Pub Date : 2020-02-12DOI: 10.2174/2210303109666190723145209
Sivaram Nallamolu, V. Jayanti, Mallikarjun Chitneni, L. Y. Khoon, P. Kesharwani
Andrographolide has potent anticancer and antimicrobial activity; however, its clinical application has been limited due to its poor water solubility as well as lack of appropriate formulation. The objective of this investigation was to formulate Self–Micro Emulsifying Drug Delivery System (SMEDDS) of andrographolide and explore its oral drug delivery aptitudes. Andrographolide SMEDDS was optimized by ternary phase approach and studied for various in vitro characteristics: Particle size, electron microscopy, polydispersity index, surface charge, dilution effect, pH stability, freeze-thaw effect, dissolution profile and stability studies. Further, antimicrobial and cytotoxic performance of andrographolide SMEDDS were evaluated in MCF–7 breast cancer cell lines and methicillin-resistant microorganisms, respectively. An optimized SMEDDS formulation of andrographolide was successfully prepared and evaluated for its drug delivery potential. The solubility of andrographolide in the developed SMEDDS formulation was increased significantly, and the drug loading was enough for making this drug clinically applicable. The andrographolide SMEDDS formulation competitively inhibited the growth of microorganisms and showed enhanced anti–microbial activity against MRSA microorganisms. The SMEDDS strategy represents one of the best approaches to deliver andrographolide via oral route, while resolving its solubility limitations.
{"title":"Self-micro Emulsifying Drug Delivery System “SMEDDS” for Efficient Oral Delivery of Andrographolide","authors":"Sivaram Nallamolu, V. Jayanti, Mallikarjun Chitneni, L. Y. Khoon, P. Kesharwani","doi":"10.2174/2210303109666190723145209","DOIUrl":"https://doi.org/10.2174/2210303109666190723145209","url":null,"abstract":"\u0000\u0000Andrographolide has potent anticancer and antimicrobial activity; however, its\u0000clinical application has been limited due to its poor water solubility as well as lack of appropriate formulation.\u0000The objective of this investigation was to formulate Self–Micro Emulsifying Drug Delivery\u0000System (SMEDDS) of andrographolide and explore its oral drug delivery aptitudes.\u0000\u0000\u0000\u0000Andrographolide SMEDDS was optimized by ternary phase approach and studied for various\u0000in vitro characteristics: Particle size, electron microscopy, polydispersity index, surface charge, dilution\u0000effect, pH stability, freeze-thaw effect, dissolution profile and stability studies. Further, antimicrobial\u0000and cytotoxic performance of andrographolide SMEDDS were evaluated in MCF–7 breast cancer cell\u0000lines and methicillin-resistant microorganisms, respectively.\u0000\u0000\u0000\u0000An optimized SMEDDS formulation of andrographolide was successfully prepared and evaluated\u0000for its drug delivery potential. The solubility of andrographolide in the developed SMEDDS formulation\u0000was increased significantly, and the drug loading was enough for making this drug clinically\u0000applicable. The andrographolide SMEDDS formulation competitively inhibited the growth of microorganisms\u0000and showed enhanced anti–microbial activity against MRSA microorganisms.\u0000\u0000\u0000\u0000The SMEDDS strategy represents one of the best approaches to deliver andrographolide\u0000via oral route, while resolving its solubility limitations.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42864582","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 : 2019-11-30DOI: 10.2174/2210303109666190619103230
A. Abd-Elrazek, Tayseer Elnawawy
Olanzapine (OLZ) is an atypical psychotic agent; the poor bioavailability of olanzapine is the most important issue in its treatment. The present work was carried out to evaluate the oral form of olanzapine solid lipid nanoparticles (OLZ-SLN) to overcome its poor bioavailability and compare between the effect of different doses of OLZ and OLZ-SLN on ketamineinduced schizophrenic-like symptoms. The study was extended to evaluate the adverse effects of subchronic administration of these doses of OLZ and its SLN.OLZ-SLN was prepared by hot homogenization, particle size, zeta potential and in vitro release and entrapping efficiency studies were performed. In order to assess the effective dose in the treatment of schizophrenia, the effect of different doses of OLZ and OLZ-SLN on open field was assessed and passive avoidance tests were carried out. The test was performed to examine the effects of excitatory and inhibitory amino acids, as well as dopamine and serotonin levels in the brain regions.The new oral formula showed high stability and sustained release. The administration of low and high dose of OLZ-SLN equivalent to (1/10 and 1/20 from the therapeutic dose before ketamine attenuated the behavioral abnormalities by blocking the effect of ketamine-induced increase in glutamate, dopamine and serotonin levels and enhanced apoptosis were studied in the brain areas. In addition, the sub-chronic treatment with OLZ-SLN showed no adverse effect while the treatment with OLZ free form did.
{"title":"The Effect of Minor Doses of Olanzapine-Solid Lipid Nanoparticles on an Animal Model of Schizophrenia (Neurochemical and Behavioral Study) and the Side Effect","authors":"A. Abd-Elrazek, Tayseer Elnawawy","doi":"10.2174/2210303109666190619103230","DOIUrl":"https://doi.org/10.2174/2210303109666190619103230","url":null,"abstract":"Olanzapine (OLZ) is an atypical psychotic agent; the poor bioavailability of olanzapine is the most important issue in its treatment. The present work was carried out to evaluate the oral form of olanzapine solid lipid nanoparticles (OLZ-SLN) to overcome its poor bioavailability and compare between the effect of different doses of OLZ and OLZ-SLN on ketamineinduced schizophrenic-like symptoms. The study was extended to evaluate the adverse effects of subchronic administration of these doses of OLZ and its SLN.OLZ-SLN was prepared by hot homogenization, particle size, zeta potential and in vitro release and entrapping efficiency studies were performed. In order to assess the effective dose in the treatment of schizophrenia, the effect of different doses of OLZ and OLZ-SLN on open field was assessed and passive avoidance tests were carried out. The test was performed to examine the effects of excitatory and inhibitory amino acids, as well as dopamine and serotonin levels in the brain regions.The new oral formula showed high stability and sustained release. The administration of low and high dose of OLZ-SLN equivalent to (1/10 and 1/20 from the therapeutic dose before ketamine attenuated the behavioral abnormalities by blocking the effect of ketamine-induced increase in glutamate, dopamine and serotonin levels and enhanced apoptosis were studied in the brain areas. In addition, the sub-chronic treatment with OLZ-SLN showed no adverse effect while the treatment with OLZ free form did.","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42690349","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 : 2019-11-30DOI: 10.2174/2210303109666190319165209
Ravi Patel
Dendrimers, a new class of synthetic polymers proved themselves very useful tools for biomedical application due to their unique characteristics including water solubility, uniform size and shape, defined molecular weight, multivalency, biological compatibility and internal cavities. The hydrophobicity of a drug molecule creates hurdles in the development of effective dosage form and presents insufficient drug delivery to the target site. Solubility enhancement is one of the key properties of a dendrimer. The hydrophobic drug molecules are entrapped in the cavities of a dendrimer by complexation and get solubilized in the aqueous solution. The present article contains information on dendrimer and its biomedical application such as API solubility. The detailed study presents year wise survey of different research articles, research papers, reviews and patents on dendrimer and its application in drug solubility.
{"title":"Role of Dendrimer in Drug Solubilisation - A Review","authors":"Ravi Patel","doi":"10.2174/2210303109666190319165209","DOIUrl":"https://doi.org/10.2174/2210303109666190319165209","url":null,"abstract":"\u0000\u0000Dendrimers, a new class of synthetic polymers proved themselves very useful\u0000tools for biomedical application due to their unique characteristics including water solubility, uniform\u0000size and shape, defined molecular weight, multivalency, biological compatibility and internal cavities.\u0000The hydrophobicity of a drug molecule creates hurdles in the development of effective dosage form and\u0000presents insufficient drug delivery to the target site.\u0000\u0000\u0000\u0000Solubility enhancement is one of the key properties of a dendrimer. The hydrophobic drug\u0000molecules are entrapped in the cavities of a dendrimer by complexation and get solubilized in the aqueous\u0000solution.\u0000\u0000\u0000\u0000The present article contains information on dendrimer and its biomedical application such\u0000as API solubility. The detailed study presents year wise survey of different research articles, research\u0000papers, reviews and patents on dendrimer and its application in drug solubility.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45631829","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 : 2019-11-30DOI: 10.2174/2210303109666190621144400
L. Singh, R. Tiwari, S. Verma, V. Sharma
Conventional approach of formulating a new dosage form is a comprehensive task and uses various sources like man, money, time and experimental efforts. The use of AI can help to obtain optimized pharmaceutical formulation with desired (best) attributes. AI minimizes the use of resources and increases the understanding of impact, of independent variable over desired dependent responses/variables. Thus, the aim of present work is to explore the use of Artificial intelligence in designing pharmaceutical products as well as the manufacturing process to get the pharmaceutical product of desired attributes with ease. The review is presenting various aspects of Artificial intelligence like Quality by Design (QbD) & Design of Experiment (DoE) to confirm the quality profile of drug product, reduce interactions among the input variables for the optimization, modelization and various simulation tools used in pharmaceutical manufacturing (scale up and production). Hence, the use of QbD approach in Artificial intelligence is not only useful in understanding the products or process but also helps in building an excellent and economical pharmaceutical product.
{"title":"The Future of Artificial Intelligence in Pharmaceutical Product Formulation","authors":"L. Singh, R. Tiwari, S. Verma, V. Sharma","doi":"10.2174/2210303109666190621144400","DOIUrl":"https://doi.org/10.2174/2210303109666190621144400","url":null,"abstract":"\u0000\u0000Conventional approach of formulating a new dosage form is a comprehensive\u0000task and uses various sources like man, money, time and experimental efforts. The use of AI can help\u0000to obtain optimized pharmaceutical formulation with desired (best) attributes. AI minimizes the use of\u0000resources and increases the understanding of impact, of independent variable over desired dependent\u0000responses/variables.\u0000\u0000\u0000\u0000Thus, the aim of present work is to explore the use of Artificial intelligence in designing\u0000pharmaceutical products as well as the manufacturing process to get the pharmaceutical product of desired\u0000attributes with ease. The review is presenting various aspects of Artificial intelligence like Quality\u0000by Design (QbD) & Design of Experiment (DoE) to confirm the quality profile of drug product, reduce\u0000interactions among the input variables for the optimization, modelization and various simulation tools\u0000used in pharmaceutical manufacturing (scale up and production).\u0000\u0000\u0000\u0000Hence, the use of QbD approach in Artificial intelligence is not only useful in understanding\u0000the products or process but also helps in building an excellent and economical pharmaceutical product.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46436708","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 : 2019-11-30DOI: 10.2174/2210303109666190614120556
R. Kaushik
The objective of the current research is systematic optimization and development of microemulsion preconcentrates to get better solubility that results in improvement of oral bioavailability profile of Telmisartan utilizing D-optimal mixture design. Solubility studies in a variety of lipidic ingredients and optimization of formulations were carried out for the development of liquid SMEDDS. D-optimal mixture design was utilized for assessing the interaction performance of desired responses (such as % cumulative drug release and globule size) and optimized using desirability approach. The optimized batch was evaluated for its % cumulative drug release and globule size performance for determining the dissolution rate and oral bioavailability of drug. The optimized batch (F-8), which contained 10% oil (Capmul MCM EP), 45% surfactant (Labrasol) and 45% co-surfactant (Transcutol HP) resulted in desired qualities of measured responses with 84.6nm globule size and 98.5% drug release within 15 minutes. Optimized SMEDDS showed brilliant goodness of fit between drug release. Stability studies indicated stability of the optimized SMEDDS batch over 3-month storage at 40°C/75% RH and improved dissolution rate in contrast to pure API. The optimized SMEDDS showed no impact of in vitro lipolysis on drug release. Developed and optimized SMEDDS showed improved in vitro dissolution rate and dissolution profile in contrast to pure drug. These investigations further confirm dose reduction in SMEDDS by gaining an equivalent therapeutic profile with non-SMEDDS formulation. This research work successfully shows the potential usage of SMEDDS for delivery of BCS-II class drugs.
{"title":"Development, Optimization, Characterization and Impact of In vitro Lipolysis on Drug Release of Telmisartan Loaded SMEDDS","authors":"R. Kaushik","doi":"10.2174/2210303109666190614120556","DOIUrl":"https://doi.org/10.2174/2210303109666190614120556","url":null,"abstract":"\u0000\u0000The objective of the current research is systematic optimization and development\u0000of microemulsion preconcentrates to get better solubility that results in improvement of oral bioavailability\u0000profile of Telmisartan utilizing D-optimal mixture design.\u0000\u0000\u0000\u0000Solubility studies in a variety of lipidic ingredients and optimization of formulations were\u0000carried out for the development of liquid SMEDDS. D-optimal mixture design was utilized for assessing\u0000the interaction performance of desired responses (such as % cumulative drug release and globule\u0000size) and optimized using desirability approach. The optimized batch was evaluated for its % cumulative\u0000drug release and globule size performance for determining the dissolution rate and oral bioavailability\u0000of drug.\u0000\u0000\u0000\u0000The optimized batch (F-8), which contained 10% oil (Capmul MCM EP), 45% surfactant\u0000(Labrasol) and 45% co-surfactant (Transcutol HP) resulted in desired qualities of measured responses\u0000with 84.6nm globule size and 98.5% drug release within 15 minutes. Optimized SMEDDS showed brilliant\u0000goodness of fit between drug release. Stability studies indicated stability of the optimized\u0000SMEDDS batch over 3-month storage at 40°C/75% RH and improved dissolution rate in contrast to\u0000pure API. The optimized SMEDDS showed no impact of in vitro lipolysis on drug release.\u0000\u0000\u0000\u0000Developed and optimized SMEDDS showed improved in vitro dissolution rate and dissolution\u0000profile in contrast to pure drug. These investigations further confirm dose reduction in SMEDDS\u0000by gaining an equivalent therapeutic profile with non-SMEDDS formulation. This research work successfully\u0000shows the potential usage of SMEDDS for delivery of BCS-II class drugs.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45433832","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 : 2019-11-30DOI: 10.2174/2210303109666190708151137
Kuldeep Singh, S. Jain, K. Razdan, Harmanpreet Singh, N. Sahajpal, Harjeet Singh, Amrinder Singh, Shubham Thakur
Ferrous ascorbate (FA) is preferentially absorbed from the upper gastrointestinal (GI) track, and has low bioavailability due to less residence time of FA in upper GI track. In addition, FA has low solubility and stability at higher pH. The aim of this study was to prepare gastro-retentive tablets of FA in order to increase its gastric residence time and hence, bioavailability. Floating tablets of FA were prepared by wet granulation method using different retarding polymers, Povidone K30 as binder and sodium bicarbonate as effervescent agent. The prepared floating tablets were compared with immediate release (IR) tablets and characterized in detail for in vitro and in vivo studies. In-vitro drug release study of the optimized batch showed 96% drug release in 12 h in 0.1 N HCl. The mechanism of drug release from the floating tablets was non-fickian and release kinetics was best fit in peppas model. The gastric retention time of optimized was found to be significantly increased (6 h) in comparison with IR tablet (<1h). Further, bioavailability was also found significantly increased (>70%) in comparison with IR tablet (15-30%). X-ray studies carried on healthy rabbits suggested that the optimized batch remained buoyant in gastric contents up to 6 h and pharmacokinetic study showed sustained released behaviour of optimized batch in comparison to conventional IR tablet. Floating tablet of FA improved the bioavailability of iron by increasing its gastric residence time, hence it could be a better approach for treating iron deficiency and help in improving the patient compliance than IR tablets.
{"title":"Formulation and Evaluation of Ferrous Ascorbate Floating Tablets for the Treatment of Anaemia","authors":"Kuldeep Singh, S. Jain, K. Razdan, Harmanpreet Singh, N. Sahajpal, Harjeet Singh, Amrinder Singh, Shubham Thakur","doi":"10.2174/2210303109666190708151137","DOIUrl":"https://doi.org/10.2174/2210303109666190708151137","url":null,"abstract":"\u0000\u0000Ferrous ascorbate (FA) is preferentially absorbed from the upper\u0000gastrointestinal (GI) track, and has low bioavailability due to less residence time of FA in upper GI\u0000track. In addition, FA has low solubility and stability at higher pH. The aim of this study was to prepare\u0000gastro-retentive tablets of FA in order to increase its gastric residence time and hence, bioavailability.\u0000\u0000\u0000\u0000Floating tablets of FA were prepared by wet granulation method using different retarding\u0000polymers, Povidone K30 as binder and sodium bicarbonate as effervescent agent. The prepared floating\u0000tablets were compared with immediate release (IR) tablets and characterized in detail for in vitro and in\u0000vivo studies.\u0000\u0000\u0000\u0000In-vitro drug release study of the optimized batch showed 96% drug release in 12 h in 0.1 N\u0000HCl. The mechanism of drug release from the floating tablets was non-fickian and release kinetics was\u0000best fit in peppas model. The gastric retention time of optimized was found to be significantly increased\u0000(6 h) in comparison with IR tablet (<1h). Further, bioavailability was also found significantly increased\u0000(>70%) in comparison with IR tablet (15-30%). X-ray studies carried on healthy rabbits suggested that\u0000the optimized batch remained buoyant in gastric contents up to 6 h and pharmacokinetic study showed\u0000sustained released behaviour of optimized batch in comparison to conventional IR tablet.\u0000\u0000\u0000\u0000Floating tablet of FA improved the bioavailability of iron by increasing its gastric residence\u0000time, hence it could be a better approach for treating iron deficiency and help in improving the\u0000patient compliance than IR tablets.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43986076","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 : 2019-11-30DOI: 10.2174/2210303109666190529123029
D. Sharma, A. Sharma, R. Garg
Background: Drug delivery across the buccal mucosal epithelium membrane is one of the promising routes to treat various recurrent ailments of the oral cavity. Aphthous stomatitis is an inflammatory oro-mucosal disorder associated with mucous membranes of mouth, cheek, lips, tongue or gingival region. Benzydamine Hydrochloride was designated as a drug of choice by virtue of its anesthetic, antimicrobial, analgesic, anti-inflammatory and antibacterial action. The medication administration through the buccal route is very testing because of restricted absorption area, shorter residence time and movements of the target region. Objective: To prepare mucoadhesive buccal gel of Benzydamine Hydrochloride and assess the effects of various HPMC polymer on in vitro and ex vivo performance with the assumption to extend the residence period and achieve maximum drug release in a sustained manner at the target region. Methods: Mucoadhesive buccal gels were formulated by utilizing various HPMC grades that served as rate controlling and mucoadhesive polymer. A total of 24 preparations were formulated and subjected to physicochemical evaluation and characterization. Results: It was found that the physicochemical parameters varied according to the polymer type and concentration used. Eight formulations were exposed to ex vivo study by virtue of maximum in vitro permeation and mucoadhesion properties. Because of higher ex vivo drug permeation and mucoadhesion, F24 was considered as the final optimized formulation. FTIR and DSC established compatibility between the drug and excipient. The amorphous nature of the drug within the optimized formulation was further unveiled by XRD study. Conclusion: The developed buccal gel has a great prospective in contrast to marketed conventional preparation for treating aphthous stomatitis.
{"title":"Preparation, Physicochemical Evaluation and Characterization of Mucoadhesive Buccal Gels Impregnated with Benzydamine Hydrochloride for the Effective Treatment of Aphthous Stomatitis: Effect of Different Grades of HPMC Polymer on In vitro and Ex vivo Performance","authors":"D. Sharma, A. Sharma, R. Garg","doi":"10.2174/2210303109666190529123029","DOIUrl":"https://doi.org/10.2174/2210303109666190529123029","url":null,"abstract":"\u0000\u0000Background: Drug delivery across the buccal mucosal epithelium membrane is one of the\u0000promising routes to treat various recurrent ailments of the oral cavity. Aphthous stomatitis is an inflammatory\u0000oro-mucosal disorder associated with mucous membranes of mouth, cheek, lips, tongue or\u0000gingival region. Benzydamine Hydrochloride was designated as a drug of choice by virtue of its anesthetic,\u0000antimicrobial, analgesic, anti-inflammatory and antibacterial action. The medication administration\u0000through the buccal route is very testing because of restricted absorption area, shorter residence time\u0000and movements of the target region.\u0000\u0000Objective: To prepare mucoadhesive buccal gel of Benzydamine Hydrochloride and assess the effects\u0000of various HPMC polymer on in vitro and ex vivo performance with the assumption to extend the residence\u0000period and achieve maximum drug release in a sustained manner at the target region.\u0000\u0000Methods: Mucoadhesive buccal gels were formulated by utilizing various HPMC grades that served as\u0000rate controlling and mucoadhesive polymer. A total of 24 preparations were formulated and subjected\u0000to physicochemical evaluation and characterization.\u0000\u0000Results: It was found that the physicochemical parameters varied according to the polymer type and\u0000concentration used. Eight formulations were exposed to ex vivo study by virtue of maximum in vitro\u0000permeation and mucoadhesion properties. Because of higher ex vivo drug permeation and mucoadhesion,\u0000F24 was considered as the final optimized formulation. FTIR and DSC established compatibility\u0000between the drug and excipient. The amorphous nature of the drug within the optimized formulation\u0000was further unveiled by XRD study.\u0000\u0000Conclusion: The developed buccal gel has a great prospective in contrast to marketed conventional\u0000preparation for treating aphthous stomatitis.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47925462","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 : 2019-10-31DOI: 10.2174/2210303109666190520081552
R. K. Dhamoon, R. Goyal, H. Popli, Madhu Gupta
Onychomycosis is a nail fungal infection which accounts for 50% of the nail diseases and is characterized by disfigurement and discoloration of nails. The current therapy includes oral and topical formulations both of which come with their own drawbacks. This has left a room for developing patient- compliant novel strategies which can facilitate drug delivery deeper into the nails effectively. The main objective of the present work was to develop and evaluate in situ gelling thermosensitive hydrogel as an aqueous nail lacquer for the treatment of onychomycosis. The idea was to enhance permeation of Luliconazole into the nail while simultaneously solubilizing it in a hydrophilic formulation. The sample of Luliconazole was authenticated using modern analytical techniques. The hydrogel- nail lacquer was prepared using poloxamer Pluronic F127. The formulation was evaluated in terms of drying time, viscosity, non- volatile content, pH, transition temperature, etc. In vitro study was done to check the drug release while determining release kinetics. In vitro transungual permeation study was done to check drug permeation through porcine hoof membrane. Stability studies were conducted to ensure formulation stability. The results confirmed a stable formulation with enhanced permeation through porcine hoof membrane. The results support the potential use of in situ gelling thermo-sensitive hydrogels as a novel transungual formulation in the treatment of onychomycosis with a slight improvement in water resistance.
{"title":"Luliconazole-Loaded Thermosensitive Hydrogel as Aqueous based Nail Lacquer for the Treatment of Onychomycosis","authors":"R. K. Dhamoon, R. Goyal, H. Popli, Madhu Gupta","doi":"10.2174/2210303109666190520081552","DOIUrl":"https://doi.org/10.2174/2210303109666190520081552","url":null,"abstract":"\u0000\u0000Onychomycosis is a nail fungal infection which accounts for 50% of the nail\u0000diseases and is characterized by disfigurement and discoloration of nails. The current therapy includes\u0000oral and topical formulations both of which come with their own drawbacks. This has left a room for\u0000developing patient- compliant novel strategies which can facilitate drug delivery deeper into the nails\u0000effectively.\u0000\u0000\u0000\u0000The main objective of the present work was to develop and evaluate in situ gelling thermosensitive\u0000hydrogel as an aqueous nail lacquer for the treatment of onychomycosis. The idea was to\u0000enhance permeation of Luliconazole into the nail while simultaneously solubilizing it in a hydrophilic\u0000formulation.\u0000\u0000\u0000\u0000The sample of Luliconazole was authenticated using modern analytical techniques. The hydrogel-\u0000nail lacquer was prepared using poloxamer Pluronic F127. The formulation was evaluated in\u0000terms of drying time, viscosity, non- volatile content, pH, transition temperature, etc. In vitro study was\u0000done to check the drug release while determining release kinetics. In vitro transungual permeation study\u0000was done to check drug permeation through porcine hoof membrane. Stability studies were conducted\u0000to ensure formulation stability.\u0000\u0000\u0000\u0000The results confirmed a stable formulation with enhanced permeation through porcine hoof\u0000membrane.\u0000\u0000\u0000\u0000The results support the potential use of in situ gelling thermo-sensitive hydrogels as a\u0000novel transungual formulation in the treatment of onychomycosis with a slight improvement in water\u0000resistance.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49426003","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 : 2019-10-31DOI: 10.2174/2210303109666190617170026
Lisa Engio and Remigius U. Agu
Peptide Hormones (PH) are mainly administered as parenteral injections due to their peculiar physicochemical properties, and susceptibility to enzymatic degradation after oral administration. With invasive routes, however, patient safety, acceptability, and compliance become a concern, especially when a patient has a chronic condition that requires repeated injections. The delivery of peptide hormones via the nasal route has gained momentum over the last few decades as a noninvasive alternative to parenteral injections and commercially available nasal liquid products. The aim of this paper was to review: (1) The benefits and limitations of nasal powder products, (2) Formulation strategies to enhance nasal delivery of peptide hormone drugs, (3) Nasal powder devices, and (4) Future perspectives of therapeutic nasal powders. The drugs examined specifically include calcitonin, desmopressin, ghrelin, glucagon, human growth hormone, insulin, octreotide, and oxytocin. Nasal delivery of peptide hormones using powders was reviewed with the following databases: EBSCO, PUBMED, Web of Science, ClinicalTrials.gov, and EU Clinical Trials Register. Nasal powders are a promising drug delivery system that may be safer and more effective than traditional injections and presently marketed nasal liquids for peptide hormone drugs. With sustained interest and growing body of supporting evidence, a range of nasal powders for systemic delivery of these drugs and delivery devices can be expected to enter the market in the future and offer more options to patients
肽激素（PH）由于其独特的物理化学性质和口服后易被酶降解，主要作为胃肠外注射给药。然而，对于侵入性途径，患者的安全性、可接受性和依从性变得至关重要，尤其是当患者患有需要反复注射的慢性病时。在过去的几十年里，通过鼻腔途径输送肽激素作为非肠道注射和市售鼻腔液体产品的非侵入性替代品获得了发展势头。本文的目的是综述：（1）鼻粉产品的优点和局限性，（2）增强肽激素药物鼻腔给药的配方策略，（3）鼻粉装置，以及（4）治疗性鼻粉的未来前景。具体检查的药物包括降钙素、去氨加压素、胃促生长素、胰高血糖素、人类生长激素、胰岛素、奥曲肽和催产素。通过以下数据库对使用粉末的肽激素鼻腔给药进行了审查：EBSCO、PUBMED、Web of Science、ClinicalTrials.gov和欧盟临床试验注册。鼻用粉末是一种很有前途的药物给药系统，可能比传统注射和目前市场上用于肽激素药物的鼻腔液体更安全、更有效。随着人们的持续兴趣和越来越多的支持证据，一系列用于系统递送这些药物和递送设备的鼻粉有望在未来进入市场，并为患者提供更多选择
{"title":"Systemic Delivery of Peptide Hormones Using Nasal Powders: Strategies and Future Perspectives","authors":"Lisa Engio and Remigius U. Agu","doi":"10.2174/2210303109666190617170026","DOIUrl":"https://doi.org/10.2174/2210303109666190617170026","url":null,"abstract":"\u0000\u0000Peptide Hormones (PH) are mainly administered as parenteral injections due\u0000to their peculiar physicochemical properties, and susceptibility to enzymatic degradation after oral administration.\u0000With invasive routes, however, patient safety, acceptability, and compliance become a\u0000concern, especially when a patient has a chronic condition that requires repeated injections. The delivery\u0000of peptide hormones via the nasal route has gained momentum over the last few decades as a noninvasive\u0000alternative to parenteral injections and commercially available nasal liquid products.\u0000\u0000\u0000\u0000The aim of this paper was to review:\u0000(1) The benefits and limitations of nasal powder products,\u0000(2) Formulation strategies to enhance nasal delivery of peptide hormone drugs,\u0000(3) Nasal powder devices, and\u0000(4) Future perspectives of therapeutic nasal powders. The drugs examined specifically include calcitonin,\u0000desmopressin, ghrelin, glucagon, human growth hormone, insulin, octreotide, and oxytocin.\u0000\u0000\u0000\u0000Nasal delivery of peptide hormones using powders was reviewed with the following databases:\u0000EBSCO, PUBMED, Web of Science, ClinicalTrials.gov, and EU Clinical Trials Register.\u0000\u0000\u0000\u0000Nasal powders are a promising drug delivery system that may be safer and more effective than\u0000traditional injections and presently marketed nasal liquids for peptide hormone drugs.\u0000\u0000\u0000\u0000With sustained interest and growing body of supporting evidence, a range of nasal powders\u0000for systemic delivery of these drugs and delivery devices can be expected to enter the market in the\u0000future and offer more options to patients\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46583460","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 : 2019-08-31DOI: 10.2174/2210303109666190508082009
K. Pawar, R. Gadhave, Swati Waydande, P. Pawar
Fungi are the heterotrophic eukaryotic organisms which are useful as they causes the biodegradation. There are still some harmful species like yeasts, molds and dermatophytes which cause the infections. As the fungi are eukaryotics, they do not respond to the antibiotic therapy due to the limitations associated with the traditional antibiotic therapies. There are several antifungal agents introduced to treat such infections. These antifungal agents posses severe problems like drug resistance and toxicity due to the higher dose which comprises the need for newer alternatives over conventional dosage forms. Novel drug delivery systems proved to be a better approach to enhance the effectiveness of the antifungals and enhance patient compliance by reducing the adverse effect. This review focused on the general information about fungal infections, types and mechanism of action of antifungal agents and overview of formulation approaches such as vesicular system, colloidal system, nanoparticulate system and in situ gelling which are often studied for antifungal treatments. We concluded that the novel drug delivery systems are the essential techniques for delivering the antifungal agents to their target site with desired concentration. Moreover, the researchers focused on these novel drug deliveries which mainly concentrate on controlling & sustaining the release of antifungal agents.
{"title":"Recent Trends in Antifungal Agents: A Reference to Formulation, Characterization and Applications","authors":"K. Pawar, R. Gadhave, Swati Waydande, P. Pawar","doi":"10.2174/2210303109666190508082009","DOIUrl":"https://doi.org/10.2174/2210303109666190508082009","url":null,"abstract":"\u0000\u0000 Fungi are the heterotrophic eukaryotic organisms which are\u0000useful as they causes the biodegradation. There are still some harmful species like yeasts, molds and dermatophytes\u0000which cause the infections. As the fungi are eukaryotics, they do not respond to the antibiotic\u0000therapy due to the limitations associated with the traditional antibiotic therapies. There are several antifungal\u0000agents introduced to treat such infections. These antifungal agents posses severe problems like drug\u0000resistance and toxicity due to the higher dose which comprises the need for newer alternatives over\u0000conventional dosage forms. Novel drug delivery systems proved to be a better approach to enhance the\u0000effectiveness of the antifungals and enhance patient compliance by reducing the adverse effect.\u0000\u0000\u0000\u0000This review focused on the general information about fungal infections, types and mechanism\u0000of action of antifungal agents and overview of formulation approaches such as vesicular system, colloidal\u0000system, nanoparticulate system and in situ gelling which are often studied for antifungal treatments.\u0000\u0000\u0000\u0000We concluded that the novel drug delivery systems are the essential techniques for delivering\u0000the antifungal agents to their target site with desired concentration. Moreover, the researchers focused\u0000on these novel drug deliveries which mainly concentrate on controlling & sustaining the release\u0000of antifungal agents.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44096674","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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