Sarah A. Stewart, Juan Domínguez-Robles, R. Donnelly, E. Larrañeta
This article investigates the potential use of microwave (MW) radiation, UV-light and gamma radiation for the sterilisation of 3D-printed implantable devices prepared using poly(lactic acid) (PLA) and poly(vinyl alcohol) (PVA). Samples were sterilised using MW, UV and gamma radiation. Subsequently, the sterility of these samples was tested following the British Pharmacopeia test for sterility and controlled contamination test. Finally, sterilised samples were characterised (DSC, FTIR and drug release studies) to evaluate potential changes in their physicochemical properties during sterilisation. MW-radiation failed the British Pharmacopeia test for sterility. UV-light did not pass the British Pharmacopoeia test for sterility, but it showed promising results for the controlled contamination test (bacterial-contamination reduction >99.9%). These techniques did not modify the physicochemical properties of PLA. On the other hand, samples treated with gamma radiation passed the British Pharmacopeia sterility tests. However, the Tg and mechanical properties of the resulting samples were affected by gamma radiation. It is important to note that none of the sterilisation methods investigated in this article resulted in any change in the in vitro release results. Only gamma radiation passed the British Pharmacopeia test for sterility. However, UV method showed potential and should be further investigated.
{"title":"Evaluation of sterilisation techniques for 3D-printed implantable devices","authors":"Sarah A. Stewart, Juan Domínguez-Robles, R. Donnelly, E. Larrañeta","doi":"10.1093/rpsppr/rqad003","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad003","url":null,"abstract":"\u0000 \u0000 \u0000 This article investigates the potential use of microwave (MW) radiation, UV-light and gamma radiation for the sterilisation of 3D-printed implantable devices prepared using poly(lactic acid) (PLA) and poly(vinyl alcohol) (PVA).\u0000 \u0000 \u0000 \u0000 Samples were sterilised using MW, UV and gamma radiation. Subsequently, the sterility of these samples was tested following the British Pharmacopeia test for sterility and controlled contamination test. Finally, sterilised samples were characterised (DSC, FTIR and drug release studies) to evaluate potential changes in their physicochemical properties during sterilisation.\u0000 \u0000 \u0000 \u0000 MW-radiation failed the British Pharmacopeia test for sterility. UV-light did not pass the British Pharmacopoeia test for sterility, but it showed promising results for the controlled contamination test (bacterial-contamination reduction >99.9%). These techniques did not modify the physicochemical properties of PLA. On the other hand, samples treated with gamma radiation passed the British Pharmacopeia sterility tests. However, the Tg and mechanical properties of the resulting samples were affected by gamma radiation. It is important to note that none of the sterilisation methods investigated in this article resulted in any change in the in vitro release results.\u0000 \u0000 \u0000 \u0000 Only gamma radiation passed the British Pharmacopeia test for sterility. However, UV method showed potential and should be further investigated.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42622258","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}
S. Sardana, Rupa Gupta, Kumud Madan, D. Bisht, V. Rana, Samir Bhargava, N. Sethiya
Berberine has attracted prominent interest recently due to its wide pharmacological actions in management and treatments of several disease including liver. However, restricted bioavailability and permeability makes this drug as better choice to develop several value added products for improvement of both safety and efficacy. Many of research already conducted in this direction using several approaches to fix this issue. Therefore, current article was designed to summarize all approaches taking together to enhance hepatoprotection by berberine including molecular mechanism. Online scientific databases from PubMed was assessed for collecting information on berberine. All the collected informations were classified and incorporated into different sections such as recent progress of research on advance drug delivery systems and combinational approaches addressing above issue for improvement of hepatoprotective action of berberine. The electronically PubMed database search yielded 7454 articles from different countries in several languages. Out of them two seventy articles published between 1932 and 2022 were included, corresponding to all detailed overview on berberine including research pertaining on toxicity and safety, biodistribution, pharmacokinetics, biopharmaceutics classification system (BCS), hepatoprotection against various hepatotoxicant agent, advance drug delivery system, combinational drug approaches, clinical Trial for hepatoprotection and patents. The review of the literature reveals that berberine exhibits a potent hepatoprotective action with several molecular action mechanisms. Additionally, current trends of formulation technology for enhancement of hepatoprotective action of berberine in terms of safety and efficacy are well co-related with present work. It was well established and concluded from present work that both advance drug delivery system and combinational drug approaches may serve for enhancement of restricted hepatoprotective action of berberine due to poor bioavailability, solubility and permeability. Additionally, berberine based advance delivery system including in combination with bioavailability and permeability enhancer may provide an added advantage in near future to meet the objectives.
{"title":"Advance drug delivery and combinational drug approaches for hepatoprotective action of berberine: A progressive overview with underlying mechanism","authors":"S. Sardana, Rupa Gupta, Kumud Madan, D. Bisht, V. Rana, Samir Bhargava, N. Sethiya","doi":"10.1093/rpsppr/rqad002","DOIUrl":"https://doi.org/10.1093/rpsppr/rqad002","url":null,"abstract":"\u0000 \u0000 \u0000 Berberine has attracted prominent interest recently due to its wide pharmacological actions in management and treatments of several disease including liver. However, restricted bioavailability and permeability makes this drug as better choice to develop several value added products for improvement of both safety and efficacy. Many of research already conducted in this direction using several approaches to fix this issue. Therefore, current article was designed to summarize all approaches taking together to enhance hepatoprotection by berberine including molecular mechanism.\u0000 \u0000 \u0000 \u0000 Online scientific databases from PubMed was assessed for collecting information on berberine. All the collected informations were classified and incorporated into different sections such as recent progress of research on advance drug delivery systems and combinational approaches addressing above issue for improvement of hepatoprotective action of berberine.\u0000 \u0000 \u0000 \u0000 The electronically PubMed database search yielded 7454 articles from different countries in several languages. Out of them two seventy articles published between 1932 and 2022 were included, corresponding to all detailed overview on berberine including research pertaining on toxicity and safety, biodistribution, pharmacokinetics, biopharmaceutics classification system (BCS), hepatoprotection against various hepatotoxicant agent, advance drug delivery system, combinational drug approaches, clinical Trial for hepatoprotection and patents. The review of the literature reveals that berberine exhibits a potent hepatoprotective action with several molecular action mechanisms. Additionally, current trends of formulation technology for enhancement of hepatoprotective action of berberine in terms of safety and efficacy are well co-related with present work.\u0000 \u0000 \u0000 \u0000 It was well established and concluded from present work that both advance drug delivery system and combinational drug approaches may serve for enhancement of restricted hepatoprotective action of berberine due to poor bioavailability, solubility and permeability. Additionally, berberine based advance delivery system including in combination with bioavailability and permeability enhancer may provide an added advantage in near future to meet the objectives.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44615339","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. Alum, Joseph E. Inya, O. Ugwu, E. Obeagu, C. Aloke, Manasseh O Orji, Ozioma Onyema
Methotrexate (MTX) is a commonly used anti-cancer drug. However, its usage could lead to various biochemical dysregulations culminating in organ toxicity. Globally, most plant products have been used for the treatment of several diseases. Thus, we investigated the effect of Datura stramonium ethanolic leaf extract (DSELE) supplementation in MXT-induced biochemical alterations in rats. Rats were divided into 4 groups: Group one received normal saline (5mg/kg b. w), Group two received DSELE (200mg/kg), Group three received 20mg/kg MXT while rats in Group four received 200mg/kg + MTX 20mg/kg. Normal saline and DSELE were administered per os for 21 days while MXT single injection was given intraperitoneally on day 18 and the rats were sacrificed after 3 days. Thereafter, biochemical parameters were evaluated. MTX caused a significant (P<0.05) increase in serum activities of liver enzymes (AST, ALT and ALP) and levels of total cholesterol and low-density lipoprotein while the levels of total protein and albumin decreased significantly relative to the normal control. Interestingly, DSELE administration favorably modulated MXT-induced biochemical alterations to levels comparable to normal control. DSELE can be a useful combinatorial natural product in MTX chemotherapy since it mitigates MXT-induced biochemical alterations in rats.
{"title":"Ethanolic leaf extract of Datura stramonium attenuates Methotrexate-induced BiochemicalAlterations in Wistar Albino rats","authors":"E. Alum, Joseph E. Inya, O. Ugwu, E. Obeagu, C. Aloke, Manasseh O Orji, Ozioma Onyema","doi":"10.1093/rpsppr/rqac011","DOIUrl":"https://doi.org/10.1093/rpsppr/rqac011","url":null,"abstract":"\u0000 \u0000 \u0000 Methotrexate (MTX) is a commonly used anti-cancer drug. However, its usage could lead to various biochemical dysregulations culminating in organ toxicity. Globally, most plant products have been used for the treatment of several diseases. Thus, we investigated the effect of Datura stramonium ethanolic leaf extract (DSELE) supplementation in MXT-induced biochemical alterations in rats.\u0000 \u0000 \u0000 \u0000 Rats were divided into 4 groups: Group one received normal saline (5mg/kg b. w), Group two received DSELE (200mg/kg), Group three received 20mg/kg MXT while rats in Group four received 200mg/kg + MTX 20mg/kg. Normal saline and DSELE were administered per os for 21 days while MXT single injection was given intraperitoneally on day 18 and the rats were sacrificed after 3 days. Thereafter, biochemical parameters were evaluated.\u0000 \u0000 \u0000 \u0000 MTX caused a significant (P<0.05) increase in serum activities of liver enzymes (AST, ALT and ALP) and levels of total cholesterol and low-density lipoprotein while the levels of total protein and albumin decreased significantly relative to the normal control. Interestingly, DSELE administration favorably modulated MXT-induced biochemical alterations to levels comparable to normal control.\u0000 \u0000 \u0000 \u0000 DSELE can be a useful combinatorial natural product in MTX chemotherapy since it mitigates MXT-induced biochemical alterations in rats.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42242531","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-01-06eCollection Date: 2023-01-01DOI: 10.1093/rpsppr/rqad001
Rami A Al-Horani, Daniel K Afosah, Srabani Kar, Kholoud F Aliter, Madhusoodanan Mottamal
Objective: Cathepsin G (CatG) is a cationic serine protease with wide substrate specificity. CatG is reported to play a role in several inflammatory pathologies. Thus, we aimed at identifying a potent and allosteric inhibitor of CatG to be used as a platform in further drug development opportunities.
Methods: Chromogenic substrate hydrolysis assays were used to evaluate the inhibition potency and selectivity of SPGG towards CatG. Salt-dependent studies, Michaelis-Menten kinetics and SDS-PAGE were exploited to decipher the mechanism of CatG inhibition by SPGG. Molecular modelling was also used to identify a plausible binding site.
Key findings: SPGG displayed an inhibition potency of 57 nM against CatG, which was substantially selective over other proteases. SPGG protected fibronectin and laminin against CatG-mediated degradation. SPGG reduced VMAX of CatG hydrolysis of a chromogenic substrate without affecting KM, suggesting an allosteric mechanism. Resolution of energy contributions indicated that non-ionic interactions contribute ~91% of binding energy, suggesting a substantial possibility of specific recognition. Molecular modelling indicated that SPGG plausibly binds to an anion-binding sequence of 109SRRVRRNRN117.
Conclusion: We present the discovery of SPGG as the first small molecule, potent, allosteric glycosaminoglycan mimetic inhibitor of CatG. SPGG is expected to open a major route to clinically relevant allosteric CatG anti-inflammatory agents.
{"title":"Sulphated penta-galloyl glucopyranoside (SPGG) is glycosaminoglycan mimetic allosteric inhibitor of cathepsin G.","authors":"Rami A Al-Horani, Daniel K Afosah, Srabani Kar, Kholoud F Aliter, Madhusoodanan Mottamal","doi":"10.1093/rpsppr/rqad001","DOIUrl":"10.1093/rpsppr/rqad001","url":null,"abstract":"<p><strong>Objective: </strong>Cathepsin G (CatG) is a cationic serine protease with wide substrate specificity. CatG is reported to play a role in several inflammatory pathologies. Thus, we aimed at identifying a potent and allosteric inhibitor of CatG to be used as a platform in further drug development opportunities.</p><p><strong>Methods: </strong>Chromogenic substrate hydrolysis assays were used to evaluate the inhibition potency and selectivity of SPGG towards CatG. Salt-dependent studies, Michaelis-Menten kinetics and SDS-PAGE were exploited to decipher the mechanism of CatG inhibition by SPGG. Molecular modelling was also used to identify a plausible binding site.</p><p><strong>Key findings: </strong>SPGG displayed an inhibition potency of 57 nM against CatG, which was substantially selective over other proteases. SPGG protected fibronectin and laminin against CatG-mediated degradation. SPGG reduced V<sub>MAX</sub> of CatG hydrolysis of a chromogenic substrate without affecting K<sub>M</sub>, suggesting an allosteric mechanism. Resolution of energy contributions indicated that non-ionic interactions contribute ~91% of binding energy, suggesting a substantial possibility of specific recognition. Molecular modelling indicated that SPGG plausibly binds to an anion-binding sequence of <sup>109</sup>SRRVRRNRN<sup>117</sup>.</p><p><strong>Conclusion: </strong>We present the discovery of SPGG as the first small molecule, potent, allosteric glycosaminoglycan mimetic inhibitor of CatG. SPGG is expected to open a major route to clinically relevant allosteric CatG anti-inflammatory agents.</p>","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":"2 1","pages":"rqad001"},"PeriodicalIF":0.0,"publicationDate":"2023-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9942669/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10793203","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
H. Mockdeci, L. Junqueira, L. Duarte, Carolina Paula de Souza Moreira, M. D. de Oliveira, M. Brandão, G. Tavares, N. R. Raposo
develop a hydrogel containing tea tree oil (TTO) encapsulated in solid lipid nanoparticles (SLNs) to treat oropharyngeal candidiasis. initially, the TTO chemical composition was evaluated. Next, SLNs containing TTO (TTO-SLNs) were produced and characterized. The TTO-SLNs were incorporated into a hydrogel, and the antifungal activity against Candida spp. was analysed. Finally, the ex vivo permeation was assessed. the chemical composition of TTO met ISO 4730:2017 standards. The TTO-SLNs were spherical and had a Z-average, PdI, ZP, and entrapment efficiency of 135.90 ± 6.65 nm, 0.19 ± 0.04 -31.07 ± 1.05 mV, and 92.74% ± 0.01%, respectively. Moreover, TTO-SLNs were stable (no changes in Z-average and PdI) for at least 120 days. In the cytotoxicity evaluation, the samples were considered cytotoxic at the following concentrations: TTO: 125-1,000 µg/mL, TTO-SLN: 348-5,568 µg/mL of TTO, and the control nanoparticle was not cytotoxic. Both TTO-SLNs and the hydrogel containing TTO-SLNs demonstrated fungicidal action against all Candida spp., while for TTO, it was found only against C. albicans. The percentage of TTO permeation was 70.52%. the hydrogel loaded with TTO-SLNs is a promising tool for TTO delivery, aiming at activity against C. albicans for the treatment of oropharyngeal candidiasis.
{"title":"Improved anti-Candida activity of hydrogel containing tea tree oil-loaded solid lipid nanoparticles for the treatment of oropharyngeal candidiasis","authors":"H. Mockdeci, L. Junqueira, L. Duarte, Carolina Paula de Souza Moreira, M. D. de Oliveira, M. Brandão, G. Tavares, N. R. Raposo","doi":"10.1093/rpsppr/rqac010","DOIUrl":"https://doi.org/10.1093/rpsppr/rqac010","url":null,"abstract":"\u0000 \u0000 \u0000 develop a hydrogel containing tea tree oil (TTO) encapsulated in solid lipid nanoparticles (SLNs) to treat oropharyngeal candidiasis.\u0000 \u0000 \u0000 \u0000 initially, the TTO chemical composition was evaluated. Next, SLNs containing TTO (TTO-SLNs) were produced and characterized. The TTO-SLNs were incorporated into a hydrogel, and the antifungal activity against Candida spp. was analysed. Finally, the ex vivo permeation was assessed.\u0000 \u0000 \u0000 \u0000 the chemical composition of TTO met ISO 4730:2017 standards. The TTO-SLNs were spherical and had a Z-average, PdI, ZP, and entrapment efficiency of 135.90 ± 6.65 nm, 0.19 ± 0.04 -31.07 ± 1.05 mV, and 92.74% ± 0.01%, respectively. Moreover, TTO-SLNs were stable (no changes in Z-average and PdI) for at least 120 days. In the cytotoxicity evaluation, the samples were considered cytotoxic at the following concentrations: TTO: 125-1,000 µg/mL, TTO-SLN: 348-5,568 µg/mL of TTO, and the control nanoparticle was not cytotoxic. Both TTO-SLNs and the hydrogel containing TTO-SLNs demonstrated fungicidal action against all Candida spp., while for TTO, it was found only against C. albicans. The percentage of TTO permeation was 70.52%.\u0000 \u0000 \u0000 \u0000 the hydrogel loaded with TTO-SLNs is a promising tool for TTO delivery, aiming at activity against C. albicans for the treatment of oropharyngeal candidiasis.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42398208","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}
Oriana Boscolo, S. Flor, C. Dobrecky, V. Tripodi, S. Lucangioli
To develop and validate an analytical method by HPLC-UV for the quantification of ursodeoxycholic acid suspension in a dissolution test followed by a solid phase extraction to circumvent the interference of sodium lauryl sulfate present in the dissolution medium. USP apparatus 2. The dissolution medium was 900 mL of an aqueous solution of 0.05 M phosphate buffer (pH 8.4) with 2% sodium lauryl sulfate. The samples were filtered and cleaned by solid phase extraction with 500 mg/3mL C18 cartridges. The analytical method was validated for specificity, linearity, LOD, LOQ accuracy and precision. Chromatographic conditions, Symmetry-C18 column (150 mm x 4.6 mm, id; 5 µm particle size), 40 ˚C, 100 µL injection volume, and UV detection at 200 nm. The flow rate was 1 mL/min using acetonitrile-phosphoric acid (pH 3.0, 0.15 mM) (48:52). Solid phase extraction provided an efficient and selective extraction of ursodeoxycholic acid from the dissolution medium. On the other hand, the solid phase extraction washing step allowed the elimination of sodium lauryl sulfate. The ursodeoxycholic acid method optimization and validation were accomplished with no less than 80% in 30 minutes. The developed analytical method was simple and adequate for the analysis of ursodeoxycholic acid suspension samples which met the USP specifications for dissolution test.
开发并验证一种HPLC-UV分析方法，用于在溶解试验中定量熊去氧胆酸悬浮液，然后进行固相萃取，以避免溶解介质中存在的十二烷基硫酸钠的干扰。USP装置2。溶解介质为900mL含有2%十二烷基硫酸钠的0.05M磷酸盐缓冲液（pH 8.4）的水溶液。用500mg/3mL C18柱通过固相萃取对样品进行过滤和清洁。验证了该分析方法的特异性、线性、LOD、LOQ的准确性和精密度。色谱条件，Symmetriy-C18柱（150 mm x 4.6 mm，id；5µm粒径），40˚C，100µL进样体积，200 nm紫外检测。使用乙腈-磷酸（pH 3.0，0.15mM）（48:52），流速为1mL/min。固相萃取提供了从溶解介质中有效和选择性地提取熊去氧胆酸。另一方面，固相萃取洗涤步骤可以消除十二烷基硫酸钠。熊去氧胆酸方法的优化和验证在30分钟内完成了不低于80%。所开发的分析方法简单，适用于分析符合USP溶出度测试规范的熊去氧胆酸混悬液样品。
{"title":"Dissolution Testing Of Ursodeoxycholic Acid Suspension Using Spe As Sample Preparation","authors":"Oriana Boscolo, S. Flor, C. Dobrecky, V. Tripodi, S. Lucangioli","doi":"10.1093/rpsppr/rqac006","DOIUrl":"https://doi.org/10.1093/rpsppr/rqac006","url":null,"abstract":"\u0000 \u0000 \u0000 To develop and validate an analytical method by HPLC-UV for the quantification of ursodeoxycholic acid suspension in a dissolution test followed by a solid phase extraction to circumvent the interference of sodium lauryl sulfate present in the dissolution medium.\u0000 \u0000 \u0000 \u0000 USP apparatus 2. The dissolution medium was 900 mL of an aqueous solution of 0.05 M phosphate buffer (pH 8.4) with 2% sodium lauryl sulfate. The samples were filtered and cleaned by solid phase extraction with 500 mg/3mL C18 cartridges. The analytical method was validated for specificity, linearity, LOD, LOQ accuracy and precision. Chromatographic conditions, Symmetry-C18 column (150 mm x 4.6 mm, id; 5 µm particle size), 40 ˚C, 100 µL injection volume, and UV detection at 200 nm. The flow rate was 1 mL/min using acetonitrile-phosphoric acid (pH 3.0, 0.15 mM) (48:52).\u0000 \u0000 \u0000 \u0000 Solid phase extraction provided an efficient and selective extraction of ursodeoxycholic acid from the dissolution medium. On the other hand, the solid phase extraction washing step allowed the elimination of sodium lauryl sulfate. The ursodeoxycholic acid method optimization and validation were accomplished with no less than 80% in 30 minutes.\u0000 \u0000 \u0000 \u0000 The developed analytical method was simple and adequate for the analysis of ursodeoxycholic acid suspension samples which met the USP specifications for dissolution test.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45712275","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}
D. Faustino, Naiara Nascimento das Chagas Lima, K. Allahdadi, Laise Cedraz Pinto
Kalanchoe daigremontiana (KD) is a succulent plant with widespread popular use as an anticancer and for the treatment of a variety of other diseases. The presence of bufadienolides (BFD), a cardiotoxic compound, and other substances may justify some of its biological properties, however, clinical studies and toxicity and safety data are still scarce. The objective of this systematic review was to describe KD’s biological properties and mechanisms, as well as its toxicity. Searches were performed in four databases with the descriptors: “kalanchoe daigremontiana” AND “cytotoxicity”, “antioxidant” OR “anti-inflammatory” OR “toxicity”. In total, 11 studies were included according to the PRISMA 2020 protocol. The aqueous and ethanolic extracts of KD showed important antioxidant and anti-inflammatory activity, associated with the presence of flavonoids and phenols in the extracts. The extracts from fractions that were rich in BFD or dichloromethane showed anticancer (related to inhibition of mitochondrial dehydrogenase activity and reduction of glutathione level) and anticoagulant actions (due to reduced fibrin clot formation and increased degradation). More studies are still needed to demonstrate the concentration limits for beneficial effects and the toxic limitations of this species, which until then, cautious use and consumption of KD is recommended.
{"title":"Biological properties of different extracts of the Kalanchoe daigremontiana (“Mother of thousands”): a review","authors":"D. Faustino, Naiara Nascimento das Chagas Lima, K. Allahdadi, Laise Cedraz Pinto","doi":"10.1093/rpsppr/rqac009","DOIUrl":"https://doi.org/10.1093/rpsppr/rqac009","url":null,"abstract":"\u0000 \u0000 \u0000 Kalanchoe daigremontiana (KD) is a succulent plant with widespread popular use as an anticancer and for the treatment of a variety of other diseases. The presence of bufadienolides (BFD), a cardiotoxic compound, and other substances may justify some of its biological properties, however, clinical studies and toxicity and safety data are still scarce. The objective of this systematic review was to describe KD’s biological properties and mechanisms, as well as its toxicity.\u0000 \u0000 \u0000 \u0000 Searches were performed in four databases with the descriptors: “kalanchoe daigremontiana” AND “cytotoxicity”, “antioxidant” OR “anti-inflammatory” OR “toxicity”. In total, 11 studies were included according to the PRISMA 2020 protocol.\u0000 \u0000 \u0000 \u0000 The aqueous and ethanolic extracts of KD showed important antioxidant and anti-inflammatory activity, associated with the presence of flavonoids and phenols in the extracts. The extracts from fractions that were rich in BFD or dichloromethane showed anticancer (related to inhibition of mitochondrial dehydrogenase activity and reduction of glutathione level) and anticoagulant actions (due to reduced fibrin clot formation and increased degradation).\u0000 \u0000 \u0000 \u0000 More studies are still needed to demonstrate the concentration limits for beneficial effects and the toxic limitations of this species, which until then, cautious use and consumption of KD is recommended.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45080965","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}
Nicolas Ripari, Maria Beatriz Toti, J. Bastos, J. M. Sforcin
Methicillin-resistant Staphylococcus aureus (MRSA) is a multidrug-resistant pathogen in nosocomial infections. Since the 1950’s, MRSA has acquired several resistance factors including efflux pumps and drug target modifications. Some studies investigated the anti-MRSA capacity of propolis samples collected in different regions and their immunomodulatory action. The aim of this review is to gather the data published up to August 2022 about propolis action on MRSA strains and its modulatory action on phagocytes. The PubMed database was used looking for articles containing the keywords “propolis”, “immunomodulation”, “MRSA” and the name of each compound. As propolis contains a variety of compounds making it impossible to isolate the major bioactive components, we reviewed the main compounds found in several propolis samples and their mechanisms towards the resistance factors displayed by MRSA. Some perspectives for using propolis-based medications and the formulation of new antimicrobial/immunomodulatory agents are discussed. Propolis extracts and active compounds exert antibacterial action over MRSA strains acting on resistance factors. Moreover, propolis modulates pro-inflammatory markers in phagocytes. Because propolis compounds may act synergistically, it’s crucial to understand how these components interact in order to synthesize standardized formulations and enhance their bioavailability for clinical applications to combat MRSA.
{"title":"Can bee propolis help us fight against methicillin-resistant Staphylococcus aureus (MRSA)?","authors":"Nicolas Ripari, Maria Beatriz Toti, J. Bastos, J. M. Sforcin","doi":"10.1093/rpsppr/rqac008","DOIUrl":"https://doi.org/10.1093/rpsppr/rqac008","url":null,"abstract":"\u0000 \u0000 \u0000 Methicillin-resistant Staphylococcus aureus (MRSA) is a multidrug-resistant pathogen in nosocomial infections. Since the 1950’s, MRSA has acquired several resistance factors including efflux pumps and drug target modifications. Some studies investigated the anti-MRSA capacity of propolis samples collected in different regions and their immunomodulatory action. The aim of this review is to gather the data published up to August 2022 about propolis action on MRSA strains and its modulatory action on phagocytes.\u0000 \u0000 \u0000 \u0000 The PubMed database was used looking for articles containing the keywords “propolis”, “immunomodulation”, “MRSA” and the name of each compound. As propolis contains a variety of compounds making it impossible to isolate the major bioactive components, we reviewed the main compounds found in several propolis samples and their mechanisms towards the resistance factors displayed by MRSA. Some perspectives for using propolis-based medications and the formulation of new antimicrobial/immunomodulatory agents are discussed.\u0000 \u0000 \u0000 \u0000 Propolis extracts and active compounds exert antibacterial action over MRSA strains acting on resistance factors. Moreover, propolis modulates pro-inflammatory markers in phagocytes.\u0000 \u0000 \u0000 \u0000 Because propolis compounds may act synergistically, it’s crucial to understand how these components interact in order to synthesize standardized formulations and enhance their bioavailability for clinical applications to combat MRSA.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43902740","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}
Compressibility of materials is determining the tableting behaviour and tablet properties during and after manufacturing. The compressibility constant has not been investigated as an in-die method yet and was therefore compared with the Heckel analysis for describing the compressibility of materials during tableting in this study. Various parameters influencing tableting, such as compression pressure, compression speed and punch diameter, were used to analyze the robustness of both methods and to evaluate the informative value of the compression parameters. Twelve common pharmaceutical excipients were used to cover a wide range of material properties. The compressibility constant was successfully applied as an in-die method and proved to be more robust against the influencing parameters during tableting than the Heckel analysis. A good correlation between the out-of-die and in-die method was found for both methods but could not be observed between the compressibility constant and the yield pressure from Heckel analysis. The methods are both describing the volume reduction of materials under pressure but focus on different material properties. For material characterization in the field of tableting, the compressibility constant can be additionally applied in the future to be able to determine another compressibility parameter in combination with the yield pressure.
{"title":"Compressibility analysis as robust in-die compression analysis for describing tableting behaviour","authors":"Sabrina Berkenkemper, P. Kleinebudde","doi":"10.1093/rpsppr/rqac004","DOIUrl":"https://doi.org/10.1093/rpsppr/rqac004","url":null,"abstract":"\u0000 \u0000 \u0000 Compressibility of materials is determining the tableting behaviour and tablet properties during and after manufacturing. The compressibility constant has not been investigated as an in-die method yet and was therefore compared with the Heckel analysis for describing the compressibility of materials during tableting in this study.\u0000 \u0000 \u0000 \u0000 Various parameters influencing tableting, such as compression pressure, compression speed and punch diameter, were used to analyze the robustness of both methods and to evaluate the informative value of the compression parameters. Twelve common pharmaceutical excipients were used to cover a wide range of material properties.\u0000 \u0000 \u0000 \u0000 The compressibility constant was successfully applied as an in-die method and proved to be more robust against the influencing parameters during tableting than the Heckel analysis. A good correlation between the out-of-die and in-die method was found for both methods but could not be observed between the compressibility constant and the yield pressure from Heckel analysis. The methods are both describing the volume reduction of materials under pressure but focus on different material properties.\u0000 \u0000 \u0000 \u0000 For material characterization in the field of tableting, the compressibility constant can be additionally applied in the future to be able to determine another compressibility parameter in combination with the yield pressure.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42645315","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}
T. Aishwarya, Nadella Mounika, Gayatri Vishwakarma, Ramu Adela
Non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) are the major public health issues. Though the prevalence of the disease is high, there is no approved pharmacological treatment. Obeticholic acid (OCA) has not been well described in terms of its efficacy and safety in NAFLD/NASH patients. Hence, we investigated the efficacy and safety of OCA in NAFLD/NASH patients. PubMed, Cochrane CENTRAL, and Google Scholar were searched from 2001 to date for identifying randomized controlled trials which examined the OCA effect on liver enzymes, lipoproteins, and liver histology in NASH/NAFLD patients. Four relevant RCTs were identified and included for quantitative analysis. OCA exhibited significant reduction in ALT, AST and GGT levels, whereas, in case of liver histology, significant improvement in steatosis, hepatocellular ballooning, lobular inflammation and fibrosis was observed in OCA treatment group [RR: 1.25, 95% CI: (1.03 to 1.52); p = 0.02; I 2=53%], [RR: 1.39, 95% CI: (1.17 to 1.64); p = 0.0001; I 2=0%], [RR: 1.23, 95% CI: (1.07 to 1.40); p = 0.002; I 2=29%] and [RR: 1.85, 95% CI: (1.44 to 2.38); p < 0.00001; I 2=0%] respectively. Our results indicate that OCA might be used as a potential therapeutic drug candidate in NAFLD/NASH management.
{"title":"Effect of Obeticholic acid in Non-alcoholic fatty liver disease (NAFLD) and Non-alcoholic steatohepatitis (NASH) patients: A Systematic review and Meta-analysis","authors":"T. Aishwarya, Nadella Mounika, Gayatri Vishwakarma, Ramu Adela","doi":"10.1093/rpsppr/rqac001","DOIUrl":"https://doi.org/10.1093/rpsppr/rqac001","url":null,"abstract":"\u0000 \u0000 \u0000 Non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) are the major public health issues. Though the prevalence of the disease is high, there is no approved pharmacological treatment. Obeticholic acid (OCA) has not been well described in terms of its efficacy and safety in NAFLD/NASH patients. Hence, we investigated the efficacy and safety of OCA in NAFLD/NASH patients.\u0000 \u0000 \u0000 \u0000 PubMed, Cochrane CENTRAL, and Google Scholar were searched from 2001 to date for identifying randomized controlled trials which examined the OCA effect on liver enzymes, lipoproteins, and liver histology in NASH/NAFLD patients.\u0000 \u0000 \u0000 \u0000 Four relevant RCTs were identified and included for quantitative analysis. OCA exhibited significant reduction in ALT, AST and GGT levels, whereas, in case of liver histology, significant improvement in steatosis, hepatocellular ballooning, lobular inflammation and fibrosis was observed in OCA treatment group [RR: 1.25, 95% CI: (1.03 to 1.52); p = 0.02; I 2=53%], [RR: 1.39, 95% CI: (1.17 to 1.64); p = 0.0001; I 2=0%], [RR: 1.23, 95% CI: (1.07 to 1.40); p = 0.002; I 2=29%] and [RR: 1.85, 95% CI: (1.44 to 2.38); p < 0.00001; I 2=0%] respectively.\u0000 \u0000 \u0000 \u0000 Our results indicate that OCA might be used as a potential therapeutic drug candidate in NAFLD/NASH management.\u0000","PeriodicalId":74744,"journal":{"name":"RPS pharmacy and pharmacology reports","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46959613","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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