Pub Date : 2022-12-26DOI: 10.55262/fabadeczacilik.1175781
B. Özüpek, S. Pekacar, D. Deliorman Orhan
Salvia officinalis L., known as medicinal sage, and Salvia triloba L., known as Anatolian sage, belong to the Lamiaceae family and are species that usually grow in the Mediterranean region. In this study, it was aimed to evaluate the in vitro antidiabetic, antiobesity and antioxidant potentials of the extracts prepared by infusion technique from S. officinalis and S. triloba grown by organic farming methods. In addition, the effects of the extracts on the pancreatic cholesterol esterase enzyme were also investigated. Reverse Phase-HPLC technique was used to analyze the phytochemical contents of the extracts. At a concentration of 2 mg/mL, S. officinalis inhibited 64.69% ± 0.23, S. triloba 47.78 ± 2.11% on the α-glucosidase enzyme. Only S. triloba had an inhibitory effect on α-amylase and pancreatic lipase enzyme. On the pancreatic cholesterol esterase enzyme, inhibition values of S. triloba extract at all tested concentrations were found to be higher than S. officinalis extract. When the antioxidant potentials of the extracts were evaluated, the reducing power absorbance values were found to be the highest of the S. officinalis extract. The metal chelating capacity of both extracts at a concentration of 2 mg/mL was calculated as 100%. It was concluded that the ABTS radical scavenging activity of the extracts increased in a dose-dependent manner. With the Reverse Phase-YPSK technique, rosmarinic acid and hesperidin were found to be higher in S. officinalis extract. The presence of hesperidin in S. triloba was detected for the first time in this study. Considering all these findings, it was concluded that activity-guided isolation and in vivo activity studies should be performed because these two species grown by organic farming method have strong α-glucosidase enzyme inhibitory and antioxidant effects.
{"title":"Evaluation of Phytochemical Contents and Biological Activities of Salvia officinalis and Salvia triloba Grown with Organic Farming","authors":"B. Özüpek, S. Pekacar, D. Deliorman Orhan","doi":"10.55262/fabadeczacilik.1175781","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1175781","url":null,"abstract":"Salvia officinalis L., known as medicinal sage, and Salvia triloba L., known as Anatolian sage, belong to the Lamiaceae family and are species that usually grow in the Mediterranean region. In this study, it was aimed to evaluate the in vitro antidiabetic, antiobesity and antioxidant potentials of the extracts prepared by infusion technique from S. officinalis and S. triloba grown by organic farming methods. In addition, the effects of the extracts on the pancreatic cholesterol esterase enzyme were also investigated. Reverse Phase-HPLC technique was used to analyze the phytochemical contents of the extracts. At a concentration of 2 mg/mL, S. officinalis inhibited 64.69% ± 0.23, S. triloba 47.78 ± 2.11% on the α-glucosidase enzyme. Only S. triloba had an inhibitory effect on α-amylase and pancreatic lipase enzyme. On the pancreatic cholesterol esterase enzyme, inhibition values of S. triloba extract at all tested concentrations were found to be higher than S. officinalis extract. When the antioxidant potentials of the extracts were evaluated, the reducing power absorbance values were found to be the highest of the S. officinalis extract. The metal chelating capacity of both extracts at a concentration of 2 mg/mL was calculated as 100%. It was concluded that the ABTS radical scavenging activity of the extracts increased in a dose-dependent manner. With the Reverse Phase-YPSK technique, rosmarinic acid and hesperidin were found to be higher in S. officinalis extract. The presence of hesperidin in S. triloba was detected for the first time in this study. Considering all these findings, it was concluded that activity-guided isolation and in vivo activity studies should be performed because these two species grown by organic farming method have strong α-glucosidase enzyme inhibitory and antioxidant effects.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86724533","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 : 2022-12-26DOI: 10.55262/fabadeczacilik.1126288
Thulasi Sathyanarayana, P. Sudheer, E. Jacob, Merlin Mary Sabu
Purpose: Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) which when administered via an oral route displays significant gastro-intestinal side effects and has low skin permeation profile. The objective of the present work is to utilise nanostructured lipid carriers (NLCs) as carrier system for transdermal delivery of ketoprofen. Methods: NLCs were prepared via hot homogenisation technique using bees wax, carnauba wax, glycerl monostearate (solid lipids), linseed oil (liquid lipid) and poloxamer188 (surfactant) and optimized using custom design via JMP. The responses evaluated were drug entrapment efficiency, particle size and drug release profile. The experimental design was evaluated for model fit with the assistance of ANOVA. The optimum formulations were characterized for particle size, zeta potential, SEM, DSC, FTIR and also drug content, entrapment efficiency, in- vitro drug release, ex-vivo drug release profile was studied. Results: The drug entrapment in the range of 34±0.03-95.06±0.01%. The drug release from the formulations over a 24 h study was found to be 80%±0.09 to 95%±0.06. The maximum desirability was found to be 0.91. The optimum formulation showed mean particle size of 425.8nm and a zeta potential of -45mV. SEM results revealed slightly agglomerated particles with uneven surfaces. The ex-vivo skin permeation of NLC optimized patch formulation exhibited a higher flux and permeability coefficient in comparison to the pure drug patch formulation and marketed gel (2.5%w/w) FTIR spectra assured the chemical and physical compatibility. Conclusion: Transdermal delivery of ketoprofen via NLCs would be a promising approach for improving the skin permeation.
{"title":"Development and Evaluation of Nanostructured Lipid Carriers for Transdermal Delivery of Ketoprofen","authors":"Thulasi Sathyanarayana, P. Sudheer, E. Jacob, Merlin Mary Sabu","doi":"10.55262/fabadeczacilik.1126288","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1126288","url":null,"abstract":"Purpose: Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) which when administered via an oral route displays significant gastro-intestinal side effects and has low skin permeation profile. The objective of the present work is to utilise nanostructured lipid carriers (NLCs) as carrier system for transdermal delivery of ketoprofen. \u0000Methods: NLCs were prepared via hot homogenisation technique using bees wax, carnauba wax, glycerl monostearate (solid lipids), linseed oil (liquid lipid) and poloxamer188 (surfactant) and optimized using custom design via JMP. The responses evaluated were drug entrapment efficiency, particle size and drug release profile. The experimental design was evaluated for model fit with the assistance of ANOVA. The optimum formulations were characterized for particle size, zeta potential, SEM, DSC, FTIR and also drug content, entrapment efficiency, in- vitro drug release, ex-vivo drug release profile was studied. \u0000Results: The drug entrapment in the range of 34±0.03-95.06±0.01%. The drug release from the formulations over a 24 h study was found to be 80%±0.09 to 95%±0.06. The maximum desirability was found to be 0.91. The optimum formulation showed mean particle size of 425.8nm and a zeta potential of -45mV. SEM results revealed slightly agglomerated particles with uneven surfaces. The ex-vivo skin permeation of NLC optimized patch formulation exhibited a higher flux and permeability coefficient in comparison to the pure drug patch formulation and marketed gel (2.5%w/w) FTIR spectra assured the chemical and physical compatibility. \u0000Conclusion: Transdermal delivery of ketoprofen via NLCs would be a promising approach for improving the skin permeation.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90728196","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 : 2022-12-01DOI: 10.55262/fabadeczacilik.1099287
Merve Karpuz, Emre Özgenç, E. Gündoğdu, Z. Burak
Enfeksiyon hastalıkları hala dünyada temel sağlık problemlerinden birini oluşturmaktadır. Enfeksiyonun erken aşamalarda teşhisi ve kanser veya inflamasyon gibi diğer patolojilerden ayrımı, enfeksiyonu akut aşamalarda tedavi etmede kritik rol oynamaktadır. Enfeksiyon teşhisinde kullanılan görüntüleme yöntemleri tüm vücut görüntüsü alabilme, enfeksiyonu odağını ve evresini tespit edebilme ve hastalığı izleyebilme gibi avantajlara sahiptir. Enfeksiyon tedavisinde çeşitli antibiyotikler kullanılmasına rağmen, klinikte antibiyotiklerin ciddi yan etkileri ve antimikrobiyal direnç gelişimi gibi problemler mevcuttur. Çalışmamızda enfeksiyon için teranostik bir ajan geliştirme amacıyla gram pozitif bakterilere karşı etkili ikinci nesil oksazolidinon antibiyotiği olan tedizolid, 177Lu radyonüklidi ile radyoişaretlenmiştir. Radyoiaşretleme, oda koşullarında gerçekleştirilmiş ve işaretleme etkinliği ile stabilitesi, kağıt kromatografisi ve HPLC ile değerlendirilmiştir. Yüksek radyoişaretleme verimi elde etmek için optimum inkübasyon süresi 60 dakika olarak bulunmuştur. 177Lu-TDZ çözeltisindeki radyokimyasal safsızlıkları belirleme amacıyla kağıt kromatografisi için farklı mobil ve sabit fazlar test edilmiş ve sabit faz olarak ITLC-SG uygun bulunmuştur. Ayrıca amonyum hidroksit: metanol: su ve DTPA çözeltileri mobil faz olarak seçilmiştir. HPLC kromatogramında serbest 177Lu ve 177Lu-TDZ kompleksinin alıkonma sürelerine bağlı olarak iki farklı pik gözlenmiştir. Ne yazık ki, radyoişaretleme stabilitesi testlerinin sonuçlarında %80'in üzerinde saflık değerleri elde edilememiştir, bu nedenle radyoişaretleme ortamına şelatla yapıcı ajan eklenmesi önerilmiştir.
{"title":"Enfeksiyon Görüntüleme ve Tedavisi için 177Lutesyum-Tedizolid","authors":"Merve Karpuz, Emre Özgenç, E. Gündoğdu, Z. Burak","doi":"10.55262/fabadeczacilik.1099287","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1099287","url":null,"abstract":"Enfeksiyon hastalıkları hala dünyada temel sağlık problemlerinden birini oluşturmaktadır. Enfeksiyonun erken aşamalarda teşhisi ve kanser veya inflamasyon gibi diğer patolojilerden ayrımı, enfeksiyonu akut aşamalarda tedavi etmede kritik rol oynamaktadır. Enfeksiyon teşhisinde kullanılan görüntüleme yöntemleri tüm vücut görüntüsü alabilme, enfeksiyonu odağını ve evresini tespit edebilme ve hastalığı izleyebilme gibi avantajlara sahiptir. Enfeksiyon tedavisinde çeşitli antibiyotikler kullanılmasına rağmen, klinikte antibiyotiklerin ciddi yan etkileri ve antimikrobiyal direnç gelişimi gibi problemler mevcuttur. Çalışmamızda enfeksiyon için teranostik bir ajan geliştirme amacıyla gram pozitif bakterilere karşı etkili ikinci nesil oksazolidinon antibiyotiği olan tedizolid, 177Lu radyonüklidi ile radyoişaretlenmiştir. Radyoiaşretleme, oda koşullarında gerçekleştirilmiş ve işaretleme etkinliği ile stabilitesi, kağıt kromatografisi ve HPLC ile değerlendirilmiştir. Yüksek radyoişaretleme verimi elde etmek için optimum inkübasyon süresi 60 dakika olarak bulunmuştur. 177Lu-TDZ çözeltisindeki radyokimyasal safsızlıkları belirleme amacıyla kağıt kromatografisi için farklı mobil ve sabit fazlar test edilmiş ve sabit faz olarak ITLC-SG uygun bulunmuştur. Ayrıca amonyum hidroksit: metanol: su ve DTPA çözeltileri mobil faz olarak seçilmiştir. HPLC kromatogramında serbest 177Lu ve 177Lu-TDZ kompleksinin alıkonma sürelerine bağlı olarak iki farklı pik gözlenmiştir. Ne yazık ki, radyoişaretleme stabilitesi testlerinin sonuçlarında %80'in üzerinde saflık değerleri elde edilememiştir, bu nedenle radyoişaretleme ortamına şelatla yapıcı ajan eklenmesi önerilmiştir.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83556145","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 : 2022-12-01DOI: 10.55262/fabadeczacilik.1164699
Y. Erzurumlu, Deniz Çataklı, Hatice Kübra Doğan, Esra Aydogdu
Breast cancer is the most frequently diagnosed cancer type among women. Chemotherapeutics are widely used for breast cancer treatment but acquired drug resistance is the main reason that limits their efficacy. Therefore, there is a continuing need for more effective treatment approaches with fewer side effects. One of the naturally occurring xanthine in coffee beans, caffeine is the most commonly used psychoactive substance worldwide. Numerous studies have drawn attention to the health benefits of coffee intake including decrement in risk of heart disease and risk of some cancers. Docetaxel is a second-generation antineoplastic agent of the taxane family and is widely used in the treatment of numerous cancers such as breast cancer. Herein, we evaluate the effect of caffeine and its combination with docetaxel on MCF-7 breast cancer cells. To test the effect of caffeine and its combination with docetaxel, we evaluate the autophagy, ubiquitin-proteasome system, unfolded protein response signaling and apoptosis-related protein levels were examined by immunoblotting. Cell viability was measured by WST-1 method. Morphological alterations in cells were evaluated in microscopical examinations. We found that caffeine remarkably induced UPR signaling, accelerated autophagic flux, and UPS-dependent protein turnover. Co-administration of caffeine and docetaxel strongly diminished the viability of MCF-7 cells by expanding the cytotoxic effect of docetaxel through accelerating the UPS-dependent protein turnover, induction of autophagy and apoptotic protein levels in a manner dose-dependently. Our results suggest that caffeine supplementation with docetaxel may expand the chemotherapeutic efficiency of docetaxel in breast cancer.
{"title":"Caffeine May Improve the Chemotherapeutic Effect of Docetaxel by Inducing UPR and Autophagy in Breast Cancer Cells","authors":"Y. Erzurumlu, Deniz Çataklı, Hatice Kübra Doğan, Esra Aydogdu","doi":"10.55262/fabadeczacilik.1164699","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1164699","url":null,"abstract":"Breast cancer is the most frequently diagnosed cancer type among women. Chemotherapeutics are widely used for breast cancer treatment but acquired drug resistance is the main reason that limits their efficacy. Therefore, there is a continuing need for more effective treatment approaches with fewer side effects. One of the naturally occurring xanthine in coffee beans, caffeine is the most commonly used psychoactive substance worldwide. Numerous studies have drawn attention to the health benefits of coffee intake including decrement in risk of heart disease and risk of some cancers. Docetaxel is a second-generation antineoplastic agent of the taxane family and is widely used in the treatment of numerous cancers such as breast cancer. Herein, we evaluate the effect of caffeine and its combination with docetaxel on MCF-7 breast cancer cells. To test the effect of caffeine and its combination with docetaxel, we evaluate the autophagy, ubiquitin-proteasome system, unfolded protein response signaling and apoptosis-related protein levels were examined by immunoblotting. Cell viability was measured by WST-1 method. Morphological alterations in cells were evaluated in microscopical examinations. We found that caffeine remarkably induced UPR signaling, accelerated autophagic flux, and UPS-dependent protein turnover. Co-administration of caffeine and docetaxel strongly diminished the viability of MCF-7 cells by expanding the cytotoxic effect of docetaxel through accelerating the UPS-dependent protein turnover, induction of autophagy and apoptotic protein levels in a manner dose-dependently. Our results suggest that caffeine supplementation with docetaxel may expand the chemotherapeutic efficiency of docetaxel in breast cancer.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73400090","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 : 2022-12-01DOI: 10.55262/fabadeczacilik.1133276
Ece Türkmen, Selin Parmaksız, M. Çelebier, S. Şenel
Miconazole nitrate (MN) and chlorhexidine digluconate (CHX) are the commonly used antimicrobials for topical treatment of dermal infections. Combination of antimicrobials has been investigated to enhance the efficacy of the treatment. Gel formulations based on bioadhesive polymers are preferred for delivery of these drugs. Chitosan is a promising bioadhesive polymer due to its penetration enhancing, antimicrobial and tissue healing properties. Yet, most of the gel-based formulations present analytical challenges during testing the drug content. It was aimed to develop an HPLC method for simultaneous determination of MN and CHX in chitosan-based gel formulations. Different solvent combinations were investigated for extraction of drugs from the gels. HPLC conditions such as mobile phase, flow rate, run time, column temperature and wavelength were explored. The method was validated according to ICH guideline Q2(R1). MN and CHX were extracted in solvent composition same with the mobile phase. The method was employed on ACE-C8 column at 40°C by isocratic elution using the mobile phase consisting of methanol:phosphate (75:25 v/v) buffer (containing triethylamine). Flow rate was 1 mL/min. The drugs were detected at 254 nm (CHX) and 230 nm (MN). Linearity was obtained between 5 to 80 μg/mL for both drugs. LOD and LOQ obtained for CHX was 1.61 and 1.06, for MN: 4.87 and 3.21 µg/mL, respectively. A new validated HPLC method was developed for simultaneous determination of CHX and MN in chitosan-based gels, with 98 to 102% recovery, without any interference with the excipients.
{"title":"Development and Validation of an HPLC Method for Simultaneous Determination of Miconazole Nitrate and Chlorhexidine Digluconate in Chitosan-Based Gel Formulations","authors":"Ece Türkmen, Selin Parmaksız, M. Çelebier, S. Şenel","doi":"10.55262/fabadeczacilik.1133276","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1133276","url":null,"abstract":"Miconazole nitrate (MN) and chlorhexidine digluconate (CHX) are the commonly used antimicrobials for topical treatment of dermal infections. Combination of antimicrobials has been investigated to enhance the efficacy of the treatment. Gel formulations based on bioadhesive polymers are preferred for delivery of these drugs. Chitosan is a promising bioadhesive polymer due to its penetration enhancing, antimicrobial and tissue healing properties. Yet, most of the gel-based formulations present analytical challenges during testing the drug content. It was aimed to develop an HPLC method for simultaneous determination of MN and CHX in chitosan-based gel formulations. Different solvent combinations were investigated for extraction of drugs from the gels. HPLC conditions such as mobile phase, flow rate, run time, column temperature and wavelength were explored. The method was validated according to ICH guideline Q2(R1). MN and CHX were extracted in solvent composition same with the mobile phase. The method was employed on ACE-C8 column at 40°C by isocratic elution using the mobile phase consisting of methanol:phosphate (75:25 v/v) buffer (containing triethylamine). Flow rate was 1 mL/min. The drugs were detected at 254 nm (CHX) and 230 nm (MN). Linearity was obtained between 5 to 80 μg/mL for both drugs. LOD and LOQ obtained for CHX was 1.61 and 1.06, for MN: 4.87 and 3.21 µg/mL, respectively. A new validated HPLC method was developed for simultaneous determination of CHX and MN in chitosan-based gels, with 98 to 102% recovery, without any interference with the excipients.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72895151","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 : 2022-11-29DOI: 10.55262/fabadeczacilik.1085351
Sw Chopade
A fast-dissolving dosage form is an approach used to improve therapeutic efficacy and bioavailability by avoiding the first-pass metabolism of the cargo. Besides, the approach causes rapid cargo absorption from the pre-gastric area which may outcome in the quick inception of action. The trimetazidine dihydrochloride (TDC) is an anti-anginal drug and there is a prerequisite to provide fast onset of action to treat angina. Therefore, the present work was aimed to prepare and evaluate fast-dissolving oral films (FDOF) of TDC to provide fast onset of action. The FDOF is prepared by using the solvent casting method and it was optimized by employing a central composite statistical design. The two independent variables such as HPMC K4M and PEG 400 are the film-forming polymers which are evaluated at three levels. The dependent variables selected as folding endurance, disintegration time, and % drug release. The formulation was prepared and optimized the batch F-4 showed the least disintegration time (19 s) and the highest drug release (98.55±7.90%). Moreover, the ex-vivo mucus permeation study showed better permeation and satisfying physicochemical properties. As per the above results, we conclude that the prepared formulation could be a novel dosage form to improve drug delivery and patient compliance.
{"title":"Central Composite Design for the Development of Trimetazidine Dihydrochloride-Loaded Fast Dissolving Film","authors":"Sw Chopade","doi":"10.55262/fabadeczacilik.1085351","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1085351","url":null,"abstract":"A fast-dissolving dosage form is an approach used to improve therapeutic efficacy and bioavailability by avoiding the first-pass metabolism of the cargo. Besides, the approach causes rapid cargo absorption from the pre-gastric area which may outcome in the quick inception of action. The trimetazidine dihydrochloride (TDC) is an anti-anginal drug and there is a prerequisite to provide fast onset of action to treat angina. Therefore, the present work was aimed to prepare and evaluate fast-dissolving oral films (FDOF) of TDC to provide fast onset of action. The FDOF is prepared by using the solvent casting method and it was optimized by employing a central composite statistical design. The two independent variables such as HPMC K4M and PEG 400 are the film-forming polymers which are evaluated at three levels. The dependent variables selected as folding endurance, disintegration time, and % drug release. The formulation was prepared and optimized the batch F-4 showed the least disintegration time (19 s) and the highest drug release (98.55±7.90%). Moreover, the ex-vivo mucus permeation study showed better permeation and satisfying physicochemical properties. As per the above results, we conclude that the prepared formulation could be a novel dosage form to improve drug delivery and patient compliance.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-11-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77309508","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 : 2022-10-25DOI: 10.55262/fabadeczacilik.1099539
Shabnam Nazir, Hina Raza, Memoona Nisar, Zermina Rashid, Rahat Shamim, B. Alam, Amjad Khan
The aim of present study is to assess anxiety and depression experienced by unpaid caregivers of chronic haemodialysis patients suffering from end-stage renal failure (ESRF). The evaluation of factors influencing anxiety and depression and care-giving burden was performed. In the present study, non-paid primary caregivers (218 study participants) of patients with ESRF receiving haemodialysis, who were providing care (minimum 6 months and up to 5 years) were interviewed by using Aga Khan University Anxiety and Depression Scale (AKUADS) and the carer’s burden of peritoneal dialysis patients (CSCDP) questionnaire. According to the scoring of AKUADS, 90.4% caregivers were found to be experiencing significant anxiety and depression. From assessment of demographic factors collected using the AKUAD scale, it was found that female gender was more in number (44%), wedded (72.01%), with a mean life span of 38.5 ± 2 (SE) years, and having monthly income below average. The main relationships of caregivers with patients, was life partners (38%) and parents (18.2%). The highest depression levels were found in mothers as attendants (67%), caregivers of age less than 30 years (22 %) and caregivers of elderly patients (87%). The outcome of this study has revealed a need to plan policies to support unpaid caregivers as well as the patients
{"title":"Assessment of Anxiety and Burden on caregivers for haemodialysis patients in southern Punjab, Pakistan","authors":"Shabnam Nazir, Hina Raza, Memoona Nisar, Zermina Rashid, Rahat Shamim, B. Alam, Amjad Khan","doi":"10.55262/fabadeczacilik.1099539","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1099539","url":null,"abstract":"The aim of present study is to assess anxiety and depression experienced by unpaid caregivers of chronic haemodialysis patients suffering from end-stage renal failure (ESRF). The evaluation of factors influencing anxiety and depression and care-giving burden was performed. In the present study, non-paid primary caregivers (218 study participants) of patients with ESRF receiving haemodialysis, who were providing care (minimum 6 months and up to 5 years) were interviewed by using Aga Khan University Anxiety and Depression Scale (AKUADS) and the carer’s burden of peritoneal dialysis patients (CSCDP) questionnaire. According to the scoring of AKUADS, 90.4% caregivers were found to be experiencing significant anxiety and depression. From assessment of demographic factors collected using the AKUAD scale, it was found that female gender was more in number (44%), wedded (72.01%), with a mean life span of 38.5 ± 2 (SE) years, and having monthly income below average. The main relationships of caregivers with patients, was life partners (38%) and parents (18.2%). The highest depression levels were found in mothers as attendants (67%), caregivers of age less than 30 years (22 %) and caregivers of elderly patients (87%). The outcome of this study has revealed a need to plan policies to support unpaid caregivers as well as the patients","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73412060","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 : 2022-10-17DOI: 10.55262/fabadeczacilik.1145208
P. Kumbhar, V. Khade, Varsha Khadake, Pradnya Marale, A. Manjappa, S. Nadaf, V. Kumbar, D. Bhagwat, J. Disouza
Background: Ifosfamide (IFS) is proved efficacious against breast cancer, an enormously diagnosed cancer across the globe. However, the clinical efficacy of IFS is limited owing to its hydrophilicity, less stability, and dose-dependent toxicities. Therefore, the primary goal of the present research was to develop IFS-loaded cubosomes with improved anticancer efficacy and reduced dose-dependent toxicities. Methods: The IFS-cubosomes were optimized using a 32 factorial design based on IFS content and zeta potential. The optimized cubosomal dispersion was further assessed for particle size, in vitro IFS release, haemolysis, cytotoxicity, cellular uptake and physical stability. Results: The optimized IFS-cubosomal dispersion exhibited maximum IFS content (89.75±4.3%) and better zeta potential value (-40.0±1.6 mV), and size in nanometer. Moreover, IFS-cubosomes retarded IFS release (about 91 %) after 12 h than plain IFS solution (>99 % within 2 h). The IFS-cubosomes displayed lower haemolysis (3.7±0.79%) towards human RBCs. Besides, the in vitro cytotoxicity of IFS-cubosomes was noticed to be substantially higher (IC50: 0.64±0.08 µM) than plain IFS solution (IC50: 1.46±0.21 µM) against multi-drug resistant (MDR) breast cancer (MDA-MB-231) cells. DAPI staining revealed death of IFS-cubosomes treated cells mainly by apoptosis. The cubosomes showed increased uptake by cancer cells. Furthermore, IFS-cubosomes were found to be more stable at refrigeration temperature than at room temperature. Conclusion: Thus, IFS-cubosomes could be a novel avenue in the treatment of breast cancer with improved anticancer efficacy and reduced toxicity. However, further in vivo investigations are desired to validate these claims.
{"title":"Ifosfamide-Loaded Cubosomes: An Approach to Potentiate Cytotoxicity against MDA-MB-231 Breast Cancer Cells","authors":"P. Kumbhar, V. Khade, Varsha Khadake, Pradnya Marale, A. Manjappa, S. Nadaf, V. Kumbar, D. Bhagwat, J. Disouza","doi":"10.55262/fabadeczacilik.1145208","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1145208","url":null,"abstract":"Background: Ifosfamide (IFS) is proved efficacious against breast cancer, an enormously diagnosed cancer across the globe. However, the clinical efficacy of IFS is limited owing to its hydrophilicity, less stability, and dose-dependent toxicities. Therefore, the primary goal of the present research was to develop IFS-loaded cubosomes with improved anticancer efficacy and reduced dose-dependent toxicities. \u0000Methods: The IFS-cubosomes were optimized using a 32 factorial design based on IFS content and zeta potential. The optimized cubosomal dispersion was further assessed for particle size, in vitro IFS release, haemolysis, cytotoxicity, cellular uptake and physical stability. \u0000Results: The optimized IFS-cubosomal dispersion exhibited maximum IFS content (89.75±4.3%) and better zeta potential value (-40.0±1.6 mV), and size in nanometer. Moreover, IFS-cubosomes retarded IFS release (about 91 %) after 12 h than plain IFS solution (>99 % within 2 h). The IFS-cubosomes displayed lower haemolysis (3.7±0.79%) towards human RBCs. Besides, the in vitro cytotoxicity of IFS-cubosomes was noticed to be substantially higher (IC50: 0.64±0.08 µM) than plain IFS solution (IC50: 1.46±0.21 µM) against multi-drug resistant (MDR) breast cancer (MDA-MB-231) cells. DAPI staining revealed death of IFS-cubosomes treated cells mainly by apoptosis. The cubosomes showed increased uptake by cancer cells. Furthermore, IFS-cubosomes were found to be more stable at refrigeration temperature than at room temperature. \u0000Conclusion: Thus, IFS-cubosomes could be a novel avenue in the treatment of breast cancer with improved anticancer efficacy and reduced toxicity. However, further in vivo investigations are desired to validate these claims.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87102758","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 : 2022-09-26DOI: 10.55262/fabadeczacilik.1103532
F. Yerlikaya, Aslıhan Arslan, Özlem Ati̇k, Seda Kozan, Ahmet Parlak, Meltem ÖZEL KARATAŞ, Onur Saglam, S. P. Aytaç
A new oral formulation of cefdinir, Cefdinir 600 mg Tablets has been developed and in this study, its relative bioavailability has been compared with another oral solid dosage form, Cefdinir 300 mg Capsules, which is already on the market. An open-label, randomized, two-period, cross-over relative bioavailability study has been conducted with healthy males under fasting conditions in compliance with Good Clinical Practice (GCP) principles. A single dose of the novel tablet formulation of 600 mg cefdinir has been compared to two doses of Cefdinir 300 mg Capsules (two capsules at once) in terms of their pharmacokinetic properties. The comparison study was performed as a single-center clinical study, and blood samples of the participants were withdrawn at specified time points, before and after dosing. The plasma concentrations and pharmacokinetic properties of two cefdinir formulations were assessed from the collected samples by using a validated LC-MS/MS analytical method. The relative bioavailability of the new formulation has been shown and both products were introduced as safe.
{"title":"The Relative Bioavailability Study of Two Cefdinir Formulations in Healthy Males Under Fasting Conditions","authors":"F. Yerlikaya, Aslıhan Arslan, Özlem Ati̇k, Seda Kozan, Ahmet Parlak, Meltem ÖZEL KARATAŞ, Onur Saglam, S. P. Aytaç","doi":"10.55262/fabadeczacilik.1103532","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1103532","url":null,"abstract":"A new oral formulation of cefdinir, Cefdinir 600 mg Tablets has been developed and in this study, its relative bioavailability has been compared with another oral solid dosage form, Cefdinir 300 mg Capsules, which is already on the market. An open-label, randomized, two-period, cross-over relative bioavailability study has been conducted with healthy males under fasting conditions in compliance with Good Clinical Practice (GCP) principles. A single dose of the novel tablet formulation of 600 mg cefdinir has been compared to two doses of Cefdinir 300 mg Capsules (two capsules at once) in terms of their pharmacokinetic properties. The comparison study was performed as a single-center clinical study, and blood samples of the participants were withdrawn at specified time points, before and after dosing. The plasma concentrations and pharmacokinetic properties of two cefdinir formulations were assessed from the collected samples by using a validated LC-MS/MS analytical method. The relative bioavailability of the new formulation has been shown and both products were introduced as safe.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75045933","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 : 2022-08-25DOI: 10.55262/fabadeczacilik.1147174
Ayşe ÇİÇEK KAYA, H. Özbek, H. Yuca, G. Yılmaz, Zeynebe Bi̇ngöl, C. Kazaz, I. Gülçin, Z. Güvenalp
Alzheimer's disease (AD) is characterized by progressive memory loss, deterioration of other cognitive functions, and inability to perform activities of daily living. Inhibiting the AChE enzyme causes Ach accumulation in cholinergic synapses and is expected to increase cognitive functions. Carbonic anhydrase enzymes (CAs) are ubiquitous in all living organisms. They have crucial physiological and pathological roles. CA inhibitors bind to catalytic zinc ion in the active site of CA isoenzymes and block their activity. The clinical use of CAIs had been established as antiglaucoma, anticonvulsant agents, diuretics, and anti-obesity drugs, in the management of mountain sickness, gastric and duodenal ulcers, neurological disorders, osteoporosis, and tumors. To evaluate the bioactive profile of dichloromethane extract prepared from Heptaptera triquetra root, isolation studies, AChE, and hCA I and II inhibitory activities were performed. According to isolation studies, one fatty acid, coniferyl palmitate (1); four sesquiterpene coumarins, umbelliprenin (2), badrakemin acetate (4), colladonin (5), karatavicinol (6); and two sterols, stigmasterol (3a), β-sitosterol (3b) were isolated. The dichloromethane extract and all isolated compounds showed high potency against all enzymes (except badrakemin acetate for AChE) when compared to standards. Umbelliprenin (2) with IC50 value of 31.500 nM against hCA I, colladonin (5) with IC50 value of 36.473 nM against hCA II and stigmasterol (3a), and β-sitosterol (3b) mixture with IC50 value 9.000 nM against AChE demonstrated the best activity.
{"title":"Phytochemical Analysis and Screening of Acetylcholinesterase and Carbonic Anhydrase I and II Isoenzymes Inhibitory Effect of Heptaptera triquetra (Vent.) Tutin Root","authors":"Ayşe ÇİÇEK KAYA, H. Özbek, H. Yuca, G. Yılmaz, Zeynebe Bi̇ngöl, C. Kazaz, I. Gülçin, Z. Güvenalp","doi":"10.55262/fabadeczacilik.1147174","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1147174","url":null,"abstract":"Alzheimer's disease (AD) is characterized by progressive memory loss, deterioration of other cognitive functions, and inability to perform activities of daily living. Inhibiting the AChE enzyme causes Ach accumulation in cholinergic synapses and is expected to increase cognitive functions. Carbonic anhydrase enzymes (CAs) are ubiquitous in all living organisms. They have crucial physiological and pathological roles. CA inhibitors bind to catalytic zinc ion in the active site of CA isoenzymes and block their activity. The clinical use of CAIs had been established as antiglaucoma, anticonvulsant agents, diuretics, and anti-obesity drugs, in the management of mountain sickness, gastric and duodenal ulcers, neurological disorders, osteoporosis, and tumors. To evaluate the bioactive profile of dichloromethane extract prepared from Heptaptera triquetra root, isolation studies, AChE, and hCA I and II inhibitory activities were performed. According to isolation studies, one fatty acid, coniferyl palmitate (1); four sesquiterpene coumarins, umbelliprenin (2), badrakemin acetate (4), colladonin (5), karatavicinol (6); and two sterols, stigmasterol (3a), β-sitosterol (3b) were isolated. The dichloromethane extract and all isolated compounds showed high potency against all enzymes (except badrakemin acetate for AChE) when compared to standards. Umbelliprenin (2) with IC50 value of 31.500 nM against hCA I, colladonin (5) with IC50 value of 36.473 nM against hCA II and stigmasterol (3a), and β-sitosterol (3b) mixture with IC50 value 9.000 nM against AChE demonstrated the best activity.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81886844","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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