparatively short biological half-life (1.2 hours) and low bioavailability (24– 29%), making it an appropriate candidate for a sustained-release drug delivery system. This study aimed to formulate biodegradable microspheres of fluvastatin sodium by optimization through an experimental design approach. Microspheres containing fluvastatin sodium were prepared by o/w emulsification solvent evaporation method using poly (lactic-co-glycolic acid) (PLGA 50:50) as a biodegradable polymer. 32 full factorial design was applied to study the effect of drug to polymer ratio and stirring speed on dependent variables, i.e. particle size, entrapment efficiency, Q1h, t80%. Prepared formulations were subjected to evaluate physicochemical properties and release characteristics. DSC and FTIR proved no interaction between the drug and excipients. Microspheres possessed size in the range of 193 to 344 μm and entrapment efficiency varied from 63.1 to 85.6%. Formulations showed drug release up to 23% within 1-hour. while t80% was found in between 3–9 hours. Regression analysis and ANOVA results suggested a significant effect (p<0.05) of variables on responses. The results of the present study suggested that biodegradable microspheres of fluvastatin sodium prepared using poly (lactic-co-glycolic acid) can be a promising alternative for conventional delivery and suitable for sustained drug release.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139349009","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 : 2023-08-25DOI: 10.25004/ijpsdr.2023.150407
P. C. Pradhan, M. Kori
The present study aimed to screen different extracts of Diospyros malabarica leaves for antiinflammatory and wound-healing effect in mice. Phytochemical screening of different extracts i.e. petroleum ether, chloroform, ethyl acetate, ethanol and aqueous extracts, were performed using different chemical test. All extracts were subjected to study antiinflammatory effects using xylene-induced edema and wound healing activity using an incision wound model. Antiinflammatory potential was recorded by observing the mice’s percent inhibition of edema, nitric oxide (NO) estimation, and myeloperoxidase (MPO) action. The wound healing effect was observed by measurement of tensile strength, protein level and hydroxyproline level in the wound tissues. Observation of phytochemical study was confirmed that ethanolic extract of D. malabarica leaves contains glycosides and flavonoids as major chemical constituents. Antiinflammatory effect was confirmed by significant (p<0.05) percent inhibition of ear edema, significant reduction of NO level and MPO level of mice by ethanol extract of D. malabarica leaves. Wound healing potential was observed by the significant increase in tensile strength of wound tissue after treatment with ethanolic extract. A significant (p<0.05) increase in protein and hydroxyproline level of tissue were observed after treatment with ethanolic extract of D. malabarica. In conclusion, the potent antiinflammatory and wound healing effects of ethanolic extract of D. malabarica may be observed due to the presence of glycoside and flavonoid components.
{"title":"PRELIMINARY INVESTIGATIONS ON DIOSPYROS MALABARICA LEAVES EXTRACTS FOR ANTI-INFLAMMATORY AND WOUND HEALING ACTIVITY","authors":"P. C. Pradhan, M. Kori","doi":"10.25004/ijpsdr.2023.150407","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150407","url":null,"abstract":"The present study aimed to screen different extracts of Diospyros malabarica leaves for antiinflammatory and wound-healing effect in mice. Phytochemical screening of different extracts i.e. petroleum ether, chloroform, ethyl acetate, ethanol and aqueous extracts, were performed using different chemical test. All extracts were subjected to study antiinflammatory effects using xylene-induced edema and wound healing activity using an incision wound model. Antiinflammatory potential was recorded by observing the mice’s percent inhibition of edema, nitric oxide (NO) estimation, and myeloperoxidase (MPO) action. The wound healing effect was observed by measurement of tensile strength, protein level and hydroxyproline level in the wound tissues. Observation of phytochemical study was confirmed that ethanolic extract of D. malabarica leaves contains glycosides and flavonoids as major chemical constituents. Antiinflammatory effect was confirmed by significant (p<0.05) percent inhibition of ear edema, significant reduction of NO level and MPO level of mice by ethanol extract of D. malabarica leaves. Wound healing potential was observed by the significant increase in tensile strength of wound tissue after treatment with ethanolic extract. A significant (p<0.05) increase in protein and hydroxyproline level of tissue were observed after treatment with ethanolic extract of D. malabarica. In conclusion, the potent antiinflammatory and wound healing effects of ethanolic extract of D. malabarica may be observed due to the presence of glycoside and flavonoid components.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139349179","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 : 2023-08-25DOI: 10.25004/ijpsdr.2023.150405
Deepak Maheshwari, Chetan M. Detroja
Paliperidone is the 9-hydroxy metabolite (9-hydroxy) of risperidone and is a psychotropic drug of the atypical antipsychotic family. Paliperidone has the racemates (+)- and (-)-paliperidone. It is a dopamine D2 antagonist with serotonergic 5-HT2A antagonistic action that acts centrally. ALZA OROS® osmotic medication release technology is used to create Invega ER tablets. It is a tri-layer longitudinally compressed tablet based on a sophisticated osmotic delivery method that is meant to administer the paliperidone in a defined way over 24 hours. This research aims to create a generic controlled-release single-layer matrix tablet of paliperidone. Different combinations of Polyox and hypromellose in the core were used, followed by coating, to assist/build a stable and strong formulation. All strengths have similar in-vitro dissolution profiles. Freeze formulation was assessed for nitrosamine risk assessment as well as challenge for alcohol dose dumping study. Paliperidone is a basic compound with a pKa1 of 8.2 (piperidine moiety) and a pKa2 of 2.6 (pyrimidine moiety). As a result, a substantial portion of the molecule is ionized at physiological pH. It is relatively insoluble in water (0.003 g/100 mL water at pH 7.4). The solubility decreases at higher pH (0.001 g/100 mL at pH 12.9) and significantly increases at lower pH (3 g/100 mL at pH 5.3). The partition coefficient octanol/water (log P) is 2.39. Hence, discriminating media was identified as pH 2.75 buffer. The Higuchi model was used for expressing the in-vitro release profile through matrix composition. Formulation withstands 0–40% alcoholic conditions under in-vitro release tests. It is easy to formulate, stable and cost-effective. The manufacturing process involves dry blending followed by compression and coating so there will be the least chemical interaction of an active substance with other excipients. Hence, there is a negligible possibility to generate nitrosamine impurity in the formulation. The formulation is classified as rugged against dose dumping.
{"title":"Controlled Release Matrix Formulation of Paliperidone in Concurrence with Regulatory Requirements","authors":"Deepak Maheshwari, Chetan M. Detroja","doi":"10.25004/ijpsdr.2023.150405","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150405","url":null,"abstract":"Paliperidone is the 9-hydroxy metabolite (9-hydroxy) of risperidone and is a psychotropic drug of the atypical antipsychotic family. Paliperidone has the racemates (+)- and (-)-paliperidone. It is a dopamine D2 antagonist with serotonergic 5-HT2A antagonistic action that acts centrally. ALZA OROS® osmotic medication release technology is used to create Invega ER tablets. It is a tri-layer longitudinally compressed tablet based on a sophisticated osmotic delivery method that is meant to administer the paliperidone in a defined way over 24 hours. This research aims to create a generic controlled-release single-layer matrix tablet of paliperidone. Different combinations of Polyox and hypromellose in the core were used, followed by coating, to assist/build a stable and strong formulation. All strengths have similar in-vitro dissolution profiles. Freeze formulation was assessed for nitrosamine risk assessment as well as challenge for alcohol dose dumping study. Paliperidone is a basic compound with a pKa1 of 8.2 (piperidine moiety) and a pKa2 of 2.6 (pyrimidine moiety). As a result, a substantial portion of the molecule is ionized at physiological pH. It is relatively insoluble in water (0.003 g/100 mL water at pH 7.4). The solubility decreases at higher pH (0.001 g/100 mL at pH 12.9) and significantly increases at lower pH (3 g/100 mL at pH 5.3). The partition coefficient octanol/water (log P) is 2.39. Hence, discriminating media was identified as pH 2.75 buffer. The Higuchi model was used for expressing the in-vitro release profile through matrix composition. Formulation withstands 0–40% alcoholic conditions under in-vitro release tests. It is easy to formulate, stable and cost-effective. The manufacturing process involves dry blending followed by compression and coating so there will be the least chemical interaction of an active substance with other excipients. Hence, there is a negligible possibility to generate nitrosamine impurity in the formulation. The formulation is classified as rugged against dose dumping.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139349182","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}
This study analyses the association between epidemiological factors and preeclampsia and the antihypertensive drug pattern used at different stages of preeclampsia. Total 252 patients were enrolled for study. Some of the study variables were maternal age, history of infertility, family income, education, antihypertensive drug use, body mass index of the mother and baby’s birth weight. The study was performed SGT Hospital, Gurugram and was given ethical clearance by the Institutional Ethical Committee (IEC). Data was collected with the help of validated questionnaires. The occurrence of pregnancy induced hypertension (PIH) in our study was found to be 47.2%. Maternal age, low socioeconomic status, less education level, >36 weeks of gestation are one of some major factors responsible for PIH. The current study implies that different dosage forms of labetalol was prescribed with p-value <0.05.
{"title":"STUDY OF EPIDEMIOLOGY AND ITS PROGNOSTIC FACTORS FOR EXPECTED THERAPEUTIC MANAGEMENT OUTCOME ALONG WITH THE ANTIHYPERTENSIVE DRUG PATTERN FOR PREECLAMPSIA IN RURAL SETTING","authors":"Shreya Singh, Vikas Jogpal, Rashmi Ray, Abhishek Sharma","doi":"10.25004/ijpsdr.2023.150409","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150409","url":null,"abstract":"This study analyses the association between epidemiological factors and preeclampsia and the antihypertensive drug pattern used at different stages of preeclampsia. Total 252 patients were enrolled for study. Some of the study variables were maternal age, history of infertility, family income, education, antihypertensive drug use, body mass index of the mother and baby’s birth weight. The study was performed SGT Hospital, Gurugram and was given ethical clearance by the Institutional Ethical Committee (IEC). Data was collected with the help of validated questionnaires. The occurrence of pregnancy induced hypertension (PIH) in our study was found to be 47.2%. Maternal age, low socioeconomic status, less education level, >36 weeks of gestation are one of some major factors responsible for PIH. The current study implies that different dosage forms of labetalol was prescribed with p-value <0.05.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139349215","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 : 2023-08-25DOI: 10.25004/ijpsdr.2023.150403
Reena Jassal, Preeti Khetarpal, Suresh Kumar
Migration and invasion of breast cancer cells to distant parts of the body is a hallmark of the disease. The disease becomes difficult to manage and treat with an increased invasion by cancer cells. Some drugs kill the cancer cells but causes general cytotoxicity but no drugs are known to inhibit the invasive potential of cancer cells. Previously, the natural components have been proven to exhibit anticancer and invasive potential. Clematis erecta L. (Ranunculaceae) Leaves infusion is traditionally used to treat syphilitic, cancerous and other foul ulcers. Moreover, methanolic extract and and ethyl acetate fraction exhibited significant analgesic and anti-inflammatory activity. The scientific literature still lacks support for the anticancer potential of C. erecta. Therefore, it was envisaged to investigate the anticancer activities of C. erecta aerial parts on breast cancer cells. The results obtained suggest that C. erecta has anti-invasive potential on triple-negative human breast cancer cells (MDA-MB-231). Three different extracts (chloroform, methanol and water) of aerial parts of C. erecta were evaluated for their effect on the growth and migration of human breast cancer cells MDA-MB-231. Interestingly, aqueous extract inhibits cell growth by more than 50% and also inhibits migration and invasion by 40 and 50%, respectively. DNA fragmentation of extract treated cells further suggested that C. erecta has the potential to kill cancer cells.
乳腺癌细胞向身体远处迁移和入侵是这种疾病的特征。随着癌细胞入侵的增加，这种疾病变得难以控制和治疗。有些药物能杀死癌细胞，但会引起一般细胞毒性，但目前还没有药物能抑制癌细胞的侵袭潜力。此前，天然成分已被证明具有抗癌和侵袭潜力。铁线莲（Ranunculaceae）叶浸液传统上用于治疗梅毒、癌症和其他恶性溃疡。此外，甲醇提取物和乙酸乙酯馏分具有显著的镇痛和抗炎活性。科学文献仍然缺乏对直立花抗癌潜力的支持。因此，我们设想研究直立花茎叶对乳腺癌细胞的抗癌活性。研究结果表明，直立草对三阴性人类乳腺癌细胞（MDA-MB-231）具有抗侵袭潜力。研究人员评估了直立草叶气生部分的三种不同提取物（氯仿、甲醇和水）对人类乳腺癌细胞 MDA-MB-231 的生长和迁移的影响。有趣的是，水提取物对细胞生长的抑制率超过 50%，对迁移和侵袭的抑制率分别为 40% 和 50%。提取物处理过的细胞的 DNA 断裂进一步表明直立花具有杀死癌细胞的潜力。
{"title":"Clematis erecta Extract Inhibits Migration, Invasion and Induce Apoptosis in Breast Cancer Cells","authors":"Reena Jassal, Preeti Khetarpal, Suresh Kumar","doi":"10.25004/ijpsdr.2023.150403","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150403","url":null,"abstract":"Migration and invasion of breast cancer cells to distant parts of the body is a hallmark of the disease. The disease becomes difficult to manage and treat with an increased invasion by cancer cells. Some drugs kill the cancer cells but causes general cytotoxicity but no drugs are known to inhibit the invasive potential of cancer cells. Previously, the natural components have been proven to exhibit anticancer and invasive potential. Clematis erecta L. (Ranunculaceae) Leaves infusion is traditionally used to treat syphilitic, cancerous and other foul ulcers. Moreover, methanolic extract and and ethyl acetate fraction exhibited significant analgesic and anti-inflammatory activity. The scientific literature still lacks support for the anticancer potential of C. erecta. Therefore, it was envisaged to investigate the anticancer activities of C. erecta aerial parts on breast cancer cells. The results obtained suggest that C. erecta has anti-invasive potential on triple-negative human breast cancer cells (MDA-MB-231). Three different extracts (chloroform, methanol and water) of aerial parts of C. erecta were evaluated for their effect on the growth and migration of human breast cancer cells MDA-MB-231. Interestingly, aqueous extract inhibits cell growth by more than 50% and also inhibits migration and invasion by 40 and 50%, respectively. DNA fragmentation of extract treated cells further suggested that C. erecta has the potential to kill cancer cells.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139349109","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 : 2023-08-25DOI: 10.25004/ijpsdr.2023.150412
Nidhi Shah, Khushbu Patel, Indrajeet Singhvi
The objective of the present research work was to develop a microemulsion for the transdermal delivery of eberconazole nitrate (EBZ). Initially, oil, surfactant and co-surfactant were selected based on their solubility and emulsification study. A pseudoternary phase diagram was constructed to optimize the surfactant-co surfactant (Smix) ratio. Eberconazole nitrate (EBZ) loaded microemulsion was optimized using central composite design (CCD) with amount of Capmul MCM (X1), tween 80 (X2) and transcutol (X3) as independent variables along with the cumulative amount of drug release (Q24) (Y1), flux (Jss) (Y2) and lag time (tL) (Y3) as dependent variables. Drug release study of all the design batches showed successfully increased permeation of drug which might be due to the compositional characteristics of ME. The globule size of the optimized batch of EBZ loaded ME (153.6 nm) confirms the micrometer size of the formulation. Zeta potential and polydispersity index (PDI) of the optimized batch was found to be -30.5 mV and 0.253, respectively, proving stability and uniform distribution of dispersed systems. The optimized batch of MEs has a pH value of 6.96 ± 0.21, indicating no chance of skin irritation. Further morphological and structural examination of the optimized batch of EBZ loaded ME was done by transmission electron microscope (TEM) and images illustrated the spherical micelles with size range of 100 to 200 nm which evidently may support the high absorption and results into the enhancement of drug permeation which may increase the therapeutic effect, decrease the dose frequency and improving the patience compliance for topical drug delivery.
本研究工作的目的是开发一种用于硝酸依康唑（EBZ）透皮给药的微乳剂。最初，根据油、表面活性剂和辅助表面活性剂的溶解性和乳化研究，对它们进行了选择。为了优化表面活性剂与辅助表面活性剂（Smix）的比例，构建了一个假三元相图。以 Capmul MCM（X1）、吐温 80（X2）和 transcutol（X3）的用量为自变量，以药物释放累积量（Q24）（Y1）、通量（Jss）（Y2）和滞后时间（tL）（Y3）为因变量，采用中心复合设计（CCD）对负载硝酸依康唑（EBZ）的微乳剂进行了优化。所有设计批次的药物释放研究均显示药物渗透性成功增加，这可能与 ME 的成分特性有关。优化批次的 EBZ 负载 ME 的球形尺寸（153.6 nm）证实了制剂的微米尺寸。优化批次的 Zeta 电位和多分散指数（PDI）分别为 -30.5 mV 和 0.253，证明了分散体系的稳定性和均匀分布。优化批次 ME 的 pH 值为 6.96 ± 0.21，表明不会对皮肤产生刺激。透射电子显微镜（TEM）对优化批次的 EBZ 负载 ME 进行了进一步的形态和结构检查，图像显示其为球形胶束，尺寸范围为 100 至 200 nm。
{"title":"Topical Delivery of Eberconazole Nitrate Loaded Microemulsion: Formulation, Design and Evaluation","authors":"Nidhi Shah, Khushbu Patel, Indrajeet Singhvi","doi":"10.25004/ijpsdr.2023.150412","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150412","url":null,"abstract":"The objective of the present research work was to develop a microemulsion for the transdermal delivery of eberconazole nitrate (EBZ). Initially, oil, surfactant and co-surfactant were selected based on their solubility and emulsification study. A pseudoternary phase diagram was constructed to optimize the surfactant-co surfactant (Smix) ratio. Eberconazole nitrate (EBZ) loaded microemulsion was optimized using central composite design (CCD) with amount of Capmul MCM (X1), tween 80 (X2) and transcutol (X3) as independent variables along with the cumulative amount of drug release (Q24) (Y1), flux (Jss) (Y2) and lag time (tL) (Y3) as dependent variables. Drug release study of all the design batches showed successfully increased permeation of drug which might be due to the compositional characteristics of ME. The globule size of the optimized batch of EBZ loaded ME (153.6 nm) confirms the micrometer size of the formulation. Zeta potential and polydispersity index (PDI) of the optimized batch was found to be -30.5 mV and 0.253, respectively, proving stability and uniform distribution of dispersed systems. The optimized batch of MEs has a pH value of 6.96 ± 0.21, indicating no chance of skin irritation. Further morphological and structural examination of the optimized batch of EBZ loaded ME was done by transmission electron microscope (TEM) and images illustrated the spherical micelles with size range of 100 to 200 nm which evidently may support the high absorption and results into the enhancement of drug permeation which may increase the therapeutic effect, decrease the dose frequency and improving the patience compliance for topical drug delivery.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139348987","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 : 2023-08-25DOI: 10.25004/ijpsdr.2023.150418
Devashish Mehta, Jpan G. Brahmbhatt, Kinjal Bhadresha, Rakesh Rawal
Breast cancer mortality rate is fifth among all cancer and increasing day by day due to modern lifestyles. Its molecular subtype is classified as per their significant receptor expression, such as estrogen receptor (ER), progesterone receptor (PR) & human epidermal growth receptor 2 (Her2). Triple-negative breast cancer (TNBC) is an aggressive subgroup among breast cancer subtypes and clinically challenging to treat due to loss of all three receptor (ER/PR/Her2) expression. Treatment modalities of TNBC include surgery, chemotherapy, radiotherapy and immunotherapy. Postoperative radiation therapy (RT) improves locoregional control and overall survival in TNBC patients. The powerful ionizing radiation (IR) response to RT is contributed by the inherent radiosensitivity of the tumor, which is influenced by genes associated with the cell cycle, DNA damage repair, apoptosis, etc. This review article narrates the role of biomarkers obtained through data mining and manual curation of published literature to predict radioresistance in patients receiving radiotherapy. Further, the role of natural radiosensitizers in overcoming radioresistance for effectively managing TNBC is also discussed.
{"title":"A Review on Biomarkers for Predicting Radioresistance and Role of Natural Radiosensitizers in Triple-Negative Breast Cancer","authors":"Devashish Mehta, Jpan G. Brahmbhatt, Kinjal Bhadresha, Rakesh Rawal","doi":"10.25004/ijpsdr.2023.150418","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150418","url":null,"abstract":"Breast cancer mortality rate is fifth among all cancer and increasing day by day due to modern lifestyles. Its molecular subtype is classified as per their significant receptor expression, such as estrogen receptor (ER), progesterone receptor (PR) & human epidermal growth receptor 2 (Her2). Triple-negative breast cancer (TNBC) is an aggressive subgroup among breast cancer subtypes and clinically challenging to treat due to loss of all three receptor (ER/PR/Her2) expression. Treatment modalities of TNBC include surgery, chemotherapy, radiotherapy and immunotherapy. Postoperative radiation therapy (RT) improves locoregional control and overall survival in TNBC patients. The powerful ionizing radiation (IR) response to RT is contributed by the inherent radiosensitivity of the tumor, which is influenced by genes associated with the cell cycle, DNA damage repair, apoptosis, etc. This review article narrates the role of biomarkers obtained through data mining and manual curation of published literature to predict radioresistance in patients receiving radiotherapy. Further, the role of natural radiosensitizers in overcoming radioresistance for effectively managing TNBC is also discussed.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139348990","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 : 2023-08-25DOI: 10.25004/ijpsdr.2023.150408
Charuvil K Biju, Radha K Lekshmi, Sivanandan Sreekumar
Dengue (breakbone fever) is a rapidly spreading arboviral infection transmitted by Aedes mosquitoes with major public health implications in more than 100 tropical and subtropical countries mostly in Southeast Asia, South and Central America and the Western Pacific. As the virus spreads to new geographic areas, more frequent dengue outbreaks occur in different parts of the world. Fifty million cases of dengue occur worldwide each year, of which 10% require hospitalization for dengue hemorrhagic fever (DHF). It is a shocking truth that more than 90% of these are children under the age of five. The mortality rate is also significant as 2.5% die from dengue. Currently, there is no effective vaccine or specific drug for Dengue/DHF. Pharmaceutical manufacturers have turned their attention to plant-based drug candidates to produce effective drugs. Following the study investigated the active phytochemicals in the medicinal plant Caesalpinia bonduc (L.) Roxb. through docking simulation. Dengue virus non-structural protein five (NS5) and human IMPDH-II were used here as targets for docking with plant compounds. Docking results revealed that 33 compounds out of 82 phytochemicals showed better binding affinity than the native ligands of the targets. Compounds exhibiting the lowest free energy levels were further screened after studying their pharmacokinetics, medicinal chemistry friendliness, lead-likeness, and toxicity prediction to identify lead molecules. At the end of the study, three compounds, Caesaldekarin A, Caesalpinin F and Taepeenin D, which potently inhibited both targets, were selected here for further ‘in-vitro’ and ‘in-vivo’ studies.
{"title":"ANTI-DENGUE LEADS FROM CAESALPINIA BONDUC - AN IN SILICO APPROACH","authors":"Charuvil K Biju, Radha K Lekshmi, Sivanandan Sreekumar","doi":"10.25004/ijpsdr.2023.150408","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150408","url":null,"abstract":"Dengue (breakbone fever) is a rapidly spreading arboviral infection transmitted by Aedes mosquitoes with major public health implications in more than 100 tropical and subtropical countries mostly in Southeast Asia, South and Central America and the Western Pacific. As the virus spreads to new geographic areas, more frequent dengue outbreaks occur in different parts of the world. Fifty million cases of dengue occur worldwide each year, of which 10% require hospitalization for dengue hemorrhagic fever (DHF). It is a shocking truth that more than 90% of these are children under the age of five. The mortality rate is also significant as 2.5% die from dengue. Currently, there is no effective vaccine or specific drug for Dengue/DHF. Pharmaceutical manufacturers have turned their attention to plant-based drug candidates to produce effective drugs. Following the study investigated the active phytochemicals in the medicinal plant Caesalpinia bonduc (L.) Roxb. through docking simulation. Dengue virus non-structural protein five (NS5) and human IMPDH-II were used here as targets for docking with plant compounds. Docking results revealed that 33 compounds out of 82 phytochemicals showed better binding affinity than the native ligands of the targets. Compounds exhibiting the lowest free energy levels were further screened after studying their pharmacokinetics, medicinal chemistry friendliness, lead-likeness, and toxicity prediction to identify lead molecules. At the end of the study, three compounds, Caesaldekarin A, Caesalpinin F and Taepeenin D, which potently inhibited both targets, were selected here for further ‘in-vitro’ and ‘in-vivo’ studies.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139349053","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}
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