Background: Efavirenz, a first line anti-retroviral drug has variable bioavailability owing to its limited aqueous solubility. Piperine, a bioavailability enhancer has been often used to enhance the bioavailability of many drugs. Objective: The present study was aimed to investigate the possibility of improving the bioavailability of efavirenz using piperine. Methods: Two doses of efavirenz 9.33 mg/kg and 28 mg/kg which corresponded to 200 and 600 mg/kg of human dose were selected. Single oral dose of efavirenz and piperine co administration was given to rabbit and at fixed time interval drug blood concentration was estimated by HPLC. Pharmacokinetic parameters of efavirenz and piperine co administration were determined. Results: Efavirenz 9.33 mg/kg co administration with piperine 20.8 mg/kg increased area under the curve significantly at p<0.01 and Cmax at p<0.05 compared to efavirenz control (9.33 mg/kg). The relative bioavailability of efavirenz and piperine co-administration was found to be 149.08%, i.e., higher than efavirenz control. T1/2 of piperine co-administration was also increased significantly at p<0.05 compared to efavirenz control. Tmax of piperine co-administration was found to be 0.5 h, followed by efavirenz control i.e., 1 h. Co-administration of efavirenz (28 mg/kg) with piperine (20.8 mg.kg) significantly increased AUC and Cmax at p<0.001 compared to efavirenz control (28 mg/kg). The relative bioavailability of Piperine co-administration was found to be 158.92%, higher than efavirenz control. There was significant increase in T1/2 of piperine co-administration at p<0.01 compared to efavirenz control. Tmax of piperine co-administration and efavirenz were found to be same i.e., 1 h. Conclusion: Based on the results it can be concluded that piperine co-administration significantly increases the oral exposure of efavirenz. Bioavailability of efavirenz with piperine was found to be higher than efavirenz control.
{"title":"Oral Bioavailability Enhancement of Efavirenz using Piperine coadministration in Experimental Rabbits","authors":"M. Asif","doi":"10.31531/jprst.1000156","DOIUrl":"https://doi.org/10.31531/jprst.1000156","url":null,"abstract":"Background: Efavirenz, a first line anti-retroviral drug has variable bioavailability owing to its limited aqueous solubility. Piperine, a bioavailability enhancer has been often used to enhance the bioavailability of many drugs. Objective: The present study was aimed to investigate the possibility of improving the bioavailability of efavirenz using piperine. Methods: Two doses of efavirenz 9.33 mg/kg and 28 mg/kg which corresponded to 200 and 600 mg/kg of human dose were selected. Single oral dose of efavirenz and piperine co administration was given to rabbit and at fixed time interval drug blood concentration was estimated by HPLC. Pharmacokinetic parameters of efavirenz and piperine co administration were determined. Results: Efavirenz 9.33 mg/kg co administration with piperine 20.8 mg/kg increased area under the curve significantly at p<0.01 and Cmax at p<0.05 compared to efavirenz control (9.33 mg/kg). The relative bioavailability of efavirenz and piperine co-administration was found to be 149.08%, i.e., higher than efavirenz control. T1/2 of piperine co-administration was also increased significantly at p<0.05 compared to efavirenz control. Tmax of piperine co-administration was found to be 0.5 h, followed by efavirenz control i.e., 1 h. Co-administration of efavirenz (28 mg/kg) with piperine (20.8 mg.kg) significantly increased AUC and Cmax at p<0.001 compared to efavirenz control (28 mg/kg). The relative bioavailability of Piperine co-administration was found to be 158.92%, higher than efavirenz control. There was significant increase in T1/2 of piperine co-administration at p<0.01 compared to efavirenz control. Tmax of piperine co-administration and efavirenz were found to be same i.e., 1 h. Conclusion: Based on the results it can be concluded that piperine co-administration significantly increases the oral exposure of efavirenz. Bioavailability of efavirenz with piperine was found to be higher than efavirenz control.","PeriodicalId":16735,"journal":{"name":"Journal of Pharmaceutical Research Science & Technology","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74463885","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}
Background: Vanillin is a white monoclinic crystalline compound whose chemical nomenclature is p-hydroxy-m-methoxy benzaldehyde. It is a phenolic aldehyde with a pleasant flavor and popularly found in vanilla beans and roasted coffee amongst many other sources. It serves as in addition; it possesses antitumor and particularly antioxidant activity which formed the essence of this study. Objectives: The insidious presence of free oxygenated and nitrogen radicals in the human body has become a worrisome concern. These chemical species continue to plague the human cells, tissues and organs resulting in different pathophysiological conditions such as cancers and neurodegenerative disorders like Alzheimer’s disease and Parkinson’s disease amongst many other ailments. The search for novel pharmacological compounds with the aim of curbing the rising incidence of these radicals led the choice of vanillin in this present study. Methodology: Vanillin was separately subjected to a series of derivatization reactions namely, acetylation, O-demethylation, reduction and oxidation. The melting points, refractive indices and optical rotations of the lead compound and derivatives were obtained. The antioxidant activities of the five compounds were determined using the DPPH (2, 2-diphenyl-1-picrylhydrazyl hydrate) test. Comparison of the obtained antioxidant activities was done to determine if any improvements could be seen in the derivatives. Results: The identities of the derivatives have been revealed to be vanillyl acetate (E-1) (acetyl derivative), 3, 4-dihydroxy benzaldehyde or protocatechui aldehyde (E-2) (demethylated derivative), o-methoxy-p-methyl cyclohexan-1-ol (J-1) (reduced derivative) and vanillic acid (J-2) (oxidized derivative) respectively using the IR spectral technique. Vanillin, E-2 and J-2 derivatives gave marginal antioxidant activity of IC50 of 0.81, 0.84 and 0.0.85 µg/mL respectively while J-1 and E-1 demonstrated moderately significant IC50 of 0.59 and 0.63 µg/mL which compare favorably with 0.44 µg/mL elicited by Vitamin C (a standard antioxidant drug). It is pertinent to point out that the obtained reduced derivative is a substituted cycloalkanol (a saturated cyclic compound) instead of a substituted phenolic compound as was expected. Conclusion: The results from this study indicate that reduction and acetylation separately enhance the antioxidant activity of vanillin.
{"title":"A Cycloalkanol from Derivatization Studies on Vanillin: Evaluation of Antioxidant Activity of Obtained Derivatives","authors":"O. Oladimeji","doi":"10.31531/jprst.1000157","DOIUrl":"https://doi.org/10.31531/jprst.1000157","url":null,"abstract":"Background: Vanillin is a white monoclinic crystalline compound whose chemical nomenclature is p-hydroxy-m-methoxy benzaldehyde. It is a phenolic aldehyde with a pleasant flavor and popularly found in vanilla beans and roasted coffee amongst many other sources. It serves as in addition; it possesses antitumor and particularly antioxidant activity which formed the essence of this study. Objectives: The insidious presence of free oxygenated and nitrogen radicals in the human body has become a worrisome concern. These chemical species continue to plague the human cells, tissues and organs resulting in different pathophysiological conditions such as cancers and neurodegenerative disorders like Alzheimer’s disease and Parkinson’s disease amongst many other ailments. The search for novel pharmacological compounds with the aim of curbing the rising incidence of these radicals led the choice of vanillin in this present study. Methodology: Vanillin was separately subjected to a series of derivatization reactions namely, acetylation, O-demethylation, reduction and oxidation. The melting points, refractive indices and optical rotations of the lead compound and derivatives were obtained. The antioxidant activities of the five compounds were determined using the DPPH (2, 2-diphenyl-1-picrylhydrazyl hydrate) test. Comparison of the obtained antioxidant activities was done to determine if any improvements could be seen in the derivatives. Results: The identities of the derivatives have been revealed to be vanillyl acetate (E-1) (acetyl derivative), 3, 4-dihydroxy benzaldehyde or protocatechui aldehyde (E-2) (demethylated derivative), o-methoxy-p-methyl cyclohexan-1-ol (J-1) (reduced derivative) and vanillic acid (J-2) (oxidized derivative) respectively using the IR spectral technique. Vanillin, E-2 and J-2 derivatives gave marginal antioxidant activity of IC50 of 0.81, 0.84 and 0.0.85 µg/mL respectively while J-1 and E-1 demonstrated moderately significant IC50 of 0.59 and 0.63 µg/mL which compare favorably with 0.44 µg/mL elicited by Vitamin C (a standard antioxidant drug). It is pertinent to point out that the obtained reduced derivative is a substituted cycloalkanol (a saturated cyclic compound) instead of a substituted phenolic compound as was expected. Conclusion: The results from this study indicate that reduction and acetylation separately enhance the antioxidant activity of vanillin.","PeriodicalId":16735,"journal":{"name":"Journal of Pharmaceutical Research Science & Technology","volume":"131 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74929655","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}
Phytomedicines are used by humans since ancient civilizations and is now considered as an important part of traditional and alternative system of medicine. In recent time, phytomedicines have gained special attention based on the fact that a number of current medicines are derived from plant source. Phytochemicals exhibits lesser side effects and are potentially strong therapeutic agents. The global market for herbal drugs is increasing day by day. It has gained widespread acceptance due to its efficacy, accessibility, minimum toxicity, and cost effectiveness. However, solubility, stability and bioavailability are some of the major hindrances in the commercialization process of phytomedicines. Nanotechnology have been potentially productive in improving the solubility, stability, bioavailability, and bioactivity of phytomedicines. Development of nano-phytomedicines or attaching phytomedicines with polymers and modifying their surface properties and permeability have altogether influenced the bioavailability of phytochemicals. Novel formulations like solid lipid nanoparticles, micelles, niosomes, dendrimers, nanotube, liposomes, nano-emulsions nanospheres, phytosomes etc. Have been developed loaded with phytomedicines and have shown extraordinary result. This chapter extensively reviews phytomedicines based novel drug delivery systems having potential activity in different diseases like metabolic disorders, cardiovascular disorders, neurological disorders, viral diseases, cancers, inflammatory diseases and wound healing and lastly future prospect is discussed.
{"title":"Phytonutrients and Technological Development in Formulations","authors":"M. Jahangir","doi":"10.31531/jprst.1000159","DOIUrl":"https://doi.org/10.31531/jprst.1000159","url":null,"abstract":"Phytomedicines are used by humans since ancient civilizations and is now considered as an important part of traditional and alternative system of medicine. In recent time, phytomedicines have gained special attention based on the fact that a number of current medicines are derived from plant source. Phytochemicals exhibits lesser side effects and are potentially strong therapeutic agents. The global market for herbal drugs is increasing day by day. It has gained widespread acceptance due to its efficacy, accessibility, minimum toxicity, and cost effectiveness. However, solubility, stability and bioavailability are some of the major hindrances in the commercialization process of phytomedicines. Nanotechnology have been potentially productive in improving the solubility, stability, bioavailability, and bioactivity of phytomedicines. Development of nano-phytomedicines or attaching phytomedicines with polymers and modifying their surface properties and permeability have altogether influenced the bioavailability of phytochemicals. Novel formulations like solid lipid nanoparticles, micelles, niosomes, dendrimers, nanotube, liposomes, nano-emulsions nanospheres, phytosomes etc. Have been developed loaded with phytomedicines and have shown extraordinary result. This chapter extensively reviews phytomedicines based novel drug delivery systems having potential activity in different diseases like metabolic disorders, cardiovascular disorders, neurological disorders, viral diseases, cancers, inflammatory diseases and wound healing and lastly future prospect is discussed.","PeriodicalId":16735,"journal":{"name":"Journal of Pharmaceutical Research Science & Technology","volume":"80 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73909360","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}
Introduction: Herbal medicines are an important ingredient of traditional and alternative medicinal system and thus being used since ancient times. Owing to their characteristic of having lesser side effects and potential therapeutic effect they have drawn attention of pharmaceutical scientists from across the globe. Herbal medicines have now strongly captured a whooping US $62 billion market globally. Herbal medicines have been widely accepted of their potential to treat chronic diseases, low toxicity profile, cheap and wide availability etc. Methods: The Safety and efficacy of herbal drugs have played an important part in their successful commercialization. With the emergence and application of nanotechnology the bioavailability and bioactivity of herbal medicines have improved drastically. Results: Development of nano-phytomedicines by reducing their size to nano scale range, attaching it with polymers and by modifying their surface properties, solubility, permeability, eventually enhances the bioavailability of herbal formulations. Conclusion: Novel formulations like niosomes, liposomes, nanospheres, phytosomes etc. can be exploited in this area. However, novel nano-phytomedicines comes with its own pros and cons. This article extensively reviews herbal nano-medicines with its reported success and failures.
{"title":"Nanophytomedicine in Clinical Management: An Introductory Evidence-based Review","authors":"M. Jahangir","doi":"10.31531/jprst.1000158","DOIUrl":"https://doi.org/10.31531/jprst.1000158","url":null,"abstract":"Introduction: Herbal medicines are an important ingredient of traditional and alternative medicinal system and thus being used since ancient times. Owing to their characteristic of having lesser side effects and potential therapeutic effect they have drawn attention of pharmaceutical scientists from across the globe. Herbal medicines have now strongly captured a whooping US $62 billion market globally. Herbal medicines have been widely accepted of their potential to treat chronic diseases, low toxicity profile, cheap and wide availability etc. Methods: The Safety and efficacy of herbal drugs have played an important part in their successful commercialization. With the emergence and application of nanotechnology the bioavailability and bioactivity of herbal medicines have improved drastically. Results: Development of nano-phytomedicines by reducing their size to nano scale range, attaching it with polymers and by modifying their surface properties, solubility, permeability, eventually enhances the bioavailability of herbal formulations. Conclusion: Novel formulations like niosomes, liposomes, nanospheres, phytosomes etc. can be exploited in this area. However, novel nano-phytomedicines comes with its own pros and cons. This article extensively reviews herbal nano-medicines with its reported success and failures.","PeriodicalId":16735,"journal":{"name":"Journal of Pharmaceutical Research Science & Technology","volume":"497 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77073185","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}
While many diseases require an efficient drug delivery technology that has the ability to improve bioavailability and alleviate side effects, various types of gastroretentive drug delivery systems (GRDDS) have been developed in order to overcome the obstacles, which are related to a narrow absorption window, instability, site of action, side effects, and dosing frequency. In this context, microsponge and microsphere systems depict two different types of GRDDS, aiming to provide adequate time for active ingredients to be absorbed in the stomach despite the variation in releasing mechanisms of the entrapped ingredients. For the successful designing of these systems, it is essential to optimize the characterizations of the formulated microparticles by considering physiological, pharmaceutical, and patient-related factors, which have a dramatic impact on the efficacy. Consequently, they will demonstrate different behaviors at the desired site of action, determining which systems are showing superiority compared to others. However, each microparticle system has some advantages over the others, providing more options for researchers to ease the difficulties that exist with conventional oral dosage forms. Therefore, this review aims to shed the light on critical factors that have significant impacts on microsponge and microsphere systems and addresses their advantages and disadvantages, providing an understanding of these criteria in order to optimize the drug systems.
{"title":"The Impact of Microsponge and Microsphere on Improving Oral Bioavailability of Medications: A Short Review","authors":"Yasir Alshehry","doi":"10.31531/jprst.1000155","DOIUrl":"https://doi.org/10.31531/jprst.1000155","url":null,"abstract":"While many diseases require an efficient drug delivery technology that has the ability to improve bioavailability and alleviate side effects, various types of gastroretentive drug delivery systems (GRDDS) have been developed in order to overcome the obstacles, which are related to a narrow absorption window, instability, site of action, side effects, and dosing frequency. In this context, microsponge and microsphere systems depict two different types of GRDDS, aiming to provide adequate time for active ingredients to be absorbed in the stomach despite the variation in releasing mechanisms of the entrapped ingredients. For the successful designing of these systems, it is essential to optimize the characterizations of the formulated microparticles by considering physiological, pharmaceutical, and patient-related factors, which have a dramatic impact on the efficacy. Consequently, they will demonstrate different behaviors at the desired site of action, determining which systems are showing superiority compared to others. However, each microparticle system has some advantages over the others, providing more options for researchers to ease the difficulties that exist with conventional oral dosage forms. Therefore, this review aims to shed the light on critical factors that have significant impacts on microsponge and microsphere systems and addresses their advantages and disadvantages, providing an understanding of these criteria in order to optimize the drug systems.","PeriodicalId":16735,"journal":{"name":"Journal of Pharmaceutical Research Science & Technology","volume":"49 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74605956","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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