Among the formulation techniques used to enhance thesolubility and dissolution rate of poorly, aqueous-soluble drugs, mesoporoussilica drug delivery systems have shown promise. A range of processes areemployed to load drugs onto silica and solvent-based approaches are widelyemployed. This study aims to understand the influence of drug concentration insolvent and drug-silica ratio on drug solid-state form and amorphization withinsilica. Ritonavirwhich belongs to BCS Class II was used asa model drug. Ritonavir wasloaded into Syloid®244FP using a solvent evaporationmethod. Ritonavir loading percentage was calculated based on the assumptionthat the entire specific surface area of silica is exposed and available fordrug adsorption. Ethanolsolutions with 3 different ritonavir concentrations; 70%, 32% and 20% saturatedsolubility at 25°C were employed. Ritonavir was loaded into silica at 1:1, 1:2and 1:3 ritonavir:silica ratios. Allsystems included ritonavir loaded beyond monolayer surface coverage. Ritonavir- Syloid®244 FP formulations were characterisedusing DSC, PXRD, FT-IR, and TGA. The results showed that all ritonavir-Syloid®244 FP systemsprepared contained ritonavir in a non-crystalline state.
{"title":"The impact of drug-loading factors on the solid-state form of ritonavir-mesoporous silica systems","authors":"Tanweer AL-Dagamin, J. O'shea, A. Crean","doi":"10.5920/bjpharm.1150","DOIUrl":"https://doi.org/10.5920/bjpharm.1150","url":null,"abstract":"Among the formulation techniques used to enhance thesolubility and dissolution rate of poorly, aqueous-soluble drugs, mesoporoussilica drug delivery systems have shown promise. A range of processes areemployed to load drugs onto silica and solvent-based approaches are widelyemployed. This study aims to understand the influence of drug concentration insolvent and drug-silica ratio on drug solid-state form and amorphization withinsilica. Ritonavirwhich belongs to BCS Class II was used asa model drug. Ritonavir wasloaded into Syloid®244FP using a solvent evaporationmethod. Ritonavir loading percentage was calculated based on the assumptionthat the entire specific surface area of silica is exposed and available fordrug adsorption. Ethanolsolutions with 3 different ritonavir concentrations; 70%, 32% and 20% saturatedsolubility at 25°C were employed. Ritonavir was loaded into silica at 1:1, 1:2and 1:3 ritonavir:silica ratios. Allsystems included ritonavir loaded beyond monolayer surface coverage. Ritonavir- Syloid®244 FP formulations were characterisedusing DSC, PXRD, FT-IR, and TGA. The results showed that all ritonavir-Syloid®244 FP systemsprepared contained ritonavir in a non-crystalline state.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"74 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82372220","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 aim of this project is to produce antibiotic-loaded poly (lactic-co-glycolic acid) (PLGA) polymer films by airbrush onto orthopaedic implants to address prosthetic joint infections (PJIs). It covered the development of an airbrush spray-coating technique, the selection and assessment of polymers and antibiotics, sample characterisation and antibacterial studies. The initial results are encouraging as the PLGA coatings exhibited a sustained drug release pattern and antibacterial ability against causative pathogens. Moreover, these PLGA coatings also possessed rapid degradation within 4 weeks which could provide favourable conditions for osseointegration. Furthermore, cytotoxicity assessment of final coatings will need to be conducted to ensure biocompatibility, as well as to determine the effect of each coating on osseointegration. Finally, the development of alternative coating techniques which are more cost-effective and suitable for large scale production might be the direction of future research.
{"title":"A biodegradable and antimicrobial polymer coating for metal implants for the prevention of prosthetic joint infection","authors":"Tiancheng Luo, M. Wylie, C. McCoy","doi":"10.5920/bjpharm.1121","DOIUrl":"https://doi.org/10.5920/bjpharm.1121","url":null,"abstract":"The aim of this project is to produce antibiotic-loaded poly (lactic-co-glycolic acid) (PLGA) polymer films by airbrush onto orthopaedic implants to address prosthetic joint infections (PJIs). It covered the development of an airbrush spray-coating technique, the selection and assessment of polymers and antibiotics, sample characterisation and antibacterial studies. The initial results are encouraging as the PLGA coatings exhibited a sustained drug release pattern and antibacterial ability against causative pathogens. Moreover, these PLGA coatings also possessed rapid degradation within 4 weeks which could provide favourable conditions for osseointegration. Furthermore, cytotoxicity assessment of final coatings will need to be conducted to ensure biocompatibility, as well as to determine the effect of each coating on osseointegration. Finally, the development of alternative coating techniques which are more cost-effective and suitable for large scale production might be the direction of future research. ","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"515 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77080624","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}
Fatemeh Mehradnia, Cara Moloney, R. Cavanagh, A. Pearce, A. Ritchie, P. Clarke, R. Rahman, Asmaa Ibrahim, Anna M. Grabowskab, C. Alexander
The therapeutic efficacy of anticancer nanocarriers ishighly dependent on their size, shape, targeting ability, andstimuli-responsiveness. Herein, we studied the in vivo therapeutic efficacy ofDoxorubicin (Dox) loaded redox responsive micellar-like nanoparticles (MNPs)based on linear 2-hydroxypropyl methacrylamide (HPMA) via histopathologicalevaluations. The therapeutic efficacy of DOX-loaded micellar-like Nanoparticlessignificantly improved while the side effects reduced as confirmed byhistopathological examinations. H&E and tunnel staining of tumor tissuesindicated the higher population of apoptotic tumor cells in both treatmentgroups containing DOX. These redox responsive crosslinked HPMA-basedmicellar-like nanoparticles with acceptable therapeutic efficacy and apoptosisinduction in cancerous cells proved to be promising nanomedicine for breast cancer chemotherapy.
{"title":"Histopathological impact of Redox-responsive methacrylamide based micellar nanoparticles on Orthotopic Models of Triple Negative Breast Cancers","authors":"Fatemeh Mehradnia, Cara Moloney, R. Cavanagh, A. Pearce, A. Ritchie, P. Clarke, R. Rahman, Asmaa Ibrahim, Anna M. Grabowskab, C. Alexander","doi":"10.5920/bjpharm.1173","DOIUrl":"https://doi.org/10.5920/bjpharm.1173","url":null,"abstract":"The therapeutic efficacy of anticancer nanocarriers ishighly dependent on their size, shape, targeting ability, andstimuli-responsiveness. Herein, we studied the in vivo therapeutic efficacy ofDoxorubicin (Dox) loaded redox responsive micellar-like nanoparticles (MNPs)based on linear 2-hydroxypropyl methacrylamide (HPMA) via histopathologicalevaluations. The therapeutic efficacy of DOX-loaded micellar-like Nanoparticlessignificantly improved while the side effects reduced as confirmed byhistopathological examinations. H&E and tunnel staining of tumor tissuesindicated the higher population of apoptotic tumor cells in both treatmentgroups containing DOX. These redox responsive crosslinked HPMA-basedmicellar-like nanoparticles with acceptable therapeutic efficacy and apoptosisinduction in cancerous cells proved to be promising nanomedicine for breast cancer chemotherapy.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86737238","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}
Ariadna Vélez Muga, Pamela Robles Martinez, A. Buanz
Three-dimensional printing (3DP)provides the opportunity to personalise different dosage forms and therapeutic regimenwhere conventional manufacturing processes might not be applicable. Limitedwork has been done to investigate using 3DP for personalising hormonal intrauterinesystems (IUSs). The aim of this work was to prepare 3DP IUS containing progesteroneusing vat photopolymerisation (VPP) technique. The device was successfullyprinted and showed a slow release in phosphate buffer (pH 7.4). VPP has theadvantages of better printing resolution producing smoother surfaces, and theelimination of the pre-printing process of hot melt extrusion (HME) needed for fuseddeposition modelling (FDM) method. To the author’s knowledge, this is the firstreport of using VPP for printing hormone-loaded IUSs.@font-face{font-family:"Cambria Math";panose-1:2 4 5 3 5 4 6 3 2 4;mso-font-charset:0;mso-generic-font-family:roman;mso-font-pitch:variable;mso-font-signature:-536870145 1107305727 0 0 415 0;}@font-face{font-family:Calibri;panose-1:2 15 5 2 2 2 4 3 2 4;mso-font-charset:0;mso-generic-font-family:swiss;mso-font-pitch:variable;mso-font-signature:-469750017 -1073732485 9 0 511 0;}p.MsoNormal, li.MsoNormal, div.MsoNormal{mso-style-unhide:no;mso-style-qformat:yes;mso-style-parent:"";margin-top:0cm;margin-right:0cm;margin-bottom:10.0pt;margin-left:0cm;line-height:115%;mso-pagination:widow-orphan;font-size:11.0pt;font-family:"Arial",sans-serif;mso-fareast-font-family:Calibri;mso-fareast-language:EN-US;}.MsoChpDefault{mso-style-type:export-only;mso-default-props:yes;font-size:10.0pt;mso-ansi-font-size:10.0pt;mso-bidi-font-size:10.0pt;font-family:"Arial",sans-serif;mso-ascii-font-family:Arial;mso-fareast-font-family:Calibri;mso-hansi-font-family:Arial;mso-bidi-font-family:Arial;}div.WordSection1{page:WordSection1;}
{"title":"3D Printing of Progesterone-Loaded Intrauterine System Using Vat Photopolymerisation","authors":"Ariadna Vélez Muga, Pamela Robles Martinez, A. Buanz","doi":"10.5920/bjpharm.1071","DOIUrl":"https://doi.org/10.5920/bjpharm.1071","url":null,"abstract":"Three-dimensional printing (3DP)provides the opportunity to personalise different dosage forms and therapeutic regimenwhere conventional manufacturing processes might not be applicable. Limitedwork has been done to investigate using 3DP for personalising hormonal intrauterinesystems (IUSs). The aim of this work was to prepare 3DP IUS containing progesteroneusing vat photopolymerisation (VPP) technique. The device was successfullyprinted and showed a slow release in phosphate buffer (pH 7.4). VPP has theadvantages of better printing resolution producing smoother surfaces, and theelimination of the pre-printing process of hot melt extrusion (HME) needed for fuseddeposition modelling (FDM) method. To the author’s knowledge, this is the firstreport of using VPP for printing hormone-loaded IUSs.@font-face{font-family:\"Cambria Math\";panose-1:2 4 5 3 5 4 6 3 2 4;mso-font-charset:0;mso-generic-font-family:roman;mso-font-pitch:variable;mso-font-signature:-536870145 1107305727 0 0 415 0;}@font-face{font-family:Calibri;panose-1:2 15 5 2 2 2 4 3 2 4;mso-font-charset:0;mso-generic-font-family:swiss;mso-font-pitch:variable;mso-font-signature:-469750017 -1073732485 9 0 511 0;}p.MsoNormal, li.MsoNormal, div.MsoNormal{mso-style-unhide:no;mso-style-qformat:yes;mso-style-parent:\"\";margin-top:0cm;margin-right:0cm;margin-bottom:10.0pt;margin-left:0cm;line-height:115%;mso-pagination:widow-orphan;font-size:11.0pt;font-family:\"Arial\",sans-serif;mso-fareast-font-family:Calibri;mso-fareast-language:EN-US;}.MsoChpDefault{mso-style-type:export-only;mso-default-props:yes;font-size:10.0pt;mso-ansi-font-size:10.0pt;mso-bidi-font-size:10.0pt;font-family:\"Arial\",sans-serif;mso-ascii-font-family:Arial;mso-fareast-font-family:Calibri;mso-hansi-font-family:Arial;mso-bidi-font-family:Arial;}div.WordSection1{page:WordSection1;}","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"128 13 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88217310","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}
We developed a set of methoxypoly(ethyleneglycol)-co-poly(N3-ε-caprolactone) (mPEG-N3PCL)copolymers with different types of amine linkers and investigated thecontribution of the introduced amino linker to the gene delivery efficiency ofnanoparticles. The nanoparticles were crosslinked from the caprolactone regionswith a redox-responsive linker. Formulation variables including Redox-crosslinkingand N:P ratio were examined to obtain nanoparticles with optimal size andhighest siRNA entrapment efficacy (EE). The nanoparticles were characterized byDLS, and nanodrop UV-vis spectroscopy. Nanoparticle size, polydispersity index and siRNAentrapment efficacy were found to depend on the all the examined formulationvariables specially the N:P ratio. The formulation with N:P ratio of 5 with56.13 nm in size and 92.24% EE was chosen as the optimal formulation.Controllable size, loading efficiency and releasepattern by redox-responsivity make this class of novel carriers a promisingcandidate for tumour targeted gene delivery applications.
{"title":"The effect of Amine modification on siRNA delivery of redox-responsive PEGylated amphiphilic micellar nanoparticles for triple negative breast cancer therapy","authors":"Fatemeh Mehradnia, C. Alexander","doi":"10.5920/bjpharm.1119","DOIUrl":"https://doi.org/10.5920/bjpharm.1119","url":null,"abstract":"We developed a set of methoxypoly(ethyleneglycol)-co-poly(N3-ε-caprolactone) (mPEG-N3PCL)copolymers with different types of amine linkers and investigated thecontribution of the introduced amino linker to the gene delivery efficiency ofnanoparticles. The nanoparticles were crosslinked from the caprolactone regionswith a redox-responsive linker. Formulation variables including Redox-crosslinkingand N:P ratio were examined to obtain nanoparticles with optimal size andhighest siRNA entrapment efficacy (EE). The nanoparticles were characterized byDLS, and nanodrop UV-vis spectroscopy. Nanoparticle size, polydispersity index and siRNAentrapment efficacy were found to depend on the all the examined formulationvariables specially the N:P ratio. The formulation with N:P ratio of 5 with56.13 nm in size and 92.24% EE was chosen as the optimal formulation.Controllable size, loading efficiency and releasepattern by redox-responsivity make this class of novel carriers a promisingcandidate for tumour targeted gene delivery applications. ","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"17 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77408343","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}
Joshua S. Walker, Syampriya Bindhu Syammohan, Z. Rattray
Thecombination of field-flow fractionation with powerful leading-edge detectors canbe applied to the measurement of nanomaterial physicochemical properties, and thecreation of harmonized robust measurement protocols. The Multiscale MetrologySuite (MMS) at the University of Strathclyde is a unique internationallyleading facility combining multiple leading-edge field flow fractionation modalities(electric, asymmetric and centrifugal) with in-line Raman, inductively-coupledplasma (ICP) mass spectrometry and multimodal detector capability. Using exemplarcase studies, we demonstrate the application of various FFF hyphenations forthe analysis of a diverse materials portfolio. One of the goals for the MMS isto raise the standards of traditional academic analytical support underpinningpioneering academic engineering, physical and life sciences research exploringnovel materials as diagnostics and therapeutics.
{"title":"The Application of Field-Flow Fractionation to the Analysis of Nanomedicines","authors":"Joshua S. Walker, Syampriya Bindhu Syammohan, Z. Rattray","doi":"10.5920/bjpharm.1132","DOIUrl":"https://doi.org/10.5920/bjpharm.1132","url":null,"abstract":"Thecombination of field-flow fractionation with powerful leading-edge detectors canbe applied to the measurement of nanomaterial physicochemical properties, and thecreation of harmonized robust measurement protocols. The Multiscale MetrologySuite (MMS) at the University of Strathclyde is a unique internationallyleading facility combining multiple leading-edge field flow fractionation modalities(electric, asymmetric and centrifugal) with in-line Raman, inductively-coupledplasma (ICP) mass spectrometry and multimodal detector capability. Using exemplarcase studies, we demonstrate the application of various FFF hyphenations forthe analysis of a diverse materials portfolio. One of the goals for the MMS isto raise the standards of traditional academic analytical support underpinningpioneering academic engineering, physical and life sciences research exploringnovel materials as diagnostics and therapeutics.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73007390","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}
Edward Paul Rhodes, N. Dawson, Jeremy Everett, Debbie Kraus, Michael Cram, Paul Whiteside
Punchsticking is a common tablet compression manufacturing issue experienced duringlate-stage large-scale manufacturing. Prediction of punch sticking propensityand identification of the sticking component is important for early-stageformulation development. Application of novel predictive capabilities offers early-stagesticking propensity assessment. 16 API compounds were utilised to assess punchsticking prediction using removable punch tip tooling. API descriptors weretested for sticking correlation using multivariate analysis. NIR imaging, SEM-EDXand Raman microscopy were used to examine the material adhered to the punch tips.Predictive modelling using linear and non-linear equations proved inaccurate inpunch sticking mass prediction. PCA analysisidentified sticking correlated physical descriptors and provided a dataset andmethod for further descriptor studies. Raman microscopy was identified as asuitable technique for chemical identification of punch sticking material, whichoffers insight towards a mechanistic understanding.
{"title":"Assessment of Prediction Models for Punch Sticking in Tablet Formulations","authors":"Edward Paul Rhodes, N. Dawson, Jeremy Everett, Debbie Kraus, Michael Cram, Paul Whiteside","doi":"10.5920/bjpharm.1118","DOIUrl":"https://doi.org/10.5920/bjpharm.1118","url":null,"abstract":"Punchsticking is a common tablet compression manufacturing issue experienced duringlate-stage large-scale manufacturing. Prediction of punch sticking propensityand identification of the sticking component is important for early-stageformulation development. Application of novel predictive capabilities offers early-stagesticking propensity assessment. 16 API compounds were utilised to assess punchsticking prediction using removable punch tip tooling. API descriptors weretested for sticking correlation using multivariate analysis. NIR imaging, SEM-EDXand Raman microscopy were used to examine the material adhered to the punch tips.Predictive modelling using linear and non-linear equations proved inaccurate inpunch sticking mass prediction. PCA analysisidentified sticking correlated physical descriptors and provided a dataset andmethod for further descriptor studies. Raman microscopy was identified as asuitable technique for chemical identification of punch sticking material, whichoffers insight towards a mechanistic understanding.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"1954 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91220352","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}
Aylla Mesquita Pestana, Ana Luiza Martins Lucas, Gabriela Gama Xavier Augusto, Lígia Ribeiro, Y. Costa, M. Franz-Montan
In a randomizedplacebo-controlledcrossover trial the present study evaluated if nanostructured lipidnanocarriers (NLC) could improve the topical anaesthetic efficacy of lidocaineand prilocaine (L+P) incorporated in a xanthan-hydrogel on the oral cavity.There was no difference among topical formulations in reducing pain duringneedle insertion or local anaesthetic injection. Nonetheless, exploratoryanalyses indicate that individuals with low mechanical pain sensitivity mightbe more susceptible to placebo effects which could also interfere with theanaesthetic effects of the topical formulations. Thus, mechanical painsensitivity can be an interesting approach to increase assay sensitivity inclinical trials of topical anaesthesia.In a randomizedplacebo-controlledcrossover trial the present study evaluated if nanostructured lipidnanocarriers (NLC) could improve the topical anaesthetic efficacy of lidocaineand prilocaine (L+P) incorporated in a xanthan-hydrogel on the oral cavity.There was no difference among topical formulations in reducing pain duringneedle insertion or local anaesthetic injection. Nonetheless, exploratoryanalyses indicate that individuals with low mechanical pain sensitivity mightbe more susceptible to placebo effects which could also interfere with theanaesthetic effects of the topical formulations. Thus, mechanical painsensitivity can be an interesting approach to increase assay sensitivity inclinical trials of topical anaesthesia.
{"title":"Anaesthetic efficacy of intraoral topical lidocaine and prilocaine in nanostrusctured lipid nanocarriers: a randomized clinical trial Efficacy of intraoral topical anaesthetics in nanostrusctured lipid nanocarriers","authors":"Aylla Mesquita Pestana, Ana Luiza Martins Lucas, Gabriela Gama Xavier Augusto, Lígia Ribeiro, Y. Costa, M. Franz-Montan","doi":"10.5920/bjpharm.1082","DOIUrl":"https://doi.org/10.5920/bjpharm.1082","url":null,"abstract":"In a randomizedplacebo-controlledcrossover trial the present study evaluated if nanostructured lipidnanocarriers (NLC) could improve the topical anaesthetic efficacy of lidocaineand prilocaine (L+P) incorporated in a xanthan-hydrogel on the oral cavity.There was no difference among topical formulations in reducing pain duringneedle insertion or local anaesthetic injection. Nonetheless, exploratoryanalyses indicate that individuals with low mechanical pain sensitivity mightbe more susceptible to placebo effects which could also interfere with theanaesthetic effects of the topical formulations. Thus, mechanical painsensitivity can be an interesting approach to increase assay sensitivity inclinical trials of topical anaesthesia.In a randomizedplacebo-controlledcrossover trial the present study evaluated if nanostructured lipidnanocarriers (NLC) could improve the topical anaesthetic efficacy of lidocaineand prilocaine (L+P) incorporated in a xanthan-hydrogel on the oral cavity.There was no difference among topical formulations in reducing pain duringneedle insertion or local anaesthetic injection. Nonetheless, exploratoryanalyses indicate that individuals with low mechanical pain sensitivity mightbe more susceptible to placebo effects which could also interfere with theanaesthetic effects of the topical formulations. Thus, mechanical painsensitivity can be an interesting approach to increase assay sensitivity inclinical trials of topical anaesthesia.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"5 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79663373","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}
Phoebe Greensides, Mark McAllister, Inese Sarcervica, I. Tomaszewska
Surfactants are often used to improve the solubility of a compound for dissolution studies in aqueous media. Having observed non-linear solubility enhancement with increasing surfactant concentration, this study investigated the effect of a poorly soluble, zwitterionic, moderately lipophilic drug, Compound A, on the critical micelle concentration (CMC)of sodium lauryl sulfate (SLS) in phosphate buffer. A force tensiometer was used to measure the surface tension of the solutions over a range of surfactant concentrations. The presence of Compound A demonstrated a decrease in the CMC, suggesting that the solution favours micellisation at lower surfactant concentrations in the presence of the drug. Future studies will use a fully saturated solution of Compound A to explore this observation further. Additional experiments will also investigate micelle formation of SLS with other compounds.
{"title":"Exploring drug-surfactant interactions and their impact on the intrinsic surface properties of aqueous dissolution media","authors":"Phoebe Greensides, Mark McAllister, Inese Sarcervica, I. Tomaszewska","doi":"10.5920/bjpharm.1081","DOIUrl":"https://doi.org/10.5920/bjpharm.1081","url":null,"abstract":"Surfactants are often used to improve the solubility of a compound for dissolution studies in aqueous media. Having observed non-linear solubility enhancement with increasing surfactant concentration, this study investigated the effect of a poorly soluble, zwitterionic, moderately lipophilic drug, Compound A, on the critical micelle concentration (CMC)of sodium lauryl sulfate (SLS) in phosphate buffer. A force tensiometer was used to measure the surface tension of the solutions over a range of surfactant concentrations. The presence of Compound A demonstrated a decrease in the CMC, suggesting that the solution favours micellisation at lower surfactant concentrations in the presence of the drug. Future studies will use a fully saturated solution of Compound A to explore this observation further. Additional experiments will also investigate micelle formation of SLS with other compounds.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"77 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77076332","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}
Dania Hussein Alhyari, K. Paluch, Helen Sheldrake Sheldrake, Harsha Kantamneni, M. Isreb, Shohreh Jafarinejad Soumehsaraei, W. Martin, N. Qinna
Gallic acid (GA) is known for its antioxidant activitywhichis restricted due to its low oral permeability. In this project the carboxylic group of (GA) was substitutedwith sulfonamide group and hydroxyl groups were methylated which resulted insignificantly (p<0.01) increased permeability of 3,4,5-trimethoxybenzenesulfonamide (TMBS) and 3,4,5-trihydroxybenzenesulfonamide (THBS) over GA, inParallel Artificial Membrane Permeability Assay studies with simulatedgastrointestinal fluids and Human intestinal epithelial cells HIEC-6 cells.Biochemical studies confirmed TMBS was O-demethylated by CYP2D6. THBS and GAhad increased antioxidant activity with increased concentration in DPPH assaywhile TMBS indicated lower activity at all tested concentration. Theantioxidant activity of TMBS was greater than GA in HIEC-6 cells which mainlyrelated to its O-demethylation by CYP2D6.
没食子酸(GA)以其抗氧化活性而闻名，但由于其口腔渗透性低，抗氧化活性受到限制。在模拟胃肠道液体和人肠上皮细胞hiec6细胞的平行人工膜通透性实验中，本项目将(GA)的羧基基替换为磺胺基，羟基甲基化，导致3,4,5-三甲氧基苯磺酰胺(TMBS)和3,4,5-三羟基苯磺酰胺(THBS)的通透性比GA增加不显著(p<0.01)。生化研究证实TMBS被CYP2D6 o -去甲基化。在DPPH实验中，THBS和gab的抗氧化活性随浓度的增加而增加，而TMBS的抗氧化活性随浓度的增加而降低。TMBS在HIEC-6细胞中的抗氧化活性高于GA，这主要与其被CYP2D6去甲基化有关。
{"title":"Physicochemical and biopharmaceutical characterization of new sulfonamide derivatives of gallic acid","authors":"Dania Hussein Alhyari, K. Paluch, Helen Sheldrake Sheldrake, Harsha Kantamneni, M. Isreb, Shohreh Jafarinejad Soumehsaraei, W. Martin, N. Qinna","doi":"10.5920/bjpharm.1138","DOIUrl":"https://doi.org/10.5920/bjpharm.1138","url":null,"abstract":"Gallic acid (GA) is known for its antioxidant activitywhichis restricted due to its low oral permeability. In this project the carboxylic group of (GA) was substitutedwith sulfonamide group and hydroxyl groups were methylated which resulted insignificantly (p<0.01) increased permeability of 3,4,5-trimethoxybenzenesulfonamide (TMBS) and 3,4,5-trihydroxybenzenesulfonamide (THBS) over GA, inParallel Artificial Membrane Permeability Assay studies with simulatedgastrointestinal fluids and Human intestinal epithelial cells HIEC-6 cells.Biochemical studies confirmed TMBS was O-demethylated by CYP2D6. THBS and GAhad increased antioxidant activity with increased concentration in DPPH assaywhile TMBS indicated lower activity at all tested concentration. Theantioxidant activity of TMBS was greater than GA in HIEC-6 cells which mainlyrelated to its O-demethylation by CYP2D6. ","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"9 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85727650","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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