Pub Date : 2023-01-02DOI: 10.1080/22297928.2022.2162830
Devangkumar Tandel, K. Patel, V. Thakkar, A. Sakure, T. Gandhi
Abstract UHPLC-MS/MS was utilised to quantitatively analyse Rifampicin and Quercetin-loaded Liquisolid compact in rat plasma. The UPLC Acquity C18 (1.7 μm, 2.1 × 15 mm) column and 0.5 ml/min were used to separate the analyte. In a low-pressure gradient mode, A: In water 0.1 % formic acid and B: In acetonitrile 0.1 % formic acid as the mobile phase. Sample pre-treatment was performed by protein precipitation technique with methanol and acetonitrile (1:1) from rat plasma. As an internal standard (IS), the analyte was found by tracking precursor-to-product ion transformations of 823 → 791.3 m/z for rifampicin, 303 → 257 m/z for quercetin, and 138 → 121 m/z for isoniazid in MRM mode. The proposed technique was validated for precisions (Intraday and Interday) accuracy, linearity, quantification at lower limits, and analyte recovery. The findings showed that the plasma samples inter and intra-day precision and consistency values were determined to be within the acceptable range. After orally administering Liquid solid compact and pure drug solution, which showed a substantial difference in the pace and extent of absorption, the method’s suitability for determining the pharmacokinetic profile of each drug was tested. GRAPHICAL ABSTRACT
{"title":"Bioanalytical Method Development and Validation for Determination of Rifampicin and Quercetin in Rat Plasma by UHPLC-MS/MS: Applications to Pharmacokinetic Study","authors":"Devangkumar Tandel, K. Patel, V. Thakkar, A. Sakure, T. Gandhi","doi":"10.1080/22297928.2022.2162830","DOIUrl":"https://doi.org/10.1080/22297928.2022.2162830","url":null,"abstract":"Abstract UHPLC-MS/MS was utilised to quantitatively analyse Rifampicin and Quercetin-loaded Liquisolid compact in rat plasma. The UPLC Acquity C18 (1.7 μm, 2.1 × 15 mm) column and 0.5 ml/min were used to separate the analyte. In a low-pressure gradient mode, A: In water 0.1 % formic acid and B: In acetonitrile 0.1 % formic acid as the mobile phase. Sample pre-treatment was performed by protein precipitation technique with methanol and acetonitrile (1:1) from rat plasma. As an internal standard (IS), the analyte was found by tracking precursor-to-product ion transformations of 823 → 791.3 m/z for rifampicin, 303 → 257 m/z for quercetin, and 138 → 121 m/z for isoniazid in MRM mode. The proposed technique was validated for precisions (Intraday and Interday) accuracy, linearity, quantification at lower limits, and analyte recovery. The findings showed that the plasma samples inter and intra-day precision and consistency values were determined to be within the acceptable range. After orally administering Liquid solid compact and pure drug solution, which showed a substantial difference in the pace and extent of absorption, the method’s suitability for determining the pharmacokinetic profile of each drug was tested. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"21 1","pages":"60 - 72"},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82543216","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 : 2023-01-02DOI: 10.1080/22297928.2023.2195862
Dhavalsinh P. Solanki, Krunal H. Solanki, Jaineel Desai, D. Shah, U. Chhalotiya
Abstract A combination of Azilsartan Medoxomil and Cilnidipine is prescribed in the treatment of Hypertension. The present work represents an accurate and precise high-performance thin layer chromatographic method for the estimation of Azilsartan Medoxomil (AZL) and Cilnidipine (CLN) in combined tablet dosage form. Pre-coated silica gel- G60 F254 aluminum sheet (100 × 100 mm, 0.2 mm layer thickness) were used as stationary phase and Ethyl Acetate: Toluene: Glacial Acetic Acid (5: 4.9: 0.1 %v/v/v) in the mixture was used as mobile phase. The method was linear in the concentration range of 200 - 2000 ng/band for AZL and 50 -500 ng/band for CLN with a correlation coefficient (r2) of 0.996 for AZL and 0.999 for CLN. The proposed method was validated with respect to linearity, accuracy, precision, and robustness as per ICH Q2 (R1) guideline. A forced degradation study was performed to assess the stability indicating the nature of the method. All the degradant peaks were well resolved from the peak of the drug without any interference. The method was successfully applied for the analysis of AZL and CLN in combined tablet formulation. GRAPHICAL ABSTRACT
{"title":"HPTLC-Densitometric Estimation of Anti-hypertensive Drug Combination Azilsartan Medoxomil and Cilnidipine in Combined Dosage Form","authors":"Dhavalsinh P. Solanki, Krunal H. Solanki, Jaineel Desai, D. Shah, U. Chhalotiya","doi":"10.1080/22297928.2023.2195862","DOIUrl":"https://doi.org/10.1080/22297928.2023.2195862","url":null,"abstract":"Abstract A combination of Azilsartan Medoxomil and Cilnidipine is prescribed in the treatment of Hypertension. The present work represents an accurate and precise high-performance thin layer chromatographic method for the estimation of Azilsartan Medoxomil (AZL) and Cilnidipine (CLN) in combined tablet dosage form. Pre-coated silica gel- G60 F254 aluminum sheet (100 × 100 mm, 0.2 mm layer thickness) were used as stationary phase and Ethyl Acetate: Toluene: Glacial Acetic Acid (5: 4.9: 0.1 %v/v/v) in the mixture was used as mobile phase. The method was linear in the concentration range of 200 - 2000 ng/band for AZL and 50 -500 ng/band for CLN with a correlation coefficient (r2) of 0.996 for AZL and 0.999 for CLN. The proposed method was validated with respect to linearity, accuracy, precision, and robustness as per ICH Q2 (R1) guideline. A forced degradation study was performed to assess the stability indicating the nature of the method. All the degradant peaks were well resolved from the peak of the drug without any interference. The method was successfully applied for the analysis of AZL and CLN in combined tablet formulation. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"8 1","pages":"82 - 94"},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81500138","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 : 2022-11-02DOI: 10.1080/22297928.2022.2155071
C. Vijaykumar, Y. Kumar, P. Aparna, V. Marisetti
Abstract A single reversed-phase HPLC method was developed for the quantification of seven impurities of Apremilast and its enantiomer in the drug substance. An immobilized chiral stationary phase with a chiral selector “tris (3,5-dimethyl phenyl carbamate) derivative of amylose-Chiralpak IA-3 (250 mm × 4.6 mm, 3 μm) was employed to achieve the desired separation. A mobile phase consists of buffer (0.01M NH4HCO3, PH 8.0) and acetonitrile in the ratio 50:50 (v/v) and is pumped at a flow rate of 0.4 mL/min with an isocratic elution mode. The column oven temperature is set at 25°C, and the chromatographic output is monitored at 225 nm with a total run time of 45 min. A test concentration of 500 µg/mL of Apremilast in the mobile phase is used with an injection volume of 10 µL. Induced degradation studies were carried out to study the intrinsic chemical behavior of the drug. The degradation sample solutions were utilized to demonstrate the stability-indicating nature of the developed analytical method. The obtained mass number [M+H]+ for the primary degradation product formed in acid hydrolysis was identified as 418.36 and in base hydrolysis 478.12. The two impurities were identified as impurity-5(Deacetylated impurity), and impurity-2(open ring acid impurity), respectively, and the degradation pathways were established. Following ICH Q2 and USP<1225>guidelines, complete method validation was carried out. The RSD for the drug and impurities in interday and intraday studies are less than 4.0%, and the recoveries for the impurities are between 96.1-102.1% and linearity r ≥ 0.9997. LOQ results for the drug and impurities are between 0.052 µg/mL and 0.107 µg/mL, and LOD results are between 0.016 µg/mL and 0.032 µg/mL. The greenness of the method was evaluated by using an analytical eco scale, GAPI, and AGREE, and it was found that the method is green. GRAPHICAL ABSTRACT
{"title":"Enantioselective Green HPLC Method for Simultaneous Determination of Enantiomer, and Potential Impurities in Apremilast Drug Substance","authors":"C. Vijaykumar, Y. Kumar, P. Aparna, V. Marisetti","doi":"10.1080/22297928.2022.2155071","DOIUrl":"https://doi.org/10.1080/22297928.2022.2155071","url":null,"abstract":"Abstract A single reversed-phase HPLC method was developed for the quantification of seven impurities of Apremilast and its enantiomer in the drug substance. An immobilized chiral stationary phase with a chiral selector “tris (3,5-dimethyl phenyl carbamate) derivative of amylose-Chiralpak IA-3 (250 mm × 4.6 mm, 3 μm) was employed to achieve the desired separation. A mobile phase consists of buffer (0.01M NH4HCO3, PH 8.0) and acetonitrile in the ratio 50:50 (v/v) and is pumped at a flow rate of 0.4 mL/min with an isocratic elution mode. The column oven temperature is set at 25°C, and the chromatographic output is monitored at 225 nm with a total run time of 45 min. A test concentration of 500 µg/mL of Apremilast in the mobile phase is used with an injection volume of 10 µL. Induced degradation studies were carried out to study the intrinsic chemical behavior of the drug. The degradation sample solutions were utilized to demonstrate the stability-indicating nature of the developed analytical method. The obtained mass number [M+H]+ for the primary degradation product formed in acid hydrolysis was identified as 418.36 and in base hydrolysis 478.12. The two impurities were identified as impurity-5(Deacetylated impurity), and impurity-2(open ring acid impurity), respectively, and the degradation pathways were established. Following ICH Q2 and USP<1225>guidelines, complete method validation was carried out. The RSD for the drug and impurities in interday and intraday studies are less than 4.0%, and the recoveries for the impurities are between 96.1-102.1% and linearity r ≥ 0.9997. LOQ results for the drug and impurities are between 0.052 µg/mL and 0.107 µg/mL, and LOD results are between 0.016 µg/mL and 0.032 µg/mL. The greenness of the method was evaluated by using an analytical eco scale, GAPI, and AGREE, and it was found that the method is green. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"30 1","pages":"691 - 714"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75316774","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}
Abstract The inclusion complex of α, β-arteether with β-cyclodextrin was prepared. The ratio was selected by implementing the QbD approach to get the best host-guest complex ratio. Further, the formation of the best complex was compared with stability analysis. Also, the enhancement in dissolution profile, as well as solubility, was compared with the pure α, β-arteether. The cyclodextrin derivative with maximum enhanced solubility and best dissolution profile was further used for PKPD modeling, permeability studies, and in-vivo and ex-vivo studies. By QbD approach as well as phase solubility studies it was confirmed that 1:1 fits best for the ART-CD inclusion complex formation. This was substantiated by a saturation solubility investigation, which found that in the presence of PVPK30, the solubility of α, β-arteether was enhanced by 77.05 times. The crystalline nature of the drug was lost or diminished greatly in the inclusion complex, showing the drug was present in a solubilized form in the formulation, according to scanning electron microscopy, X-ray diffraction, and differential scanning calorimetry. Further, the complex powder was converted into spheroids by the spheronization technique and filled in empty enteric-coated shells. In vitro release studies for spheroids-filled enteric capsules were carried out for 6 h by progressive dissolution technique. The pharmacokinetic model using Ecosim Pro 6.2.0 software confirms the enhancement of the bioavailability of the arteether. Further, the in vivo studies also confirm the enhancement in absolute bioavailability by 48.29% when compared with i.v. data of pure drugs. The complex shows an 11% maximum enhancement in antimalarial activity when compared with pure drugs. From the research, it was concluded that inclusion complexation is a suitable approach to improvise the solubility as well as bioavailability of hydrophobic drugs like α, β-arteether. GRAPHICAL ABSTRACT
摘要制备了α， β- artee醚与β-环糊精包合物。采用QbD方法选择最佳主客复合比。并对最佳配合物的形成进行了稳定性分析。与纯α， β- artether相比，其溶解谱和溶解度都有所提高。具有最大溶解度和最佳溶解谱的环糊精衍生物进一步用于PKPD建模、渗透性研究以及体内和离体研究。通过QbD方法和相溶解度研究，证实了1:1最适合ART-CD包合物的形成。饱和溶解度研究证实了这一点，发现PVPK30的存在使α， β-arteether的溶解度提高了77.05倍。根据扫描电子显微镜、x射线衍射和差示扫描量热法，药物的晶体性质在包合物中丢失或大大减少，表明药物在配方中以溶解形式存在。再通过球化技术将复合粉末转化为球状体，填充到空的肠溶壳中。采用渐进式溶出技术对球状肠溶胶囊进行6 h体外释放研究。采用Ecosim Pro 6.2.0软件建立药代动力学模型，证实了青蒿醚生物利用度的提高。此外，体内研究也证实，与纯药物的静脉注射数据相比，绝对生物利用度提高了48.29%。与纯药物相比，该复合物的抗疟活性最多可提高11%。研究结果表明，包合络合是提高疏水药物如α， β-arteether的溶解度和生物利用度的一种合适的方法。图形抽象
{"title":"Execution of Quality by Design Approach for Preparation and Optimization of Inclusion Complexes: In-vivo and ex-vivo Assessment","authors":"Neha Bajwa, P. Singh, Srishti Naryal, Trisha Sharma, Puran Singh Sijwal, Ashish Baldi","doi":"10.1080/22297928.2022.2159521","DOIUrl":"https://doi.org/10.1080/22297928.2022.2159521","url":null,"abstract":"Abstract The inclusion complex of α, β-arteether with β-cyclodextrin was prepared. The ratio was selected by implementing the QbD approach to get the best host-guest complex ratio. Further, the formation of the best complex was compared with stability analysis. Also, the enhancement in dissolution profile, as well as solubility, was compared with the pure α, β-arteether. The cyclodextrin derivative with maximum enhanced solubility and best dissolution profile was further used for PKPD modeling, permeability studies, and in-vivo and ex-vivo studies. By QbD approach as well as phase solubility studies it was confirmed that 1:1 fits best for the ART-CD inclusion complex formation. This was substantiated by a saturation solubility investigation, which found that in the presence of PVPK30, the solubility of α, β-arteether was enhanced by 77.05 times. The crystalline nature of the drug was lost or diminished greatly in the inclusion complex, showing the drug was present in a solubilized form in the formulation, according to scanning electron microscopy, X-ray diffraction, and differential scanning calorimetry. Further, the complex powder was converted into spheroids by the spheronization technique and filled in empty enteric-coated shells. In vitro release studies for spheroids-filled enteric capsules were carried out for 6 h by progressive dissolution technique. The pharmacokinetic model using Ecosim Pro 6.2.0 software confirms the enhancement of the bioavailability of the arteether. Further, the in vivo studies also confirm the enhancement in absolute bioavailability by 48.29% when compared with i.v. data of pure drugs. The complex shows an 11% maximum enhancement in antimalarial activity when compared with pure drugs. From the research, it was concluded that inclusion complexation is a suitable approach to improvise the solubility as well as bioavailability of hydrophobic drugs like α, β-arteether. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"26 1","pages":"715 - 729"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86105409","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 : 2022-11-02DOI: 10.1080/22297928.2022.2157224
K. Sarkar, R. Das
Abstract Monkeypox virus (MPXV) is considered as zoonotic disease with characteristics comparable to smallpox virus. The disease is now a global epidemic concern. Currently, tecovirimat is approved by US Food and Drug Administration (FDA) for MPXV treatment. The aim of this in silico study is to repurpose approved pharmaceutical drugs as potential inhibitors of MPXV target. In this study, molecular docking was performed on 406 pharmaceutical drugs, and results were compared with reference tecovirimat. Results showed that 7 compounds, bictegravir, glimepiride, glyburide, lasmiditan, olaparib, rimegepant, and ubrogepant, have shown higher binding energies compared to the reference. After that, these best hits were further assessed by 100 ns molecular dynamics simulation and the best results were observed for bictegravir, glimepiride, glyburide, olaparib, and ubrogepant. The docking analysis was further validated by molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) binding free energy calculations. In addition, pharmacokinetics and density functional theory (DFT) studies were also discussed for these best hits. In conclusion, three compounds, bictegravir, glimepiride, and glyburide, have satisfied all the criteria for better leads against MPXV. GRAPHICAL ABSTRACT
{"title":"Repurposing of Existing Pharmaceutical Drugs Against Monkey-pox Virus: An In Silico Study","authors":"K. Sarkar, R. Das","doi":"10.1080/22297928.2022.2157224","DOIUrl":"https://doi.org/10.1080/22297928.2022.2157224","url":null,"abstract":"Abstract Monkeypox virus (MPXV) is considered as zoonotic disease with characteristics comparable to smallpox virus. The disease is now a global epidemic concern. Currently, tecovirimat is approved by US Food and Drug Administration (FDA) for MPXV treatment. The aim of this in silico study is to repurpose approved pharmaceutical drugs as potential inhibitors of MPXV target. In this study, molecular docking was performed on 406 pharmaceutical drugs, and results were compared with reference tecovirimat. Results showed that 7 compounds, bictegravir, glimepiride, glyburide, lasmiditan, olaparib, rimegepant, and ubrogepant, have shown higher binding energies compared to the reference. After that, these best hits were further assessed by 100 ns molecular dynamics simulation and the best results were observed for bictegravir, glimepiride, glyburide, olaparib, and ubrogepant. The docking analysis was further validated by molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) binding free energy calculations. In addition, pharmacokinetics and density functional theory (DFT) studies were also discussed for these best hits. In conclusion, three compounds, bictegravir, glimepiride, and glyburide, have satisfied all the criteria for better leads against MPXV. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"81 1","pages":"655 - 670"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85137016","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 : 2022-11-02DOI: 10.1080/22297928.2022.2160273
H. Salem, Noha Abdal-Karim, Bahaa Omran, Abdel-Rahman Abdel-Gayed, Mazen Atef, Shrouq Bahaa, M. Abdelgaleel
Abstract A new, simple, green and highly sensitive method has been established for quantification of recently approved antineoplastic drug Sotorasib (SOTO) in its bulk, tablets and biological fluids. The method depends on measuring the intrinsic fluorescence of the studied drug at wavelengths 350/410 nm at the optimal conditions. Validation of this method was performed following the guidelines of ICH. The proposed method shows linearity over a range of concentration 0.1-1.0 µg mL-1 with detection and quantification limits of 0.028 and 0.89 µg mL-1 respectively. Due to its high sensitivity, the suggested method was applied for quantification of the cited drug in spiked plasma and urine. The suggested strategy was also applied to evaluate the content uniformity in commercial tablets following the USP guidelines.
{"title":"Green Chemistry Method Based on Native Fluorescence for Estimation of Recently Approved Anti-neoplastic Drug Sotorasib","authors":"H. Salem, Noha Abdal-Karim, Bahaa Omran, Abdel-Rahman Abdel-Gayed, Mazen Atef, Shrouq Bahaa, M. Abdelgaleel","doi":"10.1080/22297928.2022.2160273","DOIUrl":"https://doi.org/10.1080/22297928.2022.2160273","url":null,"abstract":"Abstract A new, simple, green and highly sensitive method has been established for quantification of recently approved antineoplastic drug Sotorasib (SOTO) in its bulk, tablets and biological fluids. The method depends on measuring the intrinsic fluorescence of the studied drug at wavelengths 350/410 nm at the optimal conditions. Validation of this method was performed following the guidelines of ICH. The proposed method shows linearity over a range of concentration 0.1-1.0 µg mL-1 with detection and quantification limits of 0.028 and 0.89 µg mL-1 respectively. Due to its high sensitivity, the suggested method was applied for quantification of the cited drug in spiked plasma and urine. The suggested strategy was also applied to evaluate the content uniformity in commercial tablets following the USP guidelines.","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"13 1","pages":"761 - 769"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80455305","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 : 2022-11-02DOI: 10.1080/22297928.2022.2157223
Rony Bhowal, Sony Kumari, C. Sarma, P. Suprasanna, Puja Roy
Abstract Citrus plants have a secure and important place in human health. Citrus is not only significant for its delicious fruits but also because of certain medicinal and pharmacological properties. The presence of secondary metabolites like flavonoids, limonoids, alkaloids, phenolics and coumarins has dramatically increased its efficacy in treating bacterial and fungal infections. Emergence of new and improved extraction techniques has helped researchers to isolate novel phytochemicals from citrus species, and there is a greater attention. Numerous studies throughout the world have focused to isolate novel metabolites from citrus plants. There is a rich biodiversity of citrus species in the Indian subcontinent based on climatic condition which supported the growth and maintenance of diverse varieties. Analysis of metabolomic and medicinal properties of local citrus plant will aid in understanding their importance in pharmacological industry. The present review is focused on the medicinal and secondary metabolite profile of citrus plants from India.
{"title":"Phytochemical Constituents and Bioactivity Profiles of Citrus Genus from India","authors":"Rony Bhowal, Sony Kumari, C. Sarma, P. Suprasanna, Puja Roy","doi":"10.1080/22297928.2022.2157223","DOIUrl":"https://doi.org/10.1080/22297928.2022.2157223","url":null,"abstract":"Abstract Citrus plants have a secure and important place in human health. Citrus is not only significant for its delicious fruits but also because of certain medicinal and pharmacological properties. The presence of secondary metabolites like flavonoids, limonoids, alkaloids, phenolics and coumarins has dramatically increased its efficacy in treating bacterial and fungal infections. Emergence of new and improved extraction techniques has helped researchers to isolate novel phytochemicals from citrus species, and there is a greater attention. Numerous studies throughout the world have focused to isolate novel metabolites from citrus plants. There is a rich biodiversity of citrus species in the Indian subcontinent based on climatic condition which supported the growth and maintenance of diverse varieties. Analysis of metabolomic and medicinal properties of local citrus plant will aid in understanding their importance in pharmacological industry. The present review is focused on the medicinal and secondary metabolite profile of citrus plants from India.","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"10 1","pages":"770 - 787"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81102367","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 : 2022-11-02DOI: 10.1080/22297928.2022.2159523
Sushank Suryawanshi, R. Pawar, R. Gonnade, Sharvil Patil
Abstract Glyceryl monooleate (GMO) forms cubic mesophase upon hydration with sustained drug release characteristics. However its stickiness and stiffness often creates processing challenges for preparation of formulations. Felodipine (FLD), BCS class II molecule was used as model drug. Thus objective of the current work was to increase manufacturing feasibility of GMO using polymer and to enhance the release of felodipine by preparing LC precursors using HME. HPMC E5 polymer was selected for processing of FLD. Batch optimization was done using 23 Factorial design. The prepared batches were characterized for DSC, FTIR, hot stage microscopy (HSM), plane polarized light microscopy (PPL), PXRD and in vitro dissolution studies. The processing of FLD using HME process showed amorphization as revealed by PXRD studies. DSC and HSM studies showed solubilization of FLD in the molten mass of GMO and HPMC E5 confirming formation of solid dispersion. PPL demonstrated formation of cubic LC phase by GMO upon hydration of prepared formulations. The optimized batch of felodipine showed significant improvement in the dissolution profile of FLD with extended release profile. HME assisted liquid crystal precursors could act as promising formulations for BCS II drugs requiring extended drug release profile with improved processing feasibility of GMO. GRAPHICAL ABSTRACT
{"title":"Hot Melt Extrusion Assisted Felodipine Loaded Liquid Crystal Precursor with Enhanced Solubility and Sustained Drug Release Characteristics","authors":"Sushank Suryawanshi, R. Pawar, R. Gonnade, Sharvil Patil","doi":"10.1080/22297928.2022.2159523","DOIUrl":"https://doi.org/10.1080/22297928.2022.2159523","url":null,"abstract":"Abstract Glyceryl monooleate (GMO) forms cubic mesophase upon hydration with sustained drug release characteristics. However its stickiness and stiffness often creates processing challenges for preparation of formulations. Felodipine (FLD), BCS class II molecule was used as model drug. Thus objective of the current work was to increase manufacturing feasibility of GMO using polymer and to enhance the release of felodipine by preparing LC precursors using HME. HPMC E5 polymer was selected for processing of FLD. Batch optimization was done using 23 Factorial design. The prepared batches were characterized for DSC, FTIR, hot stage microscopy (HSM), plane polarized light microscopy (PPL), PXRD and in vitro dissolution studies. The processing of FLD using HME process showed amorphization as revealed by PXRD studies. DSC and HSM studies showed solubilization of FLD in the molten mass of GMO and HPMC E5 confirming formation of solid dispersion. PPL demonstrated formation of cubic LC phase by GMO upon hydration of prepared formulations. The optimized batch of felodipine showed significant improvement in the dissolution profile of FLD with extended release profile. HME assisted liquid crystal precursors could act as promising formulations for BCS II drugs requiring extended drug release profile with improved processing feasibility of GMO. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"86 1","pages":"745 - 760"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89866523","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 : 2022-11-02DOI: 10.1080/22297928.2022.2151375
Roopa S. Naik, J. Seetharamappa
Abstract Several biological processes in the body involve the ligand-protein association and thereby exert a wide spectrum of pharmaceutical activities. Consequently, the research community worked hard for a long time to explore the phenomenon of drug-protein binding. Insights into the molecular and physiological processes of a flavonoid, galangin (GAL) upon binding to human serum albumin (HSA) have been explored in vitro via both experimental and theoretical approaches. GAL is a natural, multifunctional and a potential anticancer drug and HSA is a plentiful protein in the circulatory system of humans. UV absorption, calorimetric, temperature-dependent ellipticity, fluorescence lifetime decay, FRET, electrochemical, zeta potential and in silico studies were used to further investigate GAL-HSA interaction. Results of these investigations suggested the interaction between GAL and HSA. The location of GAL on HSA was identified by site probe experiments and further confirmed by molecular docking and simulation studies. GRAPHICAL ABSTRACT
{"title":"Biophysical, Calorimetric, Zeta Potential, Voltammetric and Computational Insights into the Interaction of An Antimuta-genic Agent with Human Serum Albumin","authors":"Roopa S. Naik, J. Seetharamappa","doi":"10.1080/22297928.2022.2151375","DOIUrl":"https://doi.org/10.1080/22297928.2022.2151375","url":null,"abstract":"Abstract Several biological processes in the body involve the ligand-protein association and thereby exert a wide spectrum of pharmaceutical activities. Consequently, the research community worked hard for a long time to explore the phenomenon of drug-protein binding. Insights into the molecular and physiological processes of a flavonoid, galangin (GAL) upon binding to human serum albumin (HSA) have been explored in vitro via both experimental and theoretical approaches. GAL is a natural, multifunctional and a potential anticancer drug and HSA is a plentiful protein in the circulatory system of humans. UV absorption, calorimetric, temperature-dependent ellipticity, fluorescence lifetime decay, FRET, electrochemical, zeta potential and in silico studies were used to further investigate GAL-HSA interaction. Results of these investigations suggested the interaction between GAL and HSA. The location of GAL on HSA was identified by site probe experiments and further confirmed by molecular docking and simulation studies. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"6 1","pages":"671 - 690"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91155318","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 : 2022-11-02DOI: 10.1080/22297928.2022.2159522
Ajay Kumar, R. Chalannavar
Abstract Lifitegrast API was subjected to forced degradation studies under various conditions of hydrolysis (acidic, alkaline, and neutral/water), oxidation, photolysis, and thermal as prescribed by International Conference on Harmonisation guideline Q1A (R2). A short and simple reversed phase HPLC method was developed. The method was developed on a Shimadzu Ultra C18, (100 x 2.1) mm, 3.0 μm column. The gradient method consisted of 0.1% orthophosphoric acid as mobile phase A and mixture of acetonitrile and methanol in the ratio of 50:50 (v/v) as mobile phase B. The flow rate of the mobile phase was 0.8 mL/min. The developed method was validated using ICH Q2 (R1) guidelines. The parameters considered for method validation were solution stability, specificity, DL/QL, linearity, accuracy, precision and robustness. The drug showed significant degradation in acidic and alkaline conditions while slight degradation was observed in oxidative condition. The drug was found stable in water, photolytic and thermal conditions. The characterization of three major degradation products (DP1, DP2, and DP3) was done with LC-Q-TOF-MS/MS in combination with accurate mass measurements. The most probable mechanisms for the formation of DPs have been proposed on the basis fragmentation pattern. GRAPHICAL ABSTRACT
{"title":"Characterization of Degradation Products of Lifitegrast by Mass Spectrometry: Development and Validation of a Stability-indicating Reversed Phase HPLC Method","authors":"Ajay Kumar, R. Chalannavar","doi":"10.1080/22297928.2022.2159522","DOIUrl":"https://doi.org/10.1080/22297928.2022.2159522","url":null,"abstract":"Abstract Lifitegrast API was subjected to forced degradation studies under various conditions of hydrolysis (acidic, alkaline, and neutral/water), oxidation, photolysis, and thermal as prescribed by International Conference on Harmonisation guideline Q1A (R2). A short and simple reversed phase HPLC method was developed. The method was developed on a Shimadzu Ultra C18, (100 x 2.1) mm, 3.0 μm column. The gradient method consisted of 0.1% orthophosphoric acid as mobile phase A and mixture of acetonitrile and methanol in the ratio of 50:50 (v/v) as mobile phase B. The flow rate of the mobile phase was 0.8 mL/min. The developed method was validated using ICH Q2 (R1) guidelines. The parameters considered for method validation were solution stability, specificity, DL/QL, linearity, accuracy, precision and robustness. The drug showed significant degradation in acidic and alkaline conditions while slight degradation was observed in oxidative condition. The drug was found stable in water, photolytic and thermal conditions. The characterization of three major degradation products (DP1, DP2, and DP3) was done with LC-Q-TOF-MS/MS in combination with accurate mass measurements. The most probable mechanisms for the formation of DPs have been proposed on the basis fragmentation pattern. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"14 1","pages":"730 - 744"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88087436","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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