Ivana Pantelić, Tanja Ilić, Ines Nikolić, Snežana Savić
A review of recent publications reveals an increased interest in the so-called self-assembled carriers and their applicability in drug delivery via various routes of administration. Self-assembly denotes the process of rather spontaneous formation of ordered aggregates (sometimes under specific conditions-e.g., pH, temperature, ionic strength), via diverse interactions. This process, seen in many naturally occurring substances (polysaccharides, proteins, lipids), has inspired researchers to synthetize innovative self-assembling materials or combinations of existing ones. This paper provides a review of the recently investigated self-assembling materials and the carriers they form, often belonging to the sphere of pharmaceutical nanotechnology. Self-assembled carriers may provide enhanced stability, more efficient encapsulation and/or controlled delivery of active pharmaceutical ingredients. However, the diversity of geometries obtained (spheres, polyhedrals, ellipses, discs, porous structures, etc.) presents a significant characterization challenge, often requiring the application of several complementary techniques for proper evaluation of carrier size and morphology. Commonly utilized characterization techniques for investigating physico-chemical and certain biopharmaceutical properties are discussed, along with their advantages and disadvantages. Finally, the authors offer their critical opinion on the outlook of self-assembled drug carriers.
{"title":"Self-assembled carriers as drug delivery systems: Current characterization challenges and future prospects","authors":"Ivana Pantelić, Tanja Ilić, Ines Nikolić, Snežana Savić","doi":"10.5937/arhfarm73-46975","DOIUrl":"https://doi.org/10.5937/arhfarm73-46975","url":null,"abstract":"A review of recent publications reveals an increased interest in the so-called self-assembled carriers and their applicability in drug delivery via various routes of administration. Self-assembly denotes the process of rather spontaneous formation of ordered aggregates (sometimes under specific conditions-e.g., pH, temperature, ionic strength), via diverse interactions. This process, seen in many naturally occurring substances (polysaccharides, proteins, lipids), has inspired researchers to synthetize innovative self-assembling materials or combinations of existing ones. This paper provides a review of the recently investigated self-assembling materials and the carriers they form, often belonging to the sphere of pharmaceutical nanotechnology. Self-assembled carriers may provide enhanced stability, more efficient encapsulation and/or controlled delivery of active pharmaceutical ingredients. However, the diversity of geometries obtained (spheres, polyhedrals, ellipses, discs, porous structures, etc.) presents a significant characterization challenge, often requiring the application of several complementary techniques for proper evaluation of carrier size and morphology. Commonly utilized characterization techniques for investigating physico-chemical and certain biopharmaceutical properties are discussed, along with their advantages and disadvantages. Finally, the authors offer their critical opinion on the outlook of self-assembled drug carriers.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134982050","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}
Silvia García-Hernández, M. Monserrat-Mesquida, Josep A Tur, C. Bouzas
The Mediterranean Diet (MedDiet) is characterized by a high intake of fruit, vegetables, whole grains, legumes, and olive oil, moderate consumption of poultry and fish, and a limited intake of red meat and minimal processed foods. It has been associated with many health benefits, including the prevention and management of metabolic syndrome, diabetes, cardiovascular disease, neurodegenerative diseases, and certain types of cancer, as well as increased longevity and reduced risk of mortality. The protective effects of the MedDiet are related to its antioxidant and anti-inflammatory properties. The MedDiet is not only a health-promoting dietary pattern, but it is also environmentally sustainable, showing a negative correlation with greenhouse gas emissions, among other environmental indicators. In addition to the MedDiet, the Mediterranean lifestyle, which involves regular physical activity, adequate rest, and socializing during meals, has also been linked to beneficial health outcomes. Preventive strategies for noncommunicable diseases should focus on promoting the Mediterranean lifestyle and implementing early detection and prevention programs, at both individual and social levels.
{"title":"The Mediterranean diet and lifestyle","authors":"Silvia García-Hernández, M. Monserrat-Mesquida, Josep A Tur, C. Bouzas","doi":"10.5937/arhfarm73-45492","DOIUrl":"https://doi.org/10.5937/arhfarm73-45492","url":null,"abstract":"The Mediterranean Diet (MedDiet) is characterized by a high intake of fruit, vegetables, whole grains, legumes, and olive oil, moderate consumption of poultry and fish, and a limited intake of red meat and minimal processed foods. It has been associated with many health benefits, including the prevention and management of metabolic syndrome, diabetes, cardiovascular disease, neurodegenerative diseases, and certain types of cancer, as well as increased longevity and reduced risk of mortality. The protective effects of the MedDiet are related to its antioxidant and anti-inflammatory properties. The MedDiet is not only a health-promoting dietary pattern, but it is also environmentally sustainable, showing a negative correlation with greenhouse gas emissions, among other environmental indicators. In addition to the MedDiet, the Mediterranean lifestyle, which involves regular physical activity, adequate rest, and socializing during meals, has also been linked to beneficial health outcomes. Preventive strategies for noncommunicable diseases should focus on promoting the Mediterranean lifestyle and implementing early detection and prevention programs, at both individual and social levels.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199446","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}
Jevrem Stojanović, Jovana Krmar, Biljana Otašević, A. Protić
High-pressure liquid chromatography (HPLC) is a technique of paramount importance in the analysis of pharmaceuticals because of its ability to separate moderately polar to less polar compounds, such as drugs and related substances.High-pressure liquid chromatography (HPLC) is a technique of paramount importance in the analysis of pharmaceuticals because of its ability to separate moderately polar to less polar compounds, such as drugs and related substances. The concept of green analytical chemistry (GAC) aims to provide more environmentally friendly and safer analytical methods in terms of reagents, energy, and waste. One of the major challenges of GAC is to find an appropriate approach to evaluate the greenness of analytical methods. An extension of GAC, called white analytical chemistry (WAC), has been introduced to consider not only environmental friendliness, but also other aspects that contribute to the sustainability of methods, such as analytical and economic or practical efficiency. HPLC methods are intrinsically not green, due to the high consumption of toxic organic solvents and the resulting generation of large amounts of toxic waste. Fortunately, there are many approaches to overcome the non-green character of HPLC methods. In this article, various modifications of the HPLC methods that increase its environmental friendliness are presented, as well as the various tools used to evaluate environmental friendliness. In addition, the new concept of white analytical chemistry is presented.
{"title":"Resource management in HPLC: Unveiling a green face of pharmaceutical analysis","authors":"Jevrem Stojanović, Jovana Krmar, Biljana Otašević, A. Protić","doi":"10.5937/arhfarm73-43479","DOIUrl":"https://doi.org/10.5937/arhfarm73-43479","url":null,"abstract":"High-pressure liquid chromatography (HPLC) is a technique of paramount importance in the analysis of pharmaceuticals because of its ability to separate moderately polar to less polar compounds, such as drugs and related substances.High-pressure liquid chromatography (HPLC) is a technique of paramount importance in the analysis of pharmaceuticals because of its ability to separate moderately polar to less polar compounds, such as drugs and related substances. The concept of green analytical chemistry (GAC) aims to provide more environmentally friendly and safer analytical methods in terms of reagents, energy, and waste. One of the major challenges of GAC is to find an appropriate approach to evaluate the greenness of analytical methods. An extension of GAC, called white analytical chemistry (WAC), has been introduced to consider not only environmental friendliness, but also other aspects that contribute to the sustainability of methods, such as analytical and economic or practical efficiency. HPLC methods are intrinsically not green, due to the high consumption of toxic organic solvents and the resulting generation of large amounts of toxic waste. Fortunately, there are many approaches to overcome the non-green character of HPLC methods. In this article, various modifications of the HPLC methods that increase its environmental friendliness are presented, as well as the various tools used to evaluate environmental friendliness. In addition, the new concept of white analytical chemistry is presented.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199735","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 assessment of stability in emulsion-based topical preparations can be approached through real-time monitoring and/or accelerated methods, drawing predictions from pertinent stability-related physicochemical parameters. Ensuring the robustness and durability of topical products during storage, transport, and application necessitates thorough stability testing. However, due to the diversity of emulsion types and their intended use, there is no universal standard test, placing the liability on formulators/manufacturer to tailor appropriate assessments. Notably, topical emulsions, particularly cosmetic variants, often exhibit impressive stability with extended shelf lives. Nonetheless, evaluating their stability and decision-making remain challenging and time-consuming in industrial contexts. This underscores the demand for alternative testing protocols that expedite stability assessments and predict emulsion-based product stability accurately. This article comprehensively surveys literature, enriched with practical insights, exploring core mechanisms behind emulsion stability and prevention of instability. The discussion encompasses diverse approaches to stability assessment, revealing methodologies and parameters under examination during testing. Particular focus is placed on the dynamic-mechanical thermoanalysis (DMTA) method explored as a rapid, rheologically-based alternative to the conventional freeze-thaw test, emphasizing its usefulness for expediting the stability evaluation of emulsion-based topical preparations.
{"title":"Stability evaluation of emulsion-based topical preparations: A valuable potential of dynamicmechanical thermoanalysis (DMTA) test as a rapid rheological alternative to conventional freezethaw test","authors":"Nebojša Cekić, Sanela Savić, Snežana Savić","doi":"10.5937/arhfarm73-46319","DOIUrl":"https://doi.org/10.5937/arhfarm73-46319","url":null,"abstract":"The assessment of stability in emulsion-based topical preparations can be approached through real-time monitoring and/or accelerated methods, drawing predictions from pertinent stability-related physicochemical parameters. Ensuring the robustness and durability of topical products during storage, transport, and application necessitates thorough stability testing. However, due to the diversity of emulsion types and their intended use, there is no universal standard test, placing the liability on formulators/manufacturer to tailor appropriate assessments. Notably, topical emulsions, particularly cosmetic variants, often exhibit impressive stability with extended shelf lives. Nonetheless, evaluating their stability and decision-making remain challenging and time-consuming in industrial contexts. This underscores the demand for alternative testing protocols that expedite stability assessments and predict emulsion-based product stability accurately. This article comprehensively surveys literature, enriched with practical insights, exploring core mechanisms behind emulsion stability and prevention of instability. The discussion encompasses diverse approaches to stability assessment, revealing methodologies and parameters under examination during testing. Particular focus is placed on the dynamic-mechanical thermoanalysis (DMTA) method explored as a rapid, rheologically-based alternative to the conventional freeze-thaw test, emphasizing its usefulness for expediting the stability evaluation of emulsion-based topical preparations.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134981813","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}
Anđela Tošić, Tijana Stankovic, T. Ilić, S. Savić, I. Pantelić
Tribology investigates the events that happen on the surfaces of two substances/objects that are in direct or indirect contact through assessing friction, lubrication and/or wear. In particular, friction measurements could provide the information on the textural characteristics of (per)oral pharmaceutical preparations and contribute to the understanding of palatability. On the other hand, tribological tests have been more intensively used to characterize topical preparations (pharmaceutical, cosmetic), giving a thorough insight into the tactile and texture properties of these preparations. However, these tests are often combined with rheological, textural, and certain biophysical approaches. Additionally, the materials used for constructing artificial joints and articular cartilages are true tribological systems, developed and optimized in order to have properties that resemble the natural ones. Since tribological studies can be used to assess a wide range of drug dosage forms and products in general, the equipment used may be quite diverse. Accordingly, a special section of this work is committed to the description of the testing equipment's specifications and the applied protocols. The investigation of recently regulatory discovered phenomena, such as transformation/metamorphosis of the vehicle/base of topical preparations, have brought tribology back into focus as a potential assessment method.
{"title":"Current role of tribological tests: Striving for full characterization of medicinal and cosmetic products","authors":"Anđela Tošić, Tijana Stankovic, T. Ilić, S. Savić, I. Pantelić","doi":"10.5937/arhfarm73-43515","DOIUrl":"https://doi.org/10.5937/arhfarm73-43515","url":null,"abstract":"Tribology investigates the events that happen on the surfaces of two substances/objects that are in direct or indirect contact through assessing friction, lubrication and/or wear. In particular, friction measurements could provide the information on the textural characteristics of (per)oral pharmaceutical preparations and contribute to the understanding of palatability. On the other hand, tribological tests have been more intensively used to characterize topical preparations (pharmaceutical, cosmetic), giving a thorough insight into the tactile and texture properties of these preparations. However, these tests are often combined with rheological, textural, and certain biophysical approaches. Additionally, the materials used for constructing artificial joints and articular cartilages are true tribological systems, developed and optimized in order to have properties that resemble the natural ones. Since tribological studies can be used to assess a wide range of drug dosage forms and products in general, the equipment used may be quite diverse. Accordingly, a special section of this work is committed to the description of the testing equipment's specifications and the applied protocols. The investigation of recently regulatory discovered phenomena, such as transformation/metamorphosis of the vehicle/base of topical preparations, have brought tribology back into focus as a potential assessment method.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199875","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}
Thyroid function disorders are the most common endocrine disorders in humans. They are frequently diagnosed, with prevalence varying between 2 and 6%, and a female to male ratio of up to 10:1. Disorders of thyroid function in the narrower sense are presented by its hyperactivity or underactivity, although there are conditions that lead to an increased concentration of thyroid hormones, without its increased activity. In iodine-sufficient regions, the most common cause of hyperthyroidism, as well as hypothyroidism, is an autoimmune disease of the thyroid. For hyperthyroidism, it is Graves' disease, with typical symptoms and signs of hypermetabolism. The diagnosis of hyperthyroidism is based on suppressed TSH and elevated fT4 (free, and in the differential diagnosis, elevated TSH-receptor-antibodies are crucial for Graves' disease. Management of Graves' disease relies on three equally potent approaches: medical therapy, ablative treatments with 131I-radiotherapy-RAI, and thyroidectomy. Hashimoto's thyroiditis is the most common cause of hypothyroidism in iodine-sufficient regions. Symptoms and signs of hypothyroidism are non-specific and correspond to the symptoms and signs of hypometabolism. The diagnosis is made based on elevated TSH with decreased fT4. Thyroxine-peroxidaseantibodies and thyroglobuline-antibodies are important in differential diagnosis. Sometimes elevated TRAb is found in Hashimoto's thyroiditis. The treatment of hypothyroidism is levothyroxine replacement therapy.
{"title":"Thyroid function disorders","authors":"M. Stojković","doi":"10.5937/arhfarm72-39952","DOIUrl":"https://doi.org/10.5937/arhfarm72-39952","url":null,"abstract":"Thyroid function disorders are the most common endocrine disorders in humans. They are frequently diagnosed, with prevalence varying between 2 and 6%, and a female to male ratio of up to 10:1. Disorders of thyroid function in the narrower sense are presented by its hyperactivity or underactivity, although there are conditions that lead to an increased concentration of thyroid hormones, without its increased activity. In iodine-sufficient regions, the most common cause of hyperthyroidism, as well as hypothyroidism, is an autoimmune disease of the thyroid. For hyperthyroidism, it is Graves' disease, with typical symptoms and signs of hypermetabolism. The diagnosis of hyperthyroidism is based on suppressed TSH and elevated fT4 (free, and in the differential diagnosis, elevated TSH-receptor-antibodies are crucial for Graves' disease. Management of Graves' disease relies on three equally potent approaches: medical therapy, ablative treatments with 131I-radiotherapy-RAI, and thyroidectomy. Hashimoto's thyroiditis is the most common cause of hypothyroidism in iodine-sufficient regions. Symptoms and signs of hypothyroidism are non-specific and correspond to the symptoms and signs of hypometabolism. The diagnosis is made based on elevated TSH with decreased fT4. Thyroxine-peroxidaseantibodies and thyroglobuline-antibodies are important in differential diagnosis. Sometimes elevated TRAb is found in Hashimoto's thyroiditis. The treatment of hypothyroidism is levothyroxine replacement therapy.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199194","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}
Dušan Vukmirović, I. Stević, M. Odalović, Dušanka M. Krajnović
The number of software - mobile applications intended for use in the field of people's health and well-being is constantly increasing. The aim of this review is to compare regulations on software - mobile applications as medical devices in the United States of America (USA), European Union (EU) and Serbia, with reference on the efforts for international harmonization of the regulations. The goal is to increase awareness of the broader healthcare professionals' (HCPs) audience about this topic. Publicly available information from official regulatory bodies websites was analyzed and synthesized for two regions and one country of interest. The results show differences in regulatory approaches in this area between two biggest medical device markets - the USA and the EU, while regulations in Serbia are being harmonized with the EU. Regulations clearly define criteria that software - mobile application needs to meet to be assessed as a medical device; on the other hand, they leave a number of applications that provide health-related services out of the regulated scope. Based on the increased awareness of regulations, recommendations for future research can be directed towards greater involvement of HCPs in patient counseling and decision making regarding the selection of mobile applications, to prevent the use of inadequate mobile applications and ensure that their patients are correctly using the right applications with positive effects on health and well-being.
{"title":"Review of regulatory requirements in the US, EU and Serbia on software: Mobile application as a medical device: State of the art","authors":"Dušan Vukmirović, I. Stević, M. Odalović, Dušanka M. Krajnović","doi":"10.5937/arhfarm72-36730","DOIUrl":"https://doi.org/10.5937/arhfarm72-36730","url":null,"abstract":"The number of software - mobile applications intended for use in the field of people's health and well-being is constantly increasing. The aim of this review is to compare regulations on software - mobile applications as medical devices in the United States of America (USA), European Union (EU) and Serbia, with reference on the efforts for international harmonization of the regulations. The goal is to increase awareness of the broader healthcare professionals' (HCPs) audience about this topic. Publicly available information from official regulatory bodies websites was analyzed and synthesized for two regions and one country of interest. The results show differences in regulatory approaches in this area between two biggest medical device markets - the USA and the EU, while regulations in Serbia are being harmonized with the EU. Regulations clearly define criteria that software - mobile application needs to meet to be assessed as a medical device; on the other hand, they leave a number of applications that provide health-related services out of the regulated scope. Based on the increased awareness of regulations, recommendations for future research can be directed towards greater involvement of HCPs in patient counseling and decision making regarding the selection of mobile applications, to prevent the use of inadequate mobile applications and ensure that their patients are correctly using the right applications with positive effects on health and well-being.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199325","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}
A. Ćirić, Jelena Milinković-Budinčić, Đorđe Medarević, V. Dobričić, Milena Rmandić, T. Barudžija, A. Malenović, Lidija Petrović, Ljiljana Đekić
Polyelectrolyte complexes (PECs) are attractive carriers with recognized potential to enhance oral delivery of poorly soluble high-dosed low-molecular-weight drugs. The formulation of solid oral dosage forms requires the drying of PECs, which may affect their physicochemical and biopharmaceutical properties. The aim of this study was to investigate the effect of spraydrying on the properties of ibuprofen-loaded chitosan/xanthan gum PECs and to assess the drug release kinetics from such PECs filled into hard capsules in comparison with corresponding PECs which are dried under ambient conditions. The yield, ibuprofen content, entrapment efficiency, and residual moisture content of spray-dried PECs were lower than those of ambient-dried PECs. Better flowability of spray-dried PECs was attributed to the almost spherical particle shape, shown by scanning electron microscopy. DSC and PXRD analysis confirmed the amorphization of ibuprofen during spray-drying. All the investigated PECs, obtained by drying under ambient conditions as well as by spray-drying, had high rehydration capacity both in 0.1 M hydrochloric acid (pH 1.2) and phosphate buffer pH 7.4. In vitro ibuprofen release from dried PECs was controlled during 12 h with the release of approximately 30% of entrapped ibuprofen. Spray-dried PECs provided better control of ibuprofen diffusion from the carrier compared to the ambientdried ones.
{"title":"Influence of spray-drying process on properties of chitosan/xanthan gum polyelectrolyte complexes as carriers for oral delivery of ibuprofen","authors":"A. Ćirić, Jelena Milinković-Budinčić, Đorđe Medarević, V. Dobričić, Milena Rmandić, T. Barudžija, A. Malenović, Lidija Petrović, Ljiljana Đekić","doi":"10.5937/arhfarm72-35133","DOIUrl":"https://doi.org/10.5937/arhfarm72-35133","url":null,"abstract":"Polyelectrolyte complexes (PECs) are attractive carriers with recognized potential to enhance oral delivery of poorly soluble high-dosed low-molecular-weight drugs. The formulation of solid oral dosage forms requires the drying of PECs, which may affect their physicochemical and biopharmaceutical properties. The aim of this study was to investigate the effect of spraydrying on the properties of ibuprofen-loaded chitosan/xanthan gum PECs and to assess the drug release kinetics from such PECs filled into hard capsules in comparison with corresponding PECs which are dried under ambient conditions. The yield, ibuprofen content, entrapment efficiency, and residual moisture content of spray-dried PECs were lower than those of ambient-dried PECs. Better flowability of spray-dried PECs was attributed to the almost spherical particle shape, shown by scanning electron microscopy. DSC and PXRD analysis confirmed the amorphization of ibuprofen during spray-drying. All the investigated PECs, obtained by drying under ambient conditions as well as by spray-drying, had high rehydration capacity both in 0.1 M hydrochloric acid (pH 1.2) and phosphate buffer pH 7.4. In vitro ibuprofen release from dried PECs was controlled during 12 h with the release of approximately 30% of entrapped ibuprofen. Spray-dried PECs provided better control of ibuprofen diffusion from the carrier compared to the ambientdried ones.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199364","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}
B. Ivković, D. Opačić, B. Dzudovic, Milkica Crevar, L. Gojković-Bukarica
It is well known that the presence of different chemical groups in drug molecules influences their pharmacological properties. The aim of our study is to investigate whether newly synthesized derivatives of propafenone, with changes in benzyl moiety, have a different effect upon arrhythmia, compared to propafenone. 5OCl-PF and 5OF-PF are derivatives of propafenone with -Cl or -F substituent on the ortho position of the benzyl moiety. For verification of their antiarrhythmic effect, we used an in vivo rat model of aconitine-induced arrhythmia. 5OCl-PF speeded the appearance of supraventricular premature beats (SVPB) and death more than aconitine. All animals treated with 5OCl-PF developed ventricular premature beats in salvos (VPBS), bigeminies (VPBB) and paroxysmal ventricular tachycardia (PVT). 5OF-PF had a negative chronotropic effect and potentiated atrial excitability (more SVPB). It had a positive effect on the occurrence and onset time of supraventricular tachycardia, VPBS, and PVT. Based on the obtained results, it can be concluded that newly synthesized propafenone derivatives have no better antiarrhythmic effect than the parent compound. In the future, our research will be focused on the synthesis of different derivatives and examining their antiarrhythmic effects.
{"title":"Antiarrhythmic effects of newly developed propafenone derivatives","authors":"B. Ivković, D. Opačić, B. Dzudovic, Milkica Crevar, L. Gojković-Bukarica","doi":"10.5937/arhfarm72-37114","DOIUrl":"https://doi.org/10.5937/arhfarm72-37114","url":null,"abstract":"It is well known that the presence of different chemical groups in drug molecules influences their pharmacological properties. The aim of our study is to investigate whether newly synthesized derivatives of propafenone, with changes in benzyl moiety, have a different effect upon arrhythmia, compared to propafenone. 5OCl-PF and 5OF-PF are derivatives of propafenone with -Cl or -F substituent on the ortho position of the benzyl moiety. For verification of their antiarrhythmic effect, we used an in vivo rat model of aconitine-induced arrhythmia. 5OCl-PF speeded the appearance of supraventricular premature beats (SVPB) and death more than aconitine. All animals treated with 5OCl-PF developed ventricular premature beats in salvos (VPBS), bigeminies (VPBB) and paroxysmal ventricular tachycardia (PVT). 5OF-PF had a negative chronotropic effect and potentiated atrial excitability (more SVPB). It had a positive effect on the occurrence and onset time of supraventricular tachycardia, VPBS, and PVT. Based on the obtained results, it can be concluded that newly synthesized propafenone derivatives have no better antiarrhythmic effect than the parent compound. In the future, our research will be focused on the synthesis of different derivatives and examining their antiarrhythmic effects.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71198905","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}
E. Almuradova, Durr-e-shahwar Malik, Sara Yousaf, A. Farooqi
Loss of apoptosis results in the survival and uncontrolled proliferation of cancer cells. Basic and clinical researchers have dissected myriads of central regulators of apoptosis. Second mitochondria-derived activator of caspases (SMAC)/ direct inhibitor of apoptosis protein (IAP)-binding protein with low pI (DIABLO) has attracted phenomenal attention because of its amazing ability to trigger apoptotic death. Accordingly, different teams of interdisciplinary researchers are working on the design and development of SMAC mimetics which can significantly inhibit primary and secondary tumor growth.
{"title":"Overview of the progress and prospects of SMAC mimetics in cancers: Is it a silver bullet?","authors":"E. Almuradova, Durr-e-shahwar Malik, Sara Yousaf, A. Farooqi","doi":"10.5937/arhfarm72-39318","DOIUrl":"https://doi.org/10.5937/arhfarm72-39318","url":null,"abstract":"Loss of apoptosis results in the survival and uncontrolled proliferation of cancer cells. Basic and clinical researchers have dissected myriads of central regulators of apoptosis. Second mitochondria-derived activator of caspases (SMAC)/ direct inhibitor of apoptosis protein (IAP)-binding protein with low pI (DIABLO) has attracted phenomenal attention because of its amazing ability to trigger apoptotic death. Accordingly, different teams of interdisciplinary researchers are working on the design and development of SMAC mimetics which can significantly inhibit primary and secondary tumor growth.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199098","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：